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WO2018207947A1 - Polysaccharide-containing stick-shaped base material - Google Patents

Polysaccharide-containing stick-shaped base material Download PDF

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Publication number
WO2018207947A1
WO2018207947A1 PCT/JP2018/018558 JP2018018558W WO2018207947A1 WO 2018207947 A1 WO2018207947 A1 WO 2018207947A1 JP 2018018558 W JP2018018558 W JP 2018018558W WO 2018207947 A1 WO2018207947 A1 WO 2018207947A1
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WIPO (PCT)
Prior art keywords
group
acid
extract
stick
gly
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PCT/JP2018/018558
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French (fr)
Japanese (ja)
Inventor
鷹行 井本
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Nissan Chemical Corp
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Nissan Chemical Corp
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Priority to JP2019517738A priority Critical patent/JPWO2018207947A1/en
Publication of WO2018207947A1 publication Critical patent/WO2018207947A1/en
Anticipated expiration legal-status Critical
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/46Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing sulfur
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64Proteins; Peptides; Derivatives or degradation products thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin

Definitions

  • the present invention relates to a stick-shaped substrate containing a lipid peptide-type compound, and in particular, a stick-shaped substrate that can have a breaking strength required as a stick-shaped substrate even if the amount of the lipid peptide-type compound is reduced.
  • materials e.g.
  • the aqueous solid composition provides a high refreshing feeling when applied to the skin, etc., and has no stickiness after use as compared to the oily solid composition, so that it has a smooth use feeling.
  • a variety of products are marketed and proposed.
  • As an aqueous solid composition conventionally, a solid oil-in-water makeup cosmetic (Patent Document 1) containing water, fatty acid soap, oil and powder, an alkyl and / or alkenyl oligoglycoside, an oily substance, and a nonionic emulsifier
  • Patent Document 2 A stick-like water-based cosmetic
  • an aqueous gel composition is mentioned as a kind of aqueous solid composition.
  • various compounds such as a polymer gelling agent and a low molecular gelling agent have been proposed.
  • lipid peptide type low molecular gelling agents that have high biological safety and are expected to be developed into medical materials have been proposed.
  • the stick-shaped substrate described in Patent Document 3 uses about 5% by mass of the lipid peptide type compound based on the total mass of the stick-shaped substrate.
  • the lipid peptide type compound is expensive, and therefore, A stick-like substrate capable of reducing the amount of lipid peptide type compound is desired. Accordingly, an object of the present invention is to provide a stick-like substrate that can have the breaking strength required as a stick-like substrate even if the amount of the lipid peptide type compound is reduced.
  • lipid peptide type compound comprising a low-molecular-weight lipid peptide or a pharmaceutically usable salt thereof and water as main constituent components
  • a specific surfactant and a specific thickening agent are blended to have the breaking strength required as a stick-like base material even if the amount of lipid peptide type compound is reduced.
  • the present invention was completed.
  • the present invention provides the first aspect as follows: One or more surfactants selected from the group consisting of betaine compounds and ethylene glycol alkyl ethers; water and, A lipid peptide type compound comprising at least one of the compounds represented by the following formulas (1) to (3) or a pharmaceutically usable salt thereof; At least one saturated or unsaturated monohydric alcohol having 8 to 30 carbon atoms; One or more thickeners selected from the group consisting of alginic acid derivatives and carrageenan, The present invention relates to a stick-like substrate.
  • R 1 represents an aliphatic group having 9 to 23 carbon atoms
  • R 2 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms which may have a branched chain having 1 or 2 carbon atoms
  • R 3 represents a — (CH 2 ) n —X group, n represents a number of 1 to 4, X represents an amino group, a guanidino group, a —CONH 2 group, or 1 to 3 nitrogen atoms.
  • R 4 represents an aliphatic group having 9 to 23 carbon atoms
  • R 5 to R 7 each independently represents a hydrogen atom or a carbon atom having a branched chain having 1 or 2 carbon atoms.
  • R 8 represents an aliphatic group having 9 to 23 carbon atoms
  • R 9 to R 12 each independently represents a hydrogen atom, or a carbon atom number that can have a branched chain having 1 or 2 carbon atoms.
  • n represents an -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3
  • X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3
  • This represents a 5-membered ring or 6-membered ring which may have one or a condensed heterocyclic ring composed of a 5-membered ring and a 6-membered ring.
  • the present invention further relates to the stick-like substrate according to the first aspect, further comprising 1,2-alkanediol or 1,3-alkanediol.
  • the present invention relates to the stick-shaped substrate according to the third aspect, in which the alginic acid derivative is an alginate polyhydric alcohol ester.
  • the thickener is included in a proportion of 0.1 to 1.0% by mass based on the total mass of the stick-like substrate.
  • the present invention relates to the stick-like substrate described in one.
  • the present invention relates to the stick-like substrate according to any one of the third to fifth aspects, wherein the betaine compound is sulfate-type betaine.
  • the monohydric alcohol is one or more compounds selected from the group consisting of myristyl alcohol, cetanol, stearyl alcohol, and behenyl alcohol, according to any one of the first to sixth aspects.
  • This relates to a stick-like substrate.
  • any one of the first aspect to the seventh aspect, wherein the lipid peptide type compound is contained at a ratio of 0.1 to 2% by mass based on the total mass of the stick-like substrate. It relates to the stick-like base material described in one.
  • the stick-shaped base material which can have the breaking strength calculated
  • the use of a specific surfactant and a specific thickener reduces the amount of lipid peptide type compound based on the total mass of the substrate. Even when the content is less than or equal to mass%, it may have a breaking strength required for a stick-like substrate.
  • the lipid peptide compound contained in the stick-like substrate of the present invention is a very safe artificial low molecular weight compound composed only of lipid and peptide.
  • the compound can form an aqueous gel without using a crosslinking agent or the like required for forming a synthetic polymer type gel that has been proposed in the past. The problem of remaining unreacted materials such as cross-linking agents does not occur.
  • various components contained as additives in the stick-shaped substrate of the present invention are general-purpose additives as additives for foods, cosmetics, and pharmaceuticals.
  • the stick-shaped substrate of the present invention has high biological safety, and is particularly useful in the above applications from the viewpoint of safety required for pharmaceuticals and cosmetics.
  • the stick-like base material of the present invention is expected to be a base material having a good refreshing feeling when applied to human skin, etc. It is very useful as a stick-like base material for cosmetics and cosmetics.
  • the present invention relates to one or more surfactants selected from the group consisting of betaine compounds and ethylene glycol alkyl ethers, water, compounds represented by the following formulas (1) to (3), or pharmaceuticals thereof.
  • a lipid peptide-type compound comprising at least one of the salts that can be used in the above, 1,2-alkanediol or 1,3-alkanediol, and at least one saturated or unsaturated monovalent group having 8 to 30 carbon atoms.
  • the present invention relates to a stick-like substrate comprising alcohol, one or more thickeners selected from the group consisting of alginic acid derivatives and carrageenan, and optionally other additives.
  • each component will be described.
  • the lipid peptide type compound used in the stick-shaped substrate of the present invention is a compound (lipid peptide) represented by the following formulas (1) to (3) or a pharmaceutically usable salt thereof (hydrophobic site).
  • a low molecular compound having a lipid part and a peptide part which is a hydrophilic part) can be used.
  • R 1 represents an aliphatic group having 9 to 23 carbon atoms, and preferably R 1 is a straight chain having 11 to 23 carbon atoms which may have 0 to 2 unsaturated bonds.
  • An aliphatic group is desirable.
  • Specific examples of the lipid moiety (acyl group) composed of a carbonyl group adjacent to R 1 include lauroyl group, dodecylcarbonyl group, myristoyl group, tetradecylcarbonyl group, palmitoyl group, margaroyl group, oleoyl group, and elideoyl group.
  • Examples include lauroyl group, myristoyl group, palmitoyl group, margaroyl group, stearoyl group, oleoyl group, elidoyl group, and behenoyl group.
  • R 2 contained in the peptide part represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms which may have a branched chain having 1 or 2 carbon atoms.
  • the alkyl group having 1 to 4 carbon atoms that may have a branched chain having 1 or 2 carbon atoms is a branched chain having 1 to 4 carbon atoms in the main chain and 1 or 2 carbon atoms.
  • Means an alkyl group which may have, and specific examples thereof include methyl group, ethyl group, n-propyl group, i-propyl group, n-butyl group, i-butyl group, sec-butyl group or tert-butyl group Etc.
  • R 2 is preferably a hydrogen atom or an alkyl group having 1 to 3 carbon atoms which may have a branched chain having 1 carbon atom, and more preferably a hydrogen atom.
  • the alkyl group having 1 to 3 carbon atoms which can have a branched chain having 1 carbon atom is an alkyl group having 1 to 3 carbon atoms in the main chain and having a branched chain having 1 carbon atom.
  • a methyl group an ethyl group, an n-propyl group, an i-propyl group, an i-butyl group, or a sec-butyl group, preferably a methyl group, an i-propyl group, An i-butyl group or a sec-butyl group.
  • R 3 represents a — (CH 2 ) n—X group.
  • n represents a number of 1 to 4
  • X is an amino group, a guanidino group, a —CONH 2 group, or a 5-membered cyclic group having 1 to 3 nitrogen atoms.
  • X is preferably an amino group, guanidino group, carbamoyl group (—CONH 2 group), pyrrole group, imidazole group, pyrazole group or indole group, and more Preferably it is an imidazole group.
  • the - in (CH 2) n-X group, n is preferably 1 or 2, more preferably 1. Therefore, the — (CH 2 ) n- group is preferably an aminomethyl group, 2-aminoethyl group, 3-aminopropyl group, 4-aminobutyl group, carbamoylmethyl group, 2-carbamoylethyl group, 3-carbamoyl group.
  • a lipid peptide particularly suitable as a lipid peptide type compound is a compound formed from the following lipid part and peptide part (amino acid assembly part).
  • amino acids alanine (Ala), asparagine (Asn), glutamine (Gln), glycine (Gly), histidine (His), isorosine (Ile), leucine (Leu), lysine (Lys), tryptophan (Trp) ), Valine (Val).
  • Lauroyl-Gly-His Lauroyl-Gly-Gln, Lauroyl-Gly-Asn, Lauroyl-Gly-Trp, Lauroyl-Gly-Lys, Lauroyl-Ala-His, Lauroyl-Ala-Gln, Lauroyl-Ala-Asn, Lauroyl -Ala-Trp, Lauroyl-Ala-Lys; Myristoyl-Gly-His, Myristoyl-Gly-Gln, Myristoyl-Gly-Asn, Myristoyl-Gly-Trp, Myristoyl-Gly-Lys, Myristoyl-Ala-His, Myristoyl-Ala -Gln, Myristoyl-Ala-Asn, Myristoyl-Ala-Trp, Myristoyl-Ala-Lys; Palmitoyl-Gly-His, Palmitoyl-Gly-Gln, Palmi
  • lauroyl-Gly-His lauroyl-Ala-His-myristoyl-Gly-His, myristoyl-Ala-His; palmitoyl-Gly-His, palmitoyl-Ala-His; stearoyl-Gly-His, stearoyl-Ala -His.
  • R 4 represents an aliphatic group having 9 to 23 carbon atoms, and preferred specific examples include the same groups as defined for R 1 above.
  • R 5 to R 7 are each independently a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain having 1 or 2 carbon atoms, or — ( CH 2 ) nX group, and preferably at least one of R 5 to R 7 represents a — (CH 2 ) nX group.
  • n a number of 1 to 4
  • X represents an amino group, a guanidino group, a —CONH 2 group, or a 5-membered cyclic group or a 6-membered cyclic group that may have 1 to 3 nitrogen atoms, or a 5-membered ring And a condensed heterocyclic group composed of a 6-membered ring.
  • R 5 to R 7 include the same groups as defined for R 2 and R 3 above.
  • a preferable lipid peptide is a compound formed from the following lipid part and peptide part (amino acid assembly part).
  • Lauroyl-Gly-Gly-His Lauroyl-Gly-Gly-Gln, Lauroyl-Gly-Gly-Asn, Lauroyl-Gly-Gly-Trp, Lauroyl-Gly-Gly-Lys, Lauroyl-Gly-Ala-His, Lauroyl-His Gly-Ala-Gln, Lauroyl-Gly-Ala-Asn, Lauroyl-Gly-Ala-Trp, Lauroyl-Gly-Ala-Lys, Lauroyl-Ala-Gly-His, Lauroyl-Ala-Gly-Gln, Lauroyl-Ala- Gly-Asn, Lauroyl-Ala-Gly-Trp, Lauroyl-Ala-Gly-Lys, Lauroyl-Ala-Gly-Hi
  • lauroyl-Gly-Gly-His myristoyl-Gly-Gly-His, palmitoyl-Gly-Gly-His, palmitoyl-Gly-His-Gly, palmitoyl-His-Gly-Gly, stearoyl -Gly-Gly-His.
  • R 8 represents an aliphatic group having 9 to 23 carbon atoms, and preferred specific examples include the same groups as defined for R 1 above.
  • R 9 to R 12 are each independently a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain having 1 or 2 carbon atoms, or — ( CH 2 ) nX group, and preferably at least one of R 9 to R 12 represents a — (CH 2 ) nX group.
  • n a number of 1 to 4
  • X represents an amino group, a guanidino group, a —CONH 2 group, or a 5-membered cyclic group or a 6-membered cyclic group that may have 1 to 3 nitrogen atoms, or a 5-membered ring And a condensed heterocyclic group composed of a 6-membered ring.
  • R 9 to R 12 include the same groups as defined for R 2 and R 3 above.
  • particularly preferred lipid peptides include lauroyl-Gly-Gly-Gly-His, myristoyl-Gly-Gly-Gly-His, palmitoyl. -Gly-Gly-Gly-His, Palmitoyl-Gly-Gly-His-Gly, Palmitoyl-Gly-His-Gly-Gly, Palmitoyl-His-Gly-Gly-Gly, Stearoyl-Gly-Gly-Gly-His, etc. Can be mentioned.
  • the amount of the lipid peptide type compound is, for example, 0.1 to 2% by mass, preferably 0.3 to 1.5% by mass, and more preferably based on the total mass of the stick-like substrate to be obtained. Is 0.5 to 1.0 mass%.
  • the lipid peptide type compound used in the present invention comprises at least one of the compounds represented by the above formulas (1) to (3) (lipid peptide) or a pharmaceutically usable salt thereof, and is hydrogelated. These compounds can be used alone or in combination of two or more as an agent.
  • the surfactant used in the stick-shaped substrate of the present invention includes a compound having a hydrophilic part and a hydrophobic part in the molecule, and the hydrophilic part having a betaine structure (hereinafter also referred to as a betaine compound) and ethylene glycol.
  • a betaine compound hereinafter also referred to as a betaine compound
  • An alkyl ether is mentioned.
  • betaine compounds as described above include N-alkyl-N, N-dimethylamino acid betaines such as lauryldimethylaminoacetic acid betaine (lauryl betaine); fatty acid amide alkyl-N such as cocamidopropyl betaine and lauramidopropyl betaine.
  • N-dimethylamino acid betaine N-dimethylamino acid betaine; imidazoline-type betaines such as sodium cocoamphoacetate and sodium lauroamphoacetate; alkylsulfobetaines such as laurylhydroxysulfobetaine and alkyldimethyltaurine; sulfate-type betaines such as alkyldimethylaminoethanol sulfate; alkyldimethylaminoethanol Known betaine compounds such as phosphate-type betaines such as phosphate esters can be used as amphoteric surfactants. As the betaine compound, sulfate-type betaine is preferable.
  • betaine compounds include phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, phosphatidylglycerol, diphosphatidylglycerol (cardiolipin), phosphatidic acid and other glycerophospholipids; lysophosphatidylcholine (lysolecithin), lysophosphatidylethanolamine, Examples thereof include lysoglycerophospholipids such as serine, lysophosphatidylinositol, lysophosphatidylglycerol, and lysophosphatidic acid; sphingophospholipids such as sphingomyelin; and hydrogenated products thereof.
  • phospholipids may be derived from animals and plants such as soybeans and egg yolks, or may be synthesized by a chemical or enzymatic method.
  • betaine compounds preferably lauryldimethylaminoacetic acid betaine, lauric acid amidopropyl betaine, lauryl hydroxysulfobetaine, stearyl betaine, lysophosphatidylcholine (lysolecithin), lysophosphatidylethanolamine, lysophosphatidylserine, lysophosphatidylinositol, lyso Examples include phosphatidylglycerol and lysophosphatidic acid, and more preferably lauryl hydroxysulfobetaine.
  • ethylene glycol alkyl ether examples include polyoxyethylene alkyl ether, polyoxyethylene lauryl ether, polyoxyethylene palmitoyl ether, and polyoxyethylene stearyl ether. Polyoxyethylene lauryl ether is preferable. Also, commercially available ethylene glycol alkyl ethers can be used. Examples of such products include Emulgen 102KG, Emargen 103, and Emulgen 104P in Kao's Emulgen (registered trademark) series and Emanon (registered trademark) series.
  • Emulgen 103 More preferably, Kao's Emulgen 103, Emulgen 104P, Emulgen 105, Emulgen 106, Emulgen 108, Emulgen 109P, Emulgen 210P, Emulgen 306P, Emulgen 320P, Emulgen 404, Emulgen 408, Emulgen 409PV, Emulgen 420, Emulgen 705 , Emulgen 707, Emulgen 709, Emulgen 1108, Emulgen 2020G-HA, Emanon 1112, Emanon 4110.
  • Emulgen 104P More preferably, Kao's Emulgen 104P, Emulgen 105, Emulgen 106, Emulgen 108, Emulgen 210P, Emulgen 306P, Emulgen 408, Emulgen 409PV, Emulgen 705, Emulgen 707, Emulgen 709, Emulgen 1108, Emulgen 2020G-HA, Emanon 1112, Emanon 4110.
  • it can be appropriately selected from the NIKKOL (registered trademark) series of Nikko Chemicals.
  • NIKKOL BT-5, NIKKOL BT-7, NIKKOL BT-9, NIKKOL BT-12, NIKKOL BL-2, NIKKOL BL-4.2, NIKKOL BL-9EX, etc. most preferably NIKOL BL-9EX 9EX.
  • HLB Hydrophile-Lipophile Balance
  • the compounding amount of the surfactant is, for example, 0.1 to 20% by mass, preferably 0.1 to 10% by mass with respect to the total mass of the stick-like substrate to be obtained.
  • ethylene glycol alkyl ether for example, 0.1 to 3% by mass is preferable with respect to the total mass of the obtained stick-like substrate, and when a betaine compound is used, it is obtained.
  • 0.5 to 10% by mass is preferable with respect to the total mass of the stick-shaped substrate.
  • the surfactant used in the present invention is at least one of the above-mentioned surfactant group, and these surfactants can be used alone or in combination of two or more.
  • the 1,2-alkanediol or 1,3-alkanediol used in the stick-like substrate of the present invention has a function of promoting the solubility of the lipid peptide type compound.
  • 1,3-alkanediol is preferred.
  • Specific examples of the 1,2-alkanediol include 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol, and the like. Preferred are 1,2-pentanediol, 1,2-hexanediol, and 1,2-octanediol.
  • 1,2-pentanediol or 1,2-hexanediol More preferred is 1,2-pentanediol or 1,2-hexanediol.
  • the 1,2-alkanediol used in the present invention is at least one of the aforementioned 1,2-alkanediol group.
  • Specific examples of the 1,3-alkanediol include 1,3-propanediol, 2-methyl-1,3-propanediol, 1,3-butanediol, 3-methyl-1,3-butanediol, , 3-pentanediol, 1,3-hexanediol, 2-ethyl-1,3-hexanediol, 2-ethyl-1,3-octanediol, 1,3-decanediol, and the like.
  • 1,3-pentanediol 1,3-hexanediol, 2-ethyl-1,3-hexanediol, and 2-ethyl-1,3-octanediol. More preferred are 2-ethyl-1,3-hexanediol and 2-ethyl-1,3-octanediol.
  • the 1,3-alkanediol used in the present invention is at least one of the aforementioned 1,3-alkanediol group.
  • 1,3-alkanediol for example, 1,3-butanediol is preferable.
  • These 1,2-alkanediols or 1,3-alkanediols can be used alone or in combination of two or more.
  • the blending amount of 1,2-alkanediol or 1,3-alkanediol is, for example, 0.5 to 20% by mass, preferably 1 to 1% by mass with respect to the total mass of the obtained stick-like substrate. It is 10% by mass, more preferably 2 to 8% by mass.
  • At least one saturated or unsaturated monohydric alcohol having 8 to 30 carbon atoms By adding at least one saturated or unsaturated monohydric alcohol having 8 to 30 carbon atoms to the stick-shaped substrate of the present invention, the stability of the substrate is improved, specifically the surface of the substrate. The oil release phenomenon called “sweat” can be suppressed.
  • at least one saturated or unsaturated monohydric alcohol having 8 to 30 carbon atoms is also simply referred to as “higher alcohol”. These higher alcohols are commercially available or synthesized many raw materials including derivatives, but in the stick-like base material of the present invention, preferably at least one kind of alkyl group having 8 to 30 carbon atoms.
  • Saturated or unsaturated monohydric alcohols can be used, more preferably 12 to 22 saturated monohydric alcohols, among which myristyl alcohol (14 carbon atoms), cetanol (16 carbon atoms). Stearyl alcohol (18 carbon atoms) and behenyl alcohol (22 carbon atoms) are particularly preferred because of their high versatility and high “sweat” -suppressing effect.
  • the compounding amount of the higher alcohol is, for example, 0.001 to 1% by mass, preferably 0.01 to 0.5% by mass, and more preferably 0% with respect to the total mass of the stick-like substrate to be obtained. 0.03 to 0.3% by mass.
  • the said higher alcohol used in this invention is at least 1 type of the above-mentioned higher alcohol group, These can be used individually by 1 type or in combination of 2 or more types.
  • Examples of the thickener used in the stick-shaped substrate of the present invention include alginic acid derivatives and carrageenan.
  • Examples of the alginic acid derivative used in the stick-shaped substrate of the present invention include alginic acid, alginic acid salts (sodium salt, potassium salt, calcium salt, etc.), alginic acid ester, and the like.
  • Alcohol esters are preferred.
  • Examples of the alginic acid polyhydric alcohol ester include ethylene glycol alginate and propylene glycol alginate, and propylene glycol alginate is preferable.
  • the blending amount of the thickener used is, for example, 0.3 to 1.0% by mass, preferably 0.3 to 0.7% by mass, based on the total mass of the stick-like substrate to be obtained. It is.
  • the thickener used in this invention is at least 1 sort (s) of the thickener selected from the above, These thickeners can be used individually by 1 type or in combination of 2 or more types.
  • the stick-like substrate of the present invention can also contain fatty acids, oily bases, pigments, organic acids, polyhydric alcohols, and other additives. Each component will be described below.
  • the fatty acid that can be used in the stick-shaped substrate of the present invention is preferably at least one selected from the group consisting of saturated fatty acids having 10 to 20 carbon atoms and unsaturated fatty acids and salts of these fatty acids.
  • saturated fatty acids having 10 to 20 carbon atoms and unsaturated fatty acids and salts of these fatty acids.
  • examples include capric acid, undecanoic acid, lauric acid, tridecanoic acid, myristic acid, pentadecanoic acid, palmitic acid, margaric acid, and stearic acid. More preferably, capric acid, lauric acid, myristic acid, palmitic acid, and stearic acid are mentioned, and stearic acid is particularly preferable.
  • the amount of the fatty acid used is, for example, 0.1 to 2.0% by mass, preferably 0.2 to 1.0% by mass, based on the total mass of the stick-like substrate to be obtained. is there.
  • the fatty acid which can be used in this invention is at least 1 sort (s) selected from the said fatty acid group, These fatty acids can be used individually by 1 type or in combination of 2 or more types.
  • oily base that can be used in the stick-like substrate of the present invention is not particularly limited, and examples thereof include the following oily bases: oleyl alcohol, jojoba alcohol, chimyl alcohol, seraalkyl alcohol, batyl alcohol, Higher (polyhydric) alcohols such as hexyldecanol, isostearyl alcohol, 2-octyldodecanol, dimer diol; aralkyl alcohols such as benzyl alcohol and derivatives thereof; isostearic acid, behenic acid, undecylenic acid, 12-hydroxystearic acid, palmi Tooleic acid, oleic acid, linoleic acid, linolenic acid, erucic acid, docosahexaenoic acid, eicosapentaenoic acid, isohexadecanoic acid, antiisohenicosanoic acid, long-chain branched fatty acid, dimer acid,
  • Acyl sarcosine alkyl ester Acyl sarcosine alkyl ester, cholesteryl 12-hydroxystearate, macadamia nut oil fatty acid cholesteryl, macadamia nut oil fatty acid phytosteryl, phytosteryl isostearate, soft lanolin fatty acid cholesteryl, hard lanolin fatty acid cholesteryl, long chain branched fatty acid cholesteryl, long chain ⁇ -hydroxy fatty acid cholesteryl, etc.
  • the blending amount when the oily base is used is, for example, 1 to 50% by mass, preferably 5 to 50% by mass, more preferably 5 to 5% by mass with respect to the total mass of the stick-like substrate to be obtained. It is 20% by mass, particularly preferably 10 to 20% by mass.
  • the oily base that can be used in the present invention is at least one of the above-mentioned oily base group, and these oily bases may be used alone or in combination of two or more.
  • the stick-like substrate of the present invention may further contain a pigment.
  • the pigment that can be blended is not particularly limited.
  • inorganic white pigments such as titanium dioxide and zinc oxide
  • inorganic red pigments such as red iron oxide (bengala) and iron titanate
  • Inorganic yellow pigments such as yellow iron oxide and loess
  • inorganic black pigments such as black iron oxide and low-order titanium oxide
  • inorganic purple pigments such as mango violet and cobalt violet
  • Inorganic green pigments such as chromium and cobalt titanate
  • inorganic blue pigments such as ultramarine and bitumen
  • titanium oxide coated mica, titanium oxide coated bismuth oxychloride, titanium oxide coated talc, colored titanium oxide coated mica, bismuth oxychloride, fish scale Pearl pigments such as foil; talc, sericite, mica, kaolin, calcium carbonate, magnesium carbonate, silicic anhydr
  • the blending amount is, for example, 1 to 50% by mass, preferably 5 to 50% by mass, and more preferably 6 to 20%, based on the total mass of the stick-like substrate to be obtained. % By mass, particularly preferably 10 to 20% by mass.
  • the said pigment used in this invention is at least 1 type of the above-mentioned pigment group, These pigments can be used individually by 1 type or in combination of 2 or more types.
  • the stick-like substrate of the present invention may further contain an organic acid.
  • the organic acid include ascorbic acid, citric acid, lactic acid, glycolic acid, succinic acid, acetic acid, malic acid, tartaric acid, and fumaric acid.
  • ascorbic acid, citric acid, and lactic acid are preferable, and ascorbic acid and citric acid are particularly preferable.
  • the compounding quantity in the case of using an organic acid is 1-20 mass% with respect to the total mass of the stick-shaped base material obtained, Preferably it is 1-10 mass%.
  • the stick-like substrate of the present invention may further contain a polyhydric alcohol.
  • the polyhydric alcohol is a polyhydric alcohol different from the 1,2-alkanediol or 1,3-alkanediol listed above, and specific examples thereof include glycerin, propylene glycol, and polyethylene glycol.
  • the temporal stability of the stick-like substrate can be improved.
  • polyethylene glycol having an average molecular weight of 1,000 to 4,000 can be preferably used.
  • the blending amount can be, for example, 1 to 80% by mass, preferably 1 to 60% by mass, based on the total mass of the stick-like substrate to be obtained.
  • the stick-like substrate of the present invention can be blended with additives that can generally be used as cosmetic additives, quasi-drug additives, and pharmaceutical additives as necessary.
  • additives such as physiologically active substances and functional substances that are blended in cosmetics, quasi-drugs, or pharmaceutical external preparations for skin include moisturizers, feel-improving agents, surfactants other than the above, solvents, and antioxidants.
  • Agent reducing agent, oxidizing agent, preservative, antibacterial agent, bactericidal agent, chelating agent, pH adjuster, acid, alkali, powder, inorganic salt, UV absorber, whitening agent, vitamins and derivatives thereof, for hair growth Drug, Blood circulation promoter, Stimulant, Hormones, Anti-wrinkle agent, Anti-aging agent, Tightening agent, Cool sensation agent, Warm sensation agent, Wound healing promoter, Stimulation mitigation agent, Analgesic agent, Cell activator, Plant / Animal ⁇ Microbial extract, antipruritic agent, exfoliating / dissolving agent, antiperspirant, refreshing agent, astringent, enzyme, nucleic acid, fragrance, pigment, colorant, dye, anti-inflammatory agent, anti-inflammatory agent, anti-asthma, anti-chronic obstructive Examples include pulmonary diseases, antiallergies, immune regulators, antiinfectives and antifungals It is.
  • the blending amount of these other additives may vary depending on the type of
  • moisturizers / feel improvers include glycerin, trimethylolpropane, pentaerythritol, hexylene glycol, diglycerin, polyglycerin, diethylene glycol, dipropylene glycol, polypropylene glycol, ethylene glycol / propylene glycol copolymer and the like polyols and Polymers; glycol alkyl ethers such as diethylene glycol monoethyl ether (ethoxydiglycol), ethylene glycol monoethyl ether, ethylene glycol monobutyl ether, diethylene glycol dibutyl ether; (eicosane diacid / tetradecanedioic acid) polyglyceryl-10, tetradecane Water-soluble esters such as polyglyceryl-10; sorbitol, xylitol, erythritol, man Sugar alcohols such as tol and maltitol; glucose, fructose
  • the surfactant include an anionic surfactant, a nonionic surfactant, a cationic surfactant, an amphoteric surfactant, and a polymer surfactant.
  • preferable surfactants include fatty acid salts such as potassium laurate and potassium myristate; alkyl sulfate esters such as sodium lauryl sulfate, triethanolamine lauryl sulfate, and ammonium lauryl sulfate; Polyoxyethylene alkyl sulfates such as sodium laureth sulfate and triethanolamine laureth sulfate; cocoyl methyl taurine sodium, cocoyl methyl taurine potassium, lauroyl methyl taurine sodium, myristoyl methyl taurine sodium, lauroyl methyl alanine sodium, lauroyl sarcosine sodium, lauroyl sarcosine tri Acyl N-methyl amino acid salts such as ethanolamine and sodium methylalanine sodium, la
  • Polyoxyethylene alkyl ethers with various polyoxyethylene addition numbers such as silethylene behenyl ethers), isosteares (polyoxyethylene isostearyl ether) s, octyldecesses (polyoxyethylene octyldodecyl ethers); Ether: Polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil monoisostearate, polyoxyethylene hydrogenated castor oil triisostearate, polyoxyethylene hydrogenated castor oil monopyroglutamic acid monoisostearic acid diester Castor oil and hardened castor oil derivatives such as polyoxyethylene hydrogenated castor oil maleic acid; polyoxyethylene phytosterol; polyoxyethylene cholesterol Polyoxyethylene cholestanol; polyoxyethylene lanolin; polyoxyethylene reduced lanolin; polyoxyethylene / polyoxypropylene cetyl ether, polyoxyethylene / polyoxypropylene 2-decyltetradecyl ether, polyoxy
  • Polyglyceryl ethers polyoxyethylene alkylamines; tetrapolyoxyethylene / tetrapolyoxypropylene-ethylenediamine condensates; natural surfactants such as saponins and sophorolipids; polyoxyethylene fatty acid amides; Palm oil fatty acid monoethanolamide (cocamide MEA), palm oil fatty acid diethanolamide (cocamide DEA), lauric acid monoethanolamide (Lauramide MEA), lauric acid diethanolamide (lauramide DEA), lauric acid monoisopropanolamide (lauramide MIPA), palmitic acid monoethanolamide (partamide MEA), palmitic acid diethanolamide (partamide DEA), palm oil fatty acid methylethanolamide ( Fatty acid alkanolamides such as cocamidomethyl MEA); alkyldimethylamine oxides such as lauramine oxide, cocamamine oxide, stearamine oxide, and behenamine oxide; alkylethoxydimethylamine oxide; polyoxyethylene al
  • Nonionic surfactants of silicone, etc .; cationic surfactants include alkyltrimethylammonium chlorides such as behentrimonium chloride, steartrimonium chloride, cetrimonium chloride, lauryltrimonium chloride; stearyltrimonium bromide, etc.
  • Alkyltrimethylammonium bromides dialkyldimethylammonium chlorides such as distearyldimonium chloride and dicocodimonium chloride; fatty acid amidoamines and salts thereof such as stearamidepropyldimethylamine and stearamideethyldiethylamine; alkyl ethers such as stearoxypropyldimethylamine Amines and salts or quaternary salts thereof; ethyl sulfate long chain branched fatty acid (12-31) aminopropylethyldimethylammonium Fatty acid amide type quaternary ammonium salts such as lanolin fatty acid aminopropylethyldimethylammonium; polyoxyethylene alkylamines and salts or quaternary salts thereof; alkylamine salts; fatty acid amidoguanidinium salts; alkyl etheraminemonium salts; Benzalkonium salts; benzethonium salts
  • Silicone-based cationic surfactants such as amino-modified silicone, cation-modified silicone, cation-modified and polyether-modified silicone, amino-modified and polyether-modified silicone
  • amphoteric surfactant etc N-alkyl-N, N-dimethylamino acid betaines such as lauryl betaine (lauryldimethylaminoacetic acid betaine); fatty acid amide alkyl-N, N-dimethylamino acid betaines such as cocamidopropyl betaine and lauramidopropyl betaine; sodium cocoamphoacetate; Imidazoline-type betaines such as sodium lauroamphoacetate; alkylsulfobetaines such as alkyldimethyltaurine; sulfate-type betaines such as alkyldimethylaminoethanol sulfate; phosphate-type betaines such as alkyldimethylaminoethanol phosphate; phosphati
  • Solvents include lower alcohols such as ethanol, 2-propanol (isopropyl alcohol), butanol and isobutyl alcohol; glycols such as propylene glycol, diethylene glycol, dipropylene glycol and isopentyl diol; diethylene glycol monoethyl ether (ethoxydiglycol) , Glycol ethers such as ethylene glycol monoethyl ether, ethylene glycol monobutyl ether, triethylene glycol monoethyl ether, diethylene glycol diethyl ether, diethylene glycol dibutyl ether, propylene glycol monoethyl ether, dipropylene glycol monoethyl ether; ethylene glycol monoethyl ether Acetate, diethylene glycol Glycol ether esters such as ethyl ether acetate and propylene glycol monoethyl ether acetate; glycol esters such as diethoxyethyl succinate and ethylene
  • Antioxidants include tocopherol derivatives such as tocopherol (vitamin E) and tocopherol acetate; BHT, BHA; gallic acid derivatives such as propyl gallate; vitamin C (ascorbic acid) and / or derivatives thereof; erythorbic acid and derivatives thereof; Preferred are sulfites such as sodium sulfite; bisulfites such as sodium bisulfite; thiosulfates such as sodium thiosulfate; metabisulfites; thiotaurine, hypotaurine; thioglycerol, thiourea, thioglycolic acid, cysteine hydrochloride As mentioned.
  • Preferred examples of the reducing agent include thioglycolic acid, cysteine, cysteamine and the like.
  • Preferred examples of the oxidizing agent include hydrogen peroxide water, ammonium persulfate, sodium bromate, percarbonate, and the like.
  • preservatives, antibacterial agents, and bactericides include hydroxybenzoic acid such as methylparaben, ethylparaben, propylparaben, and butylparaben, and salts or esters thereof; salicylic acid; sodium benzoate; phenoxyethanol; methylchloroisothiazolinone, methylisothiazo Isothiazolinone derivatives such as linone; imidazolinium urea; dehydroacetic acid and its salts; phenols; halogenated bisphenols such as triclosan, acid amides, quaternary ammonium salts; trichlorocarbanide, zinc pyrithione, benzalkonium chloride, chloride Benzethonium, sorbic acid, chlorhexidine, chlorhexidine gluconate, halocarban, hexachlorophene, hinokitiol; phenol, isopropylphenol, cresol, Mall
  • chelating agents include edetate (ethylenediaminetetraacetate) such as EDTA, EDTA2Na, EDTA3Na, and EDTA4Na; hydroxyethylethylenediaminetriacetate such as HEDTA3Na; pentetate (diethylenetriaminepentaacetate); phytic acid; Phosphonic acid and its sodium salt; polyamino acids such as polyaspartic acid and polyglutamic acid; sodium polyphosphate, sodium metaphosphate, phosphoric acid; sodium citrate, citric acid, alanine, dihydroxyethylglycine, gluconic acid, Ascorbic acid, succinic acid and tartaric acid are preferred.
  • edetate ethylenediaminetetraacetate
  • HEDTA3Na EDTA3Na
  • EDTA4Na hydroxyethylethylenediaminetriacetate
  • pentetate diethylenetriaminepentaacetate
  • phytic acid
  • pH adjusters / acids / alkalis include citric acid, sodium citrate, lactic acid, sodium lactate, potassium lactate, glycolic acid, succinic acid, acetic acid, sodium acetate, malic acid, tartaric acid, fumaric acid, phosphoric acid, hydrochloric acid, sulfuric acid , Monoethanolamine, diethanolamine, triethanolamine, isopropanolamine, triisopropanolamine, 2-amino-2-methyl-1,3-propanediol, 2-amino-2-hydroxymethyl-1,3-propanediol, arginine Sodium hydroxide, potassium hydroxide, aqueous ammonia, guanidine carbonate, and ammonium carbonate are preferable.
  • powders include mica, talc, kaolin, sericite, montmorillonite, kaolinite, mica, muscovite, phlogopite, synthetic mica, saucite, biotite, permiculite, magnesium carbonate, calcium carbonate, aluminum silicate, and silicic acid.
  • Inorganic salts include sodium chloride-containing salts such as salt, common salt, rock salt, sea salt, natural salt; potassium chloride, aluminum chloride, calcium chloride, magnesium chloride, bittern, zinc chloride, ammonium chloride; sodium sulfate, aluminum sulfate, Aluminum sulfate / potassium sulfate (alum), aluminum sulfate / ammonium sulfate, barium sulfate, calcium sulfate, potassium sulfate, magnesium sulfate, zinc sulfate, iron sulfate, copper sulfate; sodium phosphates such as 1Na, 2Na and 3Na phosphates, phosphoric acid Potassium, calcium phosphates and magnesium phosphates are preferred.
  • sodium chloride-containing salts such as salt, common salt, rock salt, sea salt, natural salt
  • potassium chloride aluminum chloride, calcium chloride, magnesium chloride, bittern, zinc chloride, ammonium chlor
  • ultraviolet absorbers examples include paraaminobenzoic acid, paraaminobenzoic acid monoglycerin ester, N, N-dipropoxyparaaminobenzoic acid ethyl ester, N, N-diethoxyparaaminobenzoic acid ethyl ester, and N, N-dimethylparaaminobenzoic acid ethyl ester.
  • Benzoic acid ultraviolet absorbers such as esters, N, N-dimethylparaaminobenzoic acid butyl ester, N, N-dimethylparaaminobenzoic acid methyl ester; Anthranilic acid ultraviolet absorbers such as homomenthyl-N-acetylanthranilate; Salicylic acid And salicylic acid systems such as sodium salt, amyl salicylate, menthyl salicylate, homomenthyl salicylate, octyl salicylate, phenyl salicylate, benzyl salicylate, p-isopropanol phenyl salicylate External line absorbent: octyl cinnamate, ethyl-4-isopropyl cinnamate, methyl-2,5-diisopropyl cinnamate, ethyl-2,4-diisopropyl cinnamate, methyl-2,4-diisopropyl c
  • UV absorbers 3- (4′-methylbenzylidene) -d, l-camphor, 3-benzylidene-d, l-camphor; 2-phenyl-5-methylbenzoxazole; 2,2′-hydroxy- 2- (2′-hydroxy-5′-t-octylphenyl) benzotriazole; 2- (2′-hydroxy-5′-methylphenylbenzotriazole; dibenzalazine; dianisoylmethane; 5- (3,3-dimethyl-2-norbornylidene) -3-pentan-2-one; dibenzoylmethane derivatives such as 4-t-butylmethoxydibenzoylmethane; octyl triazone; urocanic acid such as urocanic acid and ethyl urocanate Derivatives; 2- (2′-hydroxy-5′-methylphenyl) benzotriazole Hydantoin derivatives such as 1- (3,4-dimethoxypheny
  • whitening agents include hydroquinone glycosides such as arbutin and ⁇ -arbutin and their esters; ascorbic acid phosphates such as ascorbic acid, sodium ascorbic acid phosphate and magnesium ascorbic acid phosphate, ascorbic acid Ascorbic acid fatty acid esters such as tetraisopalmitic acid ester, ascorbic acid alkyl ethers such as ascorbic acid ethyl ether, ascorbic acid glucosides such as ascorbic acid-2-glucoside and fatty acid esters thereof, ascorbic acid sulfate ester, tocopheryl ascorbyl phosphate Ascorbic acid derivatives such as kojic acid, ellagic acid, tranexamic acid and its derivatives, ferulic acid and its derivatives, placenta extract, glutathione, oryzanol, butylreso Shinoru, oil-soluble Kamomiraekisu, oil-soluble licorice extract,
  • Vitamins and their derivatives include vitamin A such as retinol, retinol acetate, retinol palmitate; thiamine hydrochloride, thiamine sulfate, riboflavin, riboflavin acetate, pyridoxine hydrochloride, pyridoxine dioctanoate, pyridoxine dipalmitate, Flavin adenine dinucleotide, cyanocobalamin, folic acid, nicotinic acid such as nicotinic acid amide / benzyl nicotinate, vitamin B group such as choline; vitamin C such as ascorbic acid and its sodium salt; vitamin D; ⁇ , Vitamin E such as ⁇ , ⁇ , and ⁇ -tocopherol; other vitamins such as pantothenic acid and biotin; ascorbic acid phosphates such as ascorbic acid phosphate sodium salt and ascorbic acid phosphate magnesium salt, Ascorbic acid fatty acid esters
  • Plant extracts and tinctures such as assembly extract, red pepper tincture, ginger tincture, ginger extract, cantalis tincture; capsaicin, nonylic acid vanillylamide, gingeron, ictamol, tannic acid Borneol, cyclandrate, cinnarizine, trazoline, acetylcholine, verapamil, cephalanthin, ⁇ -oryzanol, vitamin E and derivatives such as nicotinic acid tocopherol / acetic acid tocopherol, nicotinic acid and nicotinic acid amide / nicotinic acid benzyl ester / inositol hexanicotinate Derivatives of nicotine alcohol, allantoin, photosensitive element 301, photosensitive element 401, capronium chloride, pentadecanoic acid monoglyceride, flavonol derivative, stigma Terol or stigmastanol and glycosides thereof, and the
  • hormones include estradiol, estrone, ethinyl estradiol, cortisone, hydrocortisone, prednisone and the like.
  • Other remedies such as anti-wrinkle agents, anti-aging agents, squeeze agents, cooling sensations, warming sensation agents, wound healing promoters, irritation relievers, analgesics, cell activators include retinols, retinoic acids, retinoin Acid tocopheryl; derivatives such as lactic acid, glycolic acid, gluconic acid, fruit acid, salicylic acid and glycosides / esterified products thereof, ⁇ - or such as hydroxycapric acid, long chain ⁇ -hydroxy fatty acid, long chain ⁇ -hydroxy fatty acid cholesteryl ⁇ -hydroxy acids and derivatives thereof; ⁇ -aminobutyric acid, ⁇ -amino- ⁇ -hydroxybutyric acid; carnitine; carnosine; creatine; ceramides, sphingosines; caffeine, xant
  • Antioxidant / active oxygen scavengers include catechins; flavones such as quercetin; isoflavones; gallic acid and ester sugar derivatives; polyphenols such as tannin, sesamin, protoanthocyanidin, chlorogenic acid, apple polyphenol; rutin and glycosides, etc.
  • hesperidin and glycosides Derivatives of hesperidin and glycosides; lignan glycosides; licorice extract-related substances such as grabrizine, glabrene, liquiritin, and isoliquiritin; lactoferrin; shogaol, gingerol; and fragrance substances such as menthol and cedrol; And insecticides such as diethyl toluamide; complexes of physiologically active substances and cyclodextrins are preferred.
  • Plant / animal / microbe extracts include iris extract, ashitaba extract, asunalo extract, asparagus extract, avocado extract, achacha extract, almond extract,retea extract, arnica extract, aloe extract, apricot extract, apricot kernel extract, ginkgo biloba extract , Carrot extract, fennel extract, turmeric extract, oolong tea extract, walrus extract, ages extract, echinacea leaf extract, enmeo extract, peony extract, duckweed extract, lauren extract, barley extract, ginseng extract, hypericum extract, licorice extract, Onionis extract, Dutch mustard extract, orange extract, dried seawater, seaweed extract, oyster leaf extract, oyster extract, hydrolyzed elastin, hydrolyzed wheat powder, water Denatured silk, cocoon extract, chamomile extract, oil-soluble chamomile extract, carrot extract, kawarayomigi extract, oat extract, calcade extract, licorice extract, oil-soluble
  • antipruritic agents examples include diphenhydramine hydrochloride, chlorpheniramine maleate, camphor, substance-P inhibitor, and the like.
  • exfoliating / dissolving agent examples include salicylic acid, sulfur, resorcin, selenium sulfide, pyridoxine and the like.
  • antiperspirants examples include chlorohydroxyaluminum, aluminum chloride, zinc oxide, zinc paraphenol sulfonate, and the like.
  • Examples of the refreshing agent include menthol and methyl salicylate.
  • astringents include citric acid, tartaric acid, lactic acid, aluminum sulfate / potassium, and tannic acid.
  • Enzymes include superoxide dismutase, catalase, lysozyme chloride, lipase, papain, pancreatin, protease, and the like.
  • Preferred nucleic acids include ribonucleic acid and its salts, deoxyribonucleic acid and its salts, and adenosine triphosphate disodium.
  • Orange No. 201 Orange No. 203, Orange No. 204, Orange No. 205, Orange No. 206, Orange No. 207, Orange No. 401, Orange No. 402, Orange No. 403, Yellow No. 201, Yellow No. 202-1 Yellow 202-2, Yellow 203, Yellow 204, Yellow 205, Yellow 4, Yellow 401, Yellow 402, Yellow 403-1, Yellow 404, Yellow 405, Yellow 406, Yellow Legal pigments such as No. 407 and Yellow No.
  • Anti-inflammatory / anti-inflammatory agents include glycyrrhizic acid and its derivatives, glycyrrhetinic acid derivatives, salicylic acid derivatives, hinokitiol, guaiazulene, allantoin, indomethacin, ketoprofen, ibuprofen, diclofenac, loxoprofen, celecoxib, infliximab, etanercept, zinc oxide, hydroacetic acid, zinc acetate, Preferred examples include prednisone, diphedramine hydrochloride, chlorpheniramine maleate; and plant extracts such as peach leaf extract and persimmon leaf extract.
  • Anti-asthma, anti-chronic obstructive pulmonary disease, anti-allergy, immunomodulators include aminophylline, theophylline, steroids (fluticasone, beclomethasone, etc.), leukotriene antagonists, thromboxane inhibitors, intal, ⁇ 2-stimulant (Formoterol, salmeterol, albuterol, tulobuterol, clenbuterol, epinephrine, etc.), tiotropium, ipratropium, dextromethorphan, dimemorphan, bromhexine, tranilast, ketotifen, azelastine, cetirizine, chlorpheniramine, polyquitolsine, Preferred examples include cytokine regulators, interferons, omalizumab, and protein / antibody preparations.
  • Preferred examples of the anti-infective and antifungal agents include oseltamivir, zanamivir, and itraconazole.
  • cosmetic raw material standards cosmetic ingredient-specific combination ingredient standards, Japan Cosmetic Industry Association ingredient display name list, INCI dictionary (The International Cosmetic Ingredients and Handbooks), quasi-drug ingredients standards, Japanese pharmacopoeia, pharmaceutical additive standards Ingredients listed in the Food Addendum, etc., and the international patent classification IPC described in Japan and other foreign patent gazettes and patent publications (including publications and republications) belonging to the A61K7 and A61K8 classifications It is possible to contain known cosmetic ingredients, pharmaceutical ingredients, food ingredients, etc., in known combinations, blending ratios and blending amounts.
  • the stick-like substrate of the present invention comprises a lipid peptide compound comprising at least one of the compounds represented by the formulas (1) to (3) or a pharmaceutically usable salt thereof, a surfactant and water, 1,2-alkanediol or 1,3-alkanediol, higher alcohol, thickener and, if necessary, an oily base, pigment, and other additives, mixed and stirred with heating, then allowed to stand It can be manufactured by cooling.
  • the stick-shaped substrate of the present invention is produced by the following process as an example. a) a step of blending the above-mentioned lipid peptide compound, a surfactant and water, and preparing a solution or dispersion by heating; b) adding the solution or dispersion to water and heating at a temperature of room temperature to less than 100 ° C .; c) The process which cools with stirring until it becomes temperature lower than the temperature in the said heating process, and is left still standing to cool, and forms a gel-like solid substance (stick-shaped base material).
  • 1,2-alkanediol or 1,3-alkanediol, oily base, higher alcohol, thickener, pigment and other additives are added in the step of preparing the solution or dispersion in step a).
  • it may be added in advance to the water to which the solution or dispersion is added in step b).
  • water is 20 mass% or more and less than 99 mass% with respect to the total mass of the obtained stick-shaped base material.
  • water is 30 to 80 mass% with respect to the total mass of the obtained solution or dispersion.
  • the heating temperature in the step a) and the step b) is preferably 50 ° C. to 90 ° C., more preferably 60 ° C. to 90 ° C., for example 80 ° C., and stirring is preferably performed while heating.
  • the time of heating and stirring in each step at this time varies depending on the type of lipid peptide compound used, the surfactant and other components, and the blending amount thereof, but can usually be dissolved and dispersed in about 5 to 50 minutes. .
  • cooling is performed with stirring until the liquid temperature is lower than the temperature in step b) (step c).
  • the cooling temperature is, for example, room temperature to 80 ° C., room temperature to 60 ° C., or room temperature to 40 ° C.
  • the stick-shaped base material of this invention can also be manufactured by adding suitably another compounding component to this premix.
  • the following is mentioned as a manufacturing method of the stick-shaped base material which passed through the premix.
  • the aqueous phase in the step 2-1) contains water, and may further contain an oily base, a higher alcohol, a thickener, a pigment, and 1,2-alkanediol or 1,3-alkanediol, and other additives. May be included.
  • a pigment and other additives may be mixed with the aqueous composition (premix) and then combined with the aqueous phase. Furthermore, in the said mixing process, the stick-shaped base material (formulation) which added the chemical
  • the heating temperature of the mixed system (and aqueous composition) in the steps 1-1) and 1-2) is preferably 50 ° C. to 90 ° C., more preferably 60 ° C. to 90 ° C., for example 70 ° C., or 80 ° C. It is.
  • This step is preferably carried out with stirring.
  • the time of heating (stirring) in each step at this time is usually about 5 to 50 minutes, although it varies depending on the type of lipid peptide compound, surfactant and other components contained in the aqueous composition, and their blending amount. .
  • the aqueous composition is uniformly dissolved.
  • the cooling temperature in the step 1-3) is, for example, room temperature to 80 ° C., room temperature to 60 ° C., or room temperature to 40 ° C. In this step, it is more preferable to cool with stirring, then stop stirring and leave to stand. In addition, it is preferable that water is 30 mass% or more and less than 80 mass% with respect to the total mass of the aqueous composition (premix) obtained by the 1) process.
  • the heating temperature of the aqueous phase and the aqueous composition (premix) is preferably 50 ° C. to 90 ° C., more preferably 60 ° C. to 90 ° C., such as 70 ° C., or 80 ° C., or 90 ° C. It is.
  • the aqueous phase is preferably heated with stirring because it contains other components such as an oily base. Heating (stirring) is usually carried out for about 5 to 50 minutes until the contained components are uniformly dissolved and dispersed. It is preferable to do.
  • the heating temperature of the aqueous phase may be the same as the heating temperature of the aqueous composition (premix).
  • the mixture obtained in the previous step is cooled to form a gel-like solid (stick-like substrate).
  • the mixture may be cooled with stirring.
  • the blending amount of water may be 20% by mass or more and less than 99% by mass with respect to the total mass of the stick-shaped substrate. preferable.
  • the obtained solid was dissolved in 120 g of tetrahydrofuran and 60 g of acetonitrile, heated to 60 ° C., stirred for 1 hour, cooled, and filtered.
  • the solid obtained here was washed with 120 g of water, dried under reduced pressure after filtration, and 26.9 g (yield 65) of white crystals of N-palmitoyl-Gly-His free form (hereinafter also simply referred to as “Pal-GH”). %).
  • Example 1 to 4 and Comparative Examples 1 to 3 (Premix preparation method) According to Table 1 below, each component was sample tube No. Weighed to 5. The pre-mix was prepared by heating the weighed composition to 70 ° C. or higher and dissolving it uniformly.
  • each component of the A phase or the above-mentioned premix is sample tube No. Weighed to 5.
  • the weighed phase A was heated to 70 ° C. or higher and dissolved uniformly.
  • another sample tube No. 5 was weighed 5.0 g of water as B phase and heated to 70 ° C. or higher. Thereafter, the A phase was added to the B phase, mixed in a heated state and stirred for about 30 seconds, and then allowed to stand and cool.
  • the solid base materials for external application of Examples 1 to 4 have a breaking strength: 0.4 to 1.3 ⁇ 10 5 Pa, and have the strength required particularly as a stick-shaped base material. Had.

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Abstract

[Problem] To provide a stick-shaped base material capable of having a desired break strength for a stick-shaped base material even if the lipid peptide compound amount is reduced. [Solution] A stick-shaped base material including: at least one type of surfactant selected from the group consisting of a betaine compound and ethylene glycol alkyl ether; water; a lipid peptide compound comprising at least one type selected from a compound indicted by formula (1) or a pharmaceutically useful salt thereof; at least one type of C8–3 saturated or unsaturated monohydric alcohol; and at least one type of thickener selected from the group consisting of an alginic acid derivative and carrageenan. (In the formula, R1 indicates a C9–23 aliphatic group, R2 indicates a hydrocarbon atom or a C1–4 alkyl group capable of having a C1–2 branched chain, R3 indicates a –(CH2)n–X group, n indicates a number 1–4, and X indicates a fused heterocycle comprising a 5-membered ring, a 6-membered ring, or a 5-membered ring and a 6-membered ring, and capable of having 1–3 amino groups, guanidino groups, –CONH2 groups, or nitrogen atoms.)

Description

多糖含有スティック状基材Polysaccharide-containing stick-like substrate

 本発明は脂質ペプチド型化合物を含有するスティック状基材に関するものであり、詳細には、脂質ペプチド型化合物の量を低減してもスティック状基材として求められる破断強度を有し得るスティック状基材に関する。 The present invention relates to a stick-shaped substrate containing a lipid peptide-type compound, and in particular, a stick-shaped substrate that can have a breaking strength required as a stick-shaped substrate even if the amount of the lipid peptide-type compound is reduced. Regarding materials.

 水性の固形状組成物は皮膚等への適用時に高い清涼感が得られることや、油性の固形状組成物と比べ使用後のべたつきがなく、さらっとした使用感であることなどから、化粧料等向けに様々な商品が上市、提案されている。
 水性固形状組成物としては従来、水と脂肪酸石鹸と油分と粉末を含有する固形状水中油型メーキャップ化粧料(特許文献1)、アルキル及び/またはアルケニルオリゴグリコシド、油性物質、及びノニオン性乳化剤を含有するスティック状の水性化粧品(特許文献2)等が提案されている。
The aqueous solid composition provides a high refreshing feeling when applied to the skin, etc., and has no stickiness after use as compared to the oily solid composition, so that it has a smooth use feeling. A variety of products are marketed and proposed.
As an aqueous solid composition, conventionally, a solid oil-in-water makeup cosmetic (Patent Document 1) containing water, fatty acid soap, oil and powder, an alkyl and / or alkenyl oligoglycoside, an oily substance, and a nonionic emulsifier A stick-like water-based cosmetic (Patent Document 2) and the like have been proposed.

 また水性固形状組成物の一種として、水性ゲル状組成物が挙げられる。この水性ゲルを得るための添加剤として高分子ゲル化剤や低分子ゲル化剤など、種々の化合物が提案されている。例えば近年、生体安全性が高く医用材料等への展開が期待される脂質ペプチド型の低分子ゲル化剤が提案されている。 Moreover, an aqueous gel composition is mentioned as a kind of aqueous solid composition. As an additive for obtaining this aqueous gel, various compounds such as a polymer gelling agent and a low molecular gelling agent have been proposed. For example, in recent years, lipid peptide type low molecular gelling agents that have high biological safety and are expected to be developed into medical materials have been proposed.

 また、特定の構造を有する脂質ペプチド型化合物を用いることで、高い破断強度を有するスティック状基材が得られることも報告されている(特許文献3)。 It has also been reported that a stick-like substrate having a high breaking strength can be obtained by using a lipid peptide type compound having a specific structure (Patent Document 3).

特開平3-279319号公報JP-A-3-279319 特表2002-516818号公報JP-T-2002-516818 国際公開第2015/099074号パンフレットInternational Publication No. 2015/099074 Pamphlet

 特許文献3に記載のスティック状基材は、脂質ペプチド型化合物を、スティック状基材の総質量に基づき、5質量%程度使用するものであるが、脂質ペプチド型化合物は高価であり、そのため、脂質ペプチド型化合物の量を低減し得るスティック状基材が望まれる。
 従って本発明の課題は、脂質ペプチド型化合物の量を低減してもスティック状基材として求められる破断強度を有し得るスティック状基材を提供することである。
The stick-shaped substrate described in Patent Document 3 uses about 5% by mass of the lipid peptide type compound based on the total mass of the stick-shaped substrate. However, the lipid peptide type compound is expensive, and therefore, A stick-like substrate capable of reducing the amount of lipid peptide type compound is desired.
Accordingly, an object of the present invention is to provide a stick-like substrate that can have the breaking strength required as a stick-like substrate even if the amount of the lipid peptide type compound is reduced.

 本発明者らは上記課題を解決すべく鋭意研究を行った結果、低分子脂質ペプチド又はその薬学的に使用可能な塩からなる脂質ペプチド型化合物(ゲル化剤)と水とを主たる構成成分とするスティック状基材において、特定の界面活性剤と特定の増粘剤とを配合することにより、脂質ペプチド型化合物の量を低減してもスティック状基材として求められる破断強度を有し得ることを見出し、本発明を完成させた。 As a result of intensive studies to solve the above problems, the present inventors have found that a lipid peptide type compound (gelator) comprising a low-molecular-weight lipid peptide or a pharmaceutically usable salt thereof and water as main constituent components In the stick-like base material, a specific surfactant and a specific thickening agent are blended to have the breaking strength required as a stick-like base material even if the amount of lipid peptide type compound is reduced. The present invention was completed.

 すなわち本発明は、第1観点として、
ベタイン系化合物及びエチレングリコールアルキルエーテルからなる群より選択される1種以上の界面活性剤と、
水と、
下記式(1)乃至式(3)で表される化合物又はその薬学的に使用可能な塩のうちの少なくとも一種からなる脂質ペプチド型化合物と、
炭素原子数8乃至30の少なくとも一種の飽和又は不飽和の一価アルコールと、
アルギン酸誘導体及びカラギーナンからなる群より選択される1種以上の増粘剤、
を含む、スティック状基材に関する。

Figure JPOXMLDOC01-appb-C000004
(式中、R1は炭素原子数9乃至23の脂肪族基を表し、R2は水素原子、又は炭素原子数1若しくは2の分枝鎖を有し得る炭素原子数1乃至4のアルキル基を表し、R3は-(CH2n-X基を表し、nは1乃至4の数を表し、Xはアミノ基、グアニジノ基、-CONH2基、又は窒素原子を1乃至3個有し得る5員環若しくは6員環又は5員環と6員環から構成される縮合複素環を表す。)
Figure JPOXMLDOC01-appb-C000005
(式中、R4は炭素原子数9乃至23の脂肪族基を表し、R5乃至R7はそれぞれ独立して水素原子、炭素原子数1若しくは2の分枝鎖を有し得る炭素原子数1乃至4のアルキル基、又は-(CH2n-X基を表し、nは1乃至4の数を表し、Xはアミノ基、グアニジノ基、-CONH2基、又は窒素原子を1乃至3個有し得る5員環若しくは6員環又は5員環と6員環から構成される縮合複素環を表す。)
Figure JPOXMLDOC01-appb-C000006
(式中、R8は炭素原子数9乃至23の脂肪族基を表し、R9乃至R12はそれぞれ独立して水素原子、炭素原子数1若しくは2の分枝鎖を有し得る炭素原子数1乃至4のアルキル基、又は-(CH2n-X基を表し、nは1乃至4の数を表し、Xはアミノ基、グアニジノ基、-CONH2基、又は窒素原子を1乃至3個有し得る5員環若しくは6員環又は5員環と6員環から構成される縮合複素環を表す。)
第2観点として、前記界面活性剤が、エチレングリコールアルキルエーテルである、第1観点に記載のスティック状基材に関する。
第3観点として、更に、1,2-アルカンジオール又は1,3-アルカンジオールを含む、第1観点に記載のスティック状基材に関する。
 第4観点として、前記アルギン酸誘導体が、アルギン酸多価アルコールエステルである、第3観点に記載のスティック状基材に関する。
 第5観点として、前記増粘剤が、スティック状基材の総質量に基いて0.1~1.0質量%の割合にて含まれてなる、第1観点乃至第4観点のうち何れか一つに記載のスティック状基材に関する。
 第6観点として、前記ベタイン系化合物が、硫酸型ベタインである、第3観点乃至第5観点のうち何れか一つに記載のスティック状基材に関する。
 第7観点として、前記一価アルコールが、ミリスチルアルコール、セタノール、ステアリルアルコール及びベヘニルアルコールからなる群から選択される1種以上の化合物である、第1観点乃至第6観点のうち何れか一つに記載のスティック状基材に関する。
 第8観点として、前記脂質ペプチド型化合物が、スティック状基材の総質量に基いて0.1~2質量%の割合にて含まれてなる、第1観点乃至第7観点のうち何れか一つに記載のスティック状基材に関する。 That is, the present invention provides the first aspect as follows:
One or more surfactants selected from the group consisting of betaine compounds and ethylene glycol alkyl ethers;
water and,
A lipid peptide type compound comprising at least one of the compounds represented by the following formulas (1) to (3) or a pharmaceutically usable salt thereof;
At least one saturated or unsaturated monohydric alcohol having 8 to 30 carbon atoms;
One or more thickeners selected from the group consisting of alginic acid derivatives and carrageenan,
The present invention relates to a stick-like substrate.
Figure JPOXMLDOC01-appb-C000004
(In the formula, R 1 represents an aliphatic group having 9 to 23 carbon atoms, and R 2 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms which may have a branched chain having 1 or 2 carbon atoms. R 3 represents a — (CH 2 ) n —X group, n represents a number of 1 to 4, X represents an amino group, a guanidino group, a —CONH 2 group, or 1 to 3 nitrogen atoms. And represents a condensed heterocyclic ring composed of a 5-membered ring or a 6-membered ring or a 5-membered ring and a 6-membered ring.)
Figure JPOXMLDOC01-appb-C000005
(Wherein R 4 represents an aliphatic group having 9 to 23 carbon atoms, and R 5 to R 7 each independently represents a hydrogen atom or a carbon atom having a branched chain having 1 or 2 carbon atoms. 1 to 4 alkyl groups or — (CH 2 ) n —X group, n represents a number of 1 to 4, and X represents an amino group, a guanidino group, a —CONH 2 group, or a nitrogen atom of 1 to 3 This represents a 5-membered ring or 6-membered ring which may have one or a condensed heterocyclic ring composed of a 5-membered ring and a 6-membered ring.)
Figure JPOXMLDOC01-appb-C000006
(In the formula, R 8 represents an aliphatic group having 9 to 23 carbon atoms, and R 9 to R 12 each independently represents a hydrogen atom, or a carbon atom number that can have a branched chain having 1 or 2 carbon atoms. 1 to 4 alkyl, or - (CH 2) n represents an -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3 This represents a 5-membered ring or 6-membered ring which may have one or a condensed heterocyclic ring composed of a 5-membered ring and a 6-membered ring.)
As a second aspect, the present invention relates to the stick-shaped substrate according to the first aspect, in which the surfactant is ethylene glycol alkyl ether.
As a third aspect, the present invention further relates to the stick-like substrate according to the first aspect, further comprising 1,2-alkanediol or 1,3-alkanediol.
As a fourth aspect, the present invention relates to the stick-shaped substrate according to the third aspect, in which the alginic acid derivative is an alginate polyhydric alcohol ester.
As a fifth aspect, any one of the first aspect to the fourth aspect, wherein the thickener is included in a proportion of 0.1 to 1.0% by mass based on the total mass of the stick-like substrate. The present invention relates to the stick-like substrate described in one.
As a sixth aspect, the present invention relates to the stick-like substrate according to any one of the third to fifth aspects, wherein the betaine compound is sulfate-type betaine.
As a seventh aspect, the monohydric alcohol is one or more compounds selected from the group consisting of myristyl alcohol, cetanol, stearyl alcohol, and behenyl alcohol, according to any one of the first to sixth aspects. This relates to a stick-like substrate.
As an eighth aspect, any one of the first aspect to the seventh aspect, wherein the lipid peptide type compound is contained at a ratio of 0.1 to 2% by mass based on the total mass of the stick-like substrate. It relates to the stick-like base material described in one.

 本発明によれば、脂質ペプチド型化合物の量を低減してもスティック状基材として求められる破断強度を有し得るスティック状基材を提供できる。
 特に本発明のスティック状基材では、特定の界面活性剤と特定の増粘剤とを使用することにより、該基材の総質量に基いて脂質ペプチド型化合物の量を低減し、例えば、1質量%以下とした場合においても、スティック状基材として求められる破断強度を有し得る。
ADVANTAGE OF THE INVENTION According to this invention, even if it reduces the quantity of a lipid peptide type compound, the stick-shaped base material which can have the breaking strength calculated | required as a stick-shaped base material can be provided.
In particular, in the stick-shaped substrate of the present invention, the use of a specific surfactant and a specific thickener reduces the amount of lipid peptide type compound based on the total mass of the substrate. Even when the content is less than or equal to mass%, it may have a breaking strength required for a stick-like substrate.

 また本発明のスティック状基材に含まれる脂質ペプチド化合物は、脂質とペプチドのみから構成される非常に安全性の高い人工低分子化合物である。また該化合物は、例えば従来提案されている合成高分子型のゲルの形成時に必要とされた架橋剤等を用いることなく水性ゲルを形成することができるため、得られるスティック状基材において未反応の架橋剤などの未反応物質の残存といった問題が起こらない。
 さらに本発明のスティック状基材において添加剤として含まれる各種成分は食品や化粧品、医薬品の添加剤として汎用の添加剤である。
Moreover, the lipid peptide compound contained in the stick-like substrate of the present invention is a very safe artificial low molecular weight compound composed only of lipid and peptide. In addition, the compound can form an aqueous gel without using a crosslinking agent or the like required for forming a synthetic polymer type gel that has been proposed in the past. The problem of remaining unreacted materials such as cross-linking agents does not occur.
Furthermore, various components contained as additives in the stick-shaped substrate of the present invention are general-purpose additives as additives for foods, cosmetics, and pharmaceuticals.

 すなわち、本発明のスティック状基材は生体安全性が高く、特に、医薬品や化粧品等において要求される安全性の観点からみて、上記用途において非常に有用である。
 その上、本発明のスティック状基材は、ヒトの肌等に適用した場合に清涼感がよく、また折れたり変形したりせず、伸びがよい基材となることが期待されるため、医薬品向けや化粧品向けのスティック状の基材として非常に有用である。
That is, the stick-shaped substrate of the present invention has high biological safety, and is particularly useful in the above applications from the viewpoint of safety required for pharmaceuticals and cosmetics.
In addition, the stick-like base material of the present invention is expected to be a base material having a good refreshing feeling when applied to human skin, etc. It is very useful as a stick-like base material for cosmetics and cosmetics.

 本発明は、ベタイン系化合物及びエチレングリコールアルキルエーテルからなる群より選択される1種以上の界面活性剤と、水と、下記式(1)乃至式(3)で表される化合物又はその薬学的に使用可能な塩のうちの少なくとも一種からなる脂質ペプチド型化合物と、1,2-アルカンジオール又は1,3-アルカンジオールと、炭素原子数8乃至30の少なくとも一種の飽和又は不飽和の一価アルコールと、アルギン酸誘導体及びカラギーナンからなる群より選択される1種以上の増粘剤、及び所望によりその他添加剤とを含むスティック状基材に関する。
 以下、各構成成分について説明する。
The present invention relates to one or more surfactants selected from the group consisting of betaine compounds and ethylene glycol alkyl ethers, water, compounds represented by the following formulas (1) to (3), or pharmaceuticals thereof. A lipid peptide-type compound comprising at least one of the salts that can be used in the above, 1,2-alkanediol or 1,3-alkanediol, and at least one saturated or unsaturated monovalent group having 8 to 30 carbon atoms. The present invention relates to a stick-like substrate comprising alcohol, one or more thickeners selected from the group consisting of alginic acid derivatives and carrageenan, and optionally other additives.
Hereinafter, each component will be described.

[脂質ペプチド型化合物]
 本発明のスティック状基材において用いる脂質ペプチド型化合物としては、下記式(1)乃至式(3)で表される化合物(脂質ペプチド)又はその薬学的に使用可能な塩(疎水性部位である脂質部と親水性部位であるペプチド部とを有する低分子化合物)を用いることができる。

Figure JPOXMLDOC01-appb-C000007
[Lipid peptide type compound]
The lipid peptide type compound used in the stick-shaped substrate of the present invention is a compound (lipid peptide) represented by the following formulas (1) to (3) or a pharmaceutically usable salt thereof (hydrophobic site). A low molecular compound having a lipid part and a peptide part which is a hydrophilic part) can be used.
Figure JPOXMLDOC01-appb-C000007

 上記式(1)において、R1は炭素原子数9乃至23の脂肪族基を表し、好ましくは、R1は不飽和結合を0乃至2個有し得る炭素原子数11乃至23の直鎖状脂肪族基であることが望ましい。
 R1と隣接するカルボニル基で構成される脂質部(アシル基)の具体例としては、ラウロイル基、ドデシルカルボニル基、ミリストイル基、テトラデシルカルボニル基、パルミトイル基、マルガロイル基、オレオイル基、エライドイル基、リノレオイル基、ステアロイル基、バクセノイル基、オクタデシルカルボニル基、アラキドイル基、エイコシルカルボニル基、ベヘノイル基、エルカノイル基、ドコシルカルボニル基、リグノセイル基、ネルボノイル基等を挙げることができ、特に好ましいものとして、ラウロイル基、ミリストイル基、パルミトイル基、マルガロイル基、ステアロイル基、オレオイル基、エライドイル基及びベヘノイル基が挙げられる。
In the above formula (1), R 1 represents an aliphatic group having 9 to 23 carbon atoms, and preferably R 1 is a straight chain having 11 to 23 carbon atoms which may have 0 to 2 unsaturated bonds. An aliphatic group is desirable.
Specific examples of the lipid moiety (acyl group) composed of a carbonyl group adjacent to R 1 include lauroyl group, dodecylcarbonyl group, myristoyl group, tetradecylcarbonyl group, palmitoyl group, margaroyl group, oleoyl group, and elideoyl group. Linoleoyl group, stearoyl group, baccenoyl group, octadecylcarbonyl group, arachidyl group, eicosylcarbonyl group, behenoyl group, ercanoyl group, docosylcarbonyl group, lignoceyl group, nerbonoyl group, etc. Examples include lauroyl group, myristoyl group, palmitoyl group, margaroyl group, stearoyl group, oleoyl group, elidoyl group, and behenoyl group.

 上記式(1)において、ペプチド部に含まれるR2は、水素原子、又は炭素原子数1若しくは2の分枝鎖を有し得る炭素原子数1乃至4のアルキル基を表す。
 上記炭素原子数1若しくは2の分岐鎖を有し得る炭素原子数1乃至4のアルキル基とは、主鎖の炭素原子数が1乃至4であり、かつ炭素原子数1若しくは2の分岐鎖を有し得るアルキル基を意味し、その具体例としては、メチル基、エチル基、n-プロピル基、i-プロピル基、n-ブチル基、i-ブチル基、sec-ブチル基又はtert-ブチル基などが挙げられる。
 上記R2は好ましくは、水素原子、又は炭素原子数1の分岐鎖を有し得る炭素原子数1乃至3のアルキル基であり、より好ましくは水素原子である。
 炭素原子数1の分岐鎖を有し得る炭素原子数1乃至3のアルキル基とは、主鎖の炭素原子数が1乃至3であり、かつ炭素原子数1の分岐鎖を有し得るアルキル基を意味し、その具体例としては、メチル基、エチル基、n-プロピル基、i-プロピル基、i-ブチル基又はsec-ブチル基などが挙げられ、好ましくはメチル基、i-プロピル基、i-ブチル基又はsec-ブチル基である。
In the above formula (1), R 2 contained in the peptide part represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms which may have a branched chain having 1 or 2 carbon atoms.
The alkyl group having 1 to 4 carbon atoms that may have a branched chain having 1 or 2 carbon atoms is a branched chain having 1 to 4 carbon atoms in the main chain and 1 or 2 carbon atoms. Means an alkyl group which may have, and specific examples thereof include methyl group, ethyl group, n-propyl group, i-propyl group, n-butyl group, i-butyl group, sec-butyl group or tert-butyl group Etc.
R 2 is preferably a hydrogen atom or an alkyl group having 1 to 3 carbon atoms which may have a branched chain having 1 carbon atom, and more preferably a hydrogen atom.
The alkyl group having 1 to 3 carbon atoms which can have a branched chain having 1 carbon atom is an alkyl group having 1 to 3 carbon atoms in the main chain and having a branched chain having 1 carbon atom. Specific examples thereof include a methyl group, an ethyl group, an n-propyl group, an i-propyl group, an i-butyl group, or a sec-butyl group, preferably a methyl group, an i-propyl group, An i-butyl group or a sec-butyl group.

 上記式(1)において、R3は-(CH2)n-X基を表す。上記-(CH2)n-X基において、nは1乃至4の数を表し、Xはアミノ基、グアニジノ基、-CONH2基、又は窒素原子を1乃至3個有し得る5員環式基若しくは6員環式基、又は5員環と6員環から構成される縮合複素環式基を表す。
 上記R3を表す-(CH2)n-X基において、Xは好ましくはアミノ基、グアニジノ基、カルバモイル基(-CONH2基)、ピロール基、イミダゾール基、ピラゾール基又はインドール基であり、より好ましくはイミダゾール基である。また、上記-(CH2)n-X基において、nは好ましくは1又は2であり、より好ましくは1である。
 従って、上記-(CH2)n-基は、好ましくはアミノメチル基、2-アミノエチル基、3-アミノプロピル基、4-アミノブチル基、カルバモイルメチル基、2-カルバモイルエチル基、3-カルバモイルブチル基、2-グアニジノエチル基、3-グアニジノブチル基、ピロールメチル基、4-イミダゾールメチル基、ピラゾールメチル基、又は3-インドールメチル基を表し、より好ましくは4-アミノブチル基、カルバモイルメチル基、2-カルバモイルエチル基、3-グアニジノブチル基、4-イミダゾールメチル基又は3-インドールメチル基を表し、さらに好ましくは4-イミダゾールメチル基である。
In the above formula (1), R 3 represents a — (CH 2 ) n—X group. In the — (CH 2 ) n—X group, n represents a number of 1 to 4, and X is an amino group, a guanidino group, a —CONH 2 group, or a 5-membered cyclic group having 1 to 3 nitrogen atoms. Represents a group, a 6-membered cyclic group, or a condensed heterocyclic group composed of a 5-membered ring and a 6-membered ring.
In the — (CH 2 ) n—X group representing R 3 , X is preferably an amino group, guanidino group, carbamoyl group (—CONH 2 group), pyrrole group, imidazole group, pyrazole group or indole group, and more Preferably it is an imidazole group. Also, the - in (CH 2) n-X group, n is preferably 1 or 2, more preferably 1.
Therefore, the — (CH 2 ) n- group is preferably an aminomethyl group, 2-aminoethyl group, 3-aminopropyl group, 4-aminobutyl group, carbamoylmethyl group, 2-carbamoylethyl group, 3-carbamoyl group. Represents a butyl group, a 2-guanidinoethyl group, a 3-guanidinobutyl group, a pyrrolemethyl group, a 4-imidazolemethyl group, a pyrazolemethyl group, or a 3-indolemethyl group, more preferably a 4-aminobutyl group, a carbamoylmethyl group Represents a 2-carbamoylethyl group, a 3-guanidinobutyl group, a 4-imidazolemethyl group or a 3-indolemethyl group, more preferably a 4-imidazolemethyl group.

 上記式(1)で表される化合物において、脂質ペプチド型化合物として特に好適な脂質ペプチドとしては、以下の脂質部とペプチド部(アミノ酸集合部)から形成される化合物である。なおアミノ酸の略称としては、アラニン(Ala)、アスパラギン(Asn)、グルタミン(Gln)、グリシン(Gly)、ヒスチジン(His)、イソロシン(Ile)、ロイシン(Leu)、リジン(Lys)、トリプトファン(Trp)、バリン(Val)を表す。:ラウロイル-Gly-His、ラウロイル-Gly-Gln、ラウロイル-Gly-Asn、ラウロイル-Gly-Trp、ラウロイル-Gly-Lys、ラウロイル-Ala-His、ラウロイル-Ala-Gln、ラウロイル-Ala-Asn、ラウロイル-Ala-Trp、ラウロイル-Ala-Lys;ミリストイル-Gly-His、ミリストイル-Gly-Gln、ミリストイル-Gly-Asn、ミリストイル-Gly-Trp、ミリストイル-Gly-Lys、ミリストイル-Ala-His、ミリストイル-Ala-Gln、ミリストイル-Ala-Asn、ミリストイル-Ala-Trp、ミリストイル-Ala-Lys;パルミトイル-Gly-His、パルミトイル-Gly-Gln、パルミトイル-Gly-Asn、パルミトイル-Gly-Trp、パルミトイル-Gly-Lys、パルミトイル-Ala-His、パルミトイル-Ala-Gln、パルミトイル-Ala-Asn、パルミトイル-Ala-Trp、パルミトイル-Ala-Lys;ステアロイル-Gly-His、ステアロイル-Gly-Gln、ステアロイル-Gly-Asn、ステアロイル-Gly-Trp、ステアロイル-Gly-Lys、ステアロイル-Ala-His、ステアロイル-Ala-Gln、ステアロイル-Ala-Asn、ステアロイル-Ala-Trp、ステアロイル-Ala-Lys。 In the compound represented by the above formula (1), a lipid peptide particularly suitable as a lipid peptide type compound is a compound formed from the following lipid part and peptide part (amino acid assembly part). As abbreviations for amino acids, alanine (Ala), asparagine (Asn), glutamine (Gln), glycine (Gly), histidine (His), isorosine (Ile), leucine (Leu), lysine (Lys), tryptophan (Trp) ), Valine (Val). Lauroyl-Gly-His, Lauroyl-Gly-Gln, Lauroyl-Gly-Asn, Lauroyl-Gly-Trp, Lauroyl-Gly-Lys, Lauroyl-Ala-His, Lauroyl-Ala-Gln, Lauroyl-Ala-Asn, Lauroyl -Ala-Trp, Lauroyl-Ala-Lys; Myristoyl-Gly-His, Myristoyl-Gly-Gln, Myristoyl-Gly-Asn, Myristoyl-Gly-Trp, Myristoyl-Gly-Lys, Myristoyl-Ala-His, Myristoyl-Ala -Gln, Myristoyl-Ala-Asn, Myristoyl-Ala-Trp, Myristoyl-Ala-Lys; Palmitoyl-Gly-His, Palmitoyl-Gly-Gln, Palmitoyl-Gly-A n, Palmitoyl-Gly-Trp, Palmitoyl-Gly-Lys, Palmitoyl-Ala-His, Palmitoyl-Ala-Gln, Palmitoyl-Ala-Asn, Palmitoyl-Ala-Trp, Palmitoyl-Ala-Lys; Stearoyl-Gly-His Stearoyl-Gly-Gln, stearoyl-Gly-Asn, stearoyl-Gly-Trp, stearoyl-Gly-Lys, stearoyl-Ala-His, stearoyl-Ala-Gln, stearoyl-Ala-Asn, stearoyl-Ala-Trp, stearoyl- Ala-Lys.

 最も好ましいものとして、ラウロイル-Gly-His、ラウロイル-Ala-His-ミリストイル-Gly-His、ミリストイル-Ala-His;パルミトイル-Gly-His、パルミトイル-Ala-His;ステアロイル-Gly-His、ステアロイル-Ala-Hisが挙げられる。 Most preferred are lauroyl-Gly-His, lauroyl-Ala-His-myristoyl-Gly-His, myristoyl-Ala-His; palmitoyl-Gly-His, palmitoyl-Ala-His; stearoyl-Gly-His, stearoyl-Ala -His.

Figure JPOXMLDOC01-appb-C000008
Figure JPOXMLDOC01-appb-C000008

 上記式(2)において、R4は炭素原子数9乃至23の脂肪族基を表し、好ましい具体例としては、前出のR1で定義したものと同じ基が挙げられる。
 上記式(2)において、R5乃至R7は、それぞれ独立して、水素原子、又は炭素原子数1若しくは2の分枝鎖を有し得る炭素原子数1乃至4のアルキル基、又は-(CH2)n-X基を表し、好ましくは、R5乃至R7のうち少なくとも一つ以上が-(CH2)n-X基を表す。nは1乃至4の数を表し、Xはアミノ基、グアニジノ基、-CONH2基、又は窒素原子を1乃至3個有し得る5員環式基若しくは6員環式基、又は5員環と6員環から構成される縮合複素環式基を表す。ここでR5乃至R7の好ましい具体例としては、前出のR2及びR3で定義したものと同じ基が挙げられる。
In the above formula (2), R 4 represents an aliphatic group having 9 to 23 carbon atoms, and preferred specific examples include the same groups as defined for R 1 above.
In the above formula (2), R 5 to R 7 are each independently a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain having 1 or 2 carbon atoms, or — ( CH 2 ) nX group, and preferably at least one of R 5 to R 7 represents a — (CH 2 ) nX group. n represents a number of 1 to 4, and X represents an amino group, a guanidino group, a —CONH 2 group, or a 5-membered cyclic group or a 6-membered cyclic group that may have 1 to 3 nitrogen atoms, or a 5-membered ring And a condensed heterocyclic group composed of a 6-membered ring. Here, preferred specific examples of R 5 to R 7 include the same groups as defined for R 2 and R 3 above.

 上記式(2)で表される化合物において、好適な脂質ペプチドとしては、以下の脂質部とペプチド部(アミノ酸集合部)から形成される化合物である。例えば、
ラウロイル-Gly-Gly-His、ラウロイル-Gly-Gly-Gln、ラウロイル-Gly-Gly-Asn、ラウロイル-Gly-Gly-Trp、ラウロイル-Gly-Gly-Lys、ラウロイル-Gly-Ala-His、ラウロイル-Gly-Ala-Gln、ラウロイル-Gly-Ala-Asn、ラウロイル-Gly-Ala-Trp、ラウロイル-Gly-Ala-Lys、ラウロイル-Ala-Gly-His、ラウロイル-Ala-Gly-Gln、ラウロイル-Ala-Gly-Asn、ラウロイル-Ala-Gly-Trp、ラウロイル-Ala-Gly-Lys、ラウロイル-Gly-His-Gly、ラウロイル-His-Gly-Gly、ミリストイル-Gly-Gly-His、ミリストイル-Gly-Gly-Gln、ミリストイル-Gly-Gly-Asn、ミリストイル-Gly-Gly-Trp、ミリストイル-Gly-Gly-Lys、ミリストイル-Gly-Ala-His、ミリストイル-Gly-Ala-Gln、ミリストイル-Gly-Ala-Asn、ミリストイル-Gly-Ala-Trp、ミリストイル-Gly-Ala-Lys、ミリストイル-Ala-Gly-His、ミリストイル-Ala-Gly-Gln、ミリストイル-Ala-Gly-Asn、ミリストイル-Ala-Gly-Trp、ミリストイル-Ala-Gly-Lys、ミリストイル-Gly-His-Gly、ミリストイル-His-Gly-Gly、パルミトイル-Gly-Gly-His、パルミトイル-Gly-Gly-Gln、パルミトイル-Gly-Gly-Asn、パルミトイル-Gly-Gly-Trp、パルミトイル-Gly-Gly-Lys、パルミトイル-Gly-Ala-His、パルミトイル-Gly-Ala-Gln、パルミトイル-Gly-Ala-Asn、パルミトイル-Gly-Ala-Trp、パルミトイル-Gly-Ala-Lys、パルミトイル-Ala-Gly-His、パルミトイル-Ala-Gly-Gln、パルミトイル-Ala-Gly-Asn、パルミトイル-Ala-Gly-Trp、パルミトイル-Ala-Gly-Lys、パルミトイル-Gly-His-Gly、パルミトイル-His-Gly-Gly、ステアロイル-Gly-Gly-His、ステアロイル-Gly-Gly-Gln、ステアロイル-Gly-Gly-Asn、ステアロイル-Gly-Gly-Trp、ステアロイル-Gly-Gly-Lys、ステアロイル-Gly-Ala-His、ステアロイル-Gly-Ala-Gln、ステアロイル-Gly-Ala-Asn、ステアロイル-Gly-Ala-Trp、ステアロイル-Gly-Ala-Lys、ステアロイル-Ala-Gly-His、ステアロイル-Ala-Gly-Gln、ステアロイル-Ala-Gly-Asn、ステアロイル-Ala-Gly-Trp、ステアロイル-Ala-Gly-Lys、ステアロイル-Gly-His-Gly、ステアロイル-His-Gly-Gly。
In the compound represented by the above formula (2), a preferable lipid peptide is a compound formed from the following lipid part and peptide part (amino acid assembly part). For example,
Lauroyl-Gly-Gly-His, Lauroyl-Gly-Gly-Gln, Lauroyl-Gly-Gly-Asn, Lauroyl-Gly-Gly-Trp, Lauroyl-Gly-Gly-Lys, Lauroyl-Gly-Ala-His, Lauroyl-His Gly-Ala-Gln, Lauroyl-Gly-Ala-Asn, Lauroyl-Gly-Ala-Trp, Lauroyl-Gly-Ala-Lys, Lauroyl-Ala-Gly-His, Lauroyl-Ala-Gly-Gln, Lauroyl-Ala- Gly-Asn, Lauroyl-Ala-Gly-Trp, Lauroyl-Ala-Gly-Lys, Lauroyl-Gly-His-Gly, Lauroyl-His-Gly-Gly, Myristoyl-Gly-Gly-His, Myristoyl-G y-Gly-Gln, Myristoyl-Gly-Gly-Asn, Myristoyl-Gly-Gly-Trp, Myristoyl-Gly-Gly-Lys, Myristoyl-Gly-Ala-His, Myristoyl-Gly-Ala-Gln, Myristoyl-Gly- Ala-Asn, Myristoyl-Gly-Ala-Trp, Myristoyl-Gly-Ala-Lys, Myristoyl-Ala-Gly-His, Myristoyl-Ala-Gly-Gln, Myristoyl-Ala-Gly-Asn, Myristoyl-Ala-Gly- Trp, Myristoyl-Ala-Gly-Lys, Myristoyl-Gly-His-Gly, Myristoyl-His-Gly-Gly, Palmitoyl-Gly-Gly-His, Palmitoyl-Gly-Gly-Gln Palmitoyl-Gly-Gly-Asn, Palmitoyl-Gly-Gly-Trp, Palmitoyl-Gly-Gly-Lys, Palmitoyl-Gly-Ala-His, Palmitoyl-Gly-Ala-Gln, Palmitoyl-Gly-Ala-Asyl Gly-Ala-Trp, Palmitoyl-Gly-Ala-Lys, Palmitoyl-Ala-Gly-His, Palmitoyl-Ala-Gly-Gln, Palmitoyl-Ala-Gly-Asn, Palmitoyl-Ala-Gly-Trp, Palmitoyl-Ala- Gly-Lys, Palmitoyl-Gly-His-Gly, Palmitoyl-His-Gly-Gly, Stearoyl-Gly-Gly-His, Stearoyl-Gly-Gly-Gln, Stearoyl-Gly -Gly-Asn, stearoyl-Gly-Gly-Trp, stearoyl-Gly-Gly-Lys, stearoyl-Gly-Ala-His, stearoyl-Gly-Ala-Gln, stearoyl-Gly-Ala-Asn, stearoyl-Gly-Ala -Trp, stearoyl-Gly-Ala-Lys, stearoyl-Ala-Gly-His, stearoyl-Ala-Gly-Gln, stearoyl-Ala-Gly-Asn, stearoyl-Ala-Gly-Trp, stearoyl-Ala-Gly-Lys Stearoyl-Gly-His-Gly, stearoyl-His-Gly-Gly.

 これらのうち、最も好ましいものとして、ラウロイル-Gly-Gly-His、ミリストイル-Gly-Gly-His、パルミトイル-Gly-Gly-His、パルミトイル-Gly-His-Gly、パルミトイル-His-Gly-Gly、ステアロイル-Gly-Gly-Hisが挙げられる。 Of these, lauroyl-Gly-Gly-His, myristoyl-Gly-Gly-His, palmitoyl-Gly-Gly-His, palmitoyl-Gly-His-Gly, palmitoyl-His-Gly-Gly, stearoyl -Gly-Gly-His.

Figure JPOXMLDOC01-appb-C000009
Figure JPOXMLDOC01-appb-C000009

 上記式(3)において、R8は炭素原子数9乃至23の脂肪族基を表し、好ましい具体例としては、前出のR1で定義したものと同じ基が挙げられる。
 上記式(3)において、R9乃至R12は、それぞれ独立して、水素原子、又は炭素原子数1若しくは2の分枝鎖を有し得る炭素原子数1乃至4のアルキル基、又は-(CH2)n-X基を表し、好ましくは、R9乃至R12のうち少なくとも一つ以上が-(CH2)n-X基を表す。nは1乃至4の数を表し、Xはアミノ基、グアニジノ基、-CONH2基、又は窒素原子を1乃至3個有し得る5員環式基若しくは6員環式基、又は5員環と6員環から構成される縮合複素環式基を表す。ここでR9乃至R12の好ましい具体例としては、前出のR2及びR3で定義したものと同じ基が挙げられる。
In the above formula (3), R 8 represents an aliphatic group having 9 to 23 carbon atoms, and preferred specific examples include the same groups as defined for R 1 above.
In the above formula (3), R 9 to R 12 are each independently a hydrogen atom, an alkyl group having 1 to 4 carbon atoms which may have a branched chain having 1 or 2 carbon atoms, or — ( CH 2 ) nX group, and preferably at least one of R 9 to R 12 represents a — (CH 2 ) nX group. n represents a number of 1 to 4, and X represents an amino group, a guanidino group, a —CONH 2 group, or a 5-membered cyclic group or a 6-membered cyclic group that may have 1 to 3 nitrogen atoms, or a 5-membered ring And a condensed heterocyclic group composed of a 6-membered ring. Here, preferred specific examples of R 9 to R 12 include the same groups as defined for R 2 and R 3 above.

 したがって上記式(3)で表される化合物において、好適な脂質ペプチド型化合物として、特に好適な脂質ペプチドとしては、ラウロイル-Gly-Gly-Gly-His、ミリストイル-Gly-Gly-Gly-His、パルミトイル-Gly-Gly-Gly-His、パルミトイル-Gly-Gly-His-Gly、パルミトイル-Gly-His-Gly-Gly、パルミトイル-His-Gly-Gly-Gly、ステアロイル-Gly-Gly-Gly-His等が挙げられる。 Therefore, in the compound represented by the above formula (3), as preferred lipid peptide type compounds, particularly preferred lipid peptides include lauroyl-Gly-Gly-Gly-His, myristoyl-Gly-Gly-Gly-His, palmitoyl. -Gly-Gly-Gly-His, Palmitoyl-Gly-Gly-His-Gly, Palmitoyl-Gly-His-Gly-Gly, Palmitoyl-His-Gly-Gly-Gly, Stearoyl-Gly-Gly-Gly-His, etc. Can be mentioned.

 本発明において、脂質ペプチド型化合物の配合量は、得られるスティック状基材の総質量に対して、例えば0.1乃至2質量%、好ましくは、0.3乃至1.5質量%、より好ましくは0.5乃至1.0質量%である。
 なお本発明において用いられる脂質ペプチド型化合物は、上記式(1)乃至式(3)で表される化合物(脂質ペプチド)又はその薬学的な使用可能な塩のうちの少なくとも一種からなり、ヒドロゲル化剤としてこれら化合物を一種単独で、或いは二種以上を組み合わせて用いることができる。
In the present invention, the amount of the lipid peptide type compound is, for example, 0.1 to 2% by mass, preferably 0.3 to 1.5% by mass, and more preferably based on the total mass of the stick-like substrate to be obtained. Is 0.5 to 1.0 mass%.
The lipid peptide type compound used in the present invention comprises at least one of the compounds represented by the above formulas (1) to (3) (lipid peptide) or a pharmaceutically usable salt thereof, and is hydrogelated. These compounds can be used alone or in combination of two or more as an agent.

[界面活性剤]
 本発明のスティック状基材において使用する界面活性剤としては、分子内に親水部と疎水部を有し、かつ該親水部がベタイン構造を有する化合物(以下、ベタイン系化合物とも称する)及びエチレングリコールアルキルエーテルが挙げられる。
[Surfactant]
The surfactant used in the stick-shaped substrate of the present invention includes a compound having a hydrophilic part and a hydrophobic part in the molecule, and the hydrophilic part having a betaine structure (hereinafter also referred to as a betaine compound) and ethylene glycol. An alkyl ether is mentioned.

 上述のようなベタイン系化合物としては、例えばラウリルジメチルアミノ酢酸ベタイン(ラウリルベタイン)等のN-アルキル-N,N-ジメチルアミノ酸ベタイン;コカミドプロピルベタイン、ラウラミドプロピルベタイン等の脂肪酸アミドアルキル-N,N-ジメチルアミノ酸ベタイン;ココアンホ酢酸ナトリウム、ラウロアンホ酢酸ナトリウム等のイミダゾリン型ベタイン;ラウリルヒドロキシスルホベタイン、アルキルジメチルタウリン等のアルキルスルホベタイン;アルキルジメチルアミノエタノール硫酸エステル等の硫酸型ベタイン;アルキルジメチルアミノエタノールリン酸エステル等のリン酸型ベタイン等、両性界面活性剤として既知のベタイン系化合物を使用出来る。
 ベタイン系化合物としては、硫酸型ベタインが好ましい。
 また、上記ベタイン系化合物として、ホスファチジルコリン、ホスファチジルエタノールアミン、ホスファチジルセリン、ホスファチジルイノシトール、ホスファチジルグリセロール、ジホスファチジルグリセロール(カルジオリピン)、ホスファチジン酸などのグリセロリン脂質;リゾホスファチジルコリン(リゾレシチン)、リゾホスファチジルエタノールアミン、リゾホスファチジルセリン、リゾホスファチジルイノシトール、リゾホスファチジルグリセロール、リゾホスファチジン酸などのリゾグリセロリン脂質;スフィンゴミエリンなどのスフィンゴリン脂質;及びこれらの水素添加物などが挙げられる。これらのリン脂質は、大豆、卵黄などの動植物由来のものでもよく、化学的もしくは酵素的方法により合成されたものでもよい。
 上記ベタイン系化合物の中でも、好ましくは、ラウリルジメチルアミノ酢酸ベタイン、ラウリン酸アミドプロピルベタイン、ラウリルヒドロキシスルホベタイン、ステアリルベタイン、リゾホスファチジルコリン(リゾレシチン)、リゾホスファチジルエタノールアミン、リゾホスファチジルセリン、リゾホスファチジルイノシトール、リゾホスファチジルグリセロール、リゾホスファチジン酸などが挙げられ、さらに好ましくは、ラウリルヒドロキシスルホベタインが挙げられる。
Examples of the betaine compounds as described above include N-alkyl-N, N-dimethylamino acid betaines such as lauryldimethylaminoacetic acid betaine (lauryl betaine); fatty acid amide alkyl-N such as cocamidopropyl betaine and lauramidopropyl betaine. N-dimethylamino acid betaine; imidazoline-type betaines such as sodium cocoamphoacetate and sodium lauroamphoacetate; alkylsulfobetaines such as laurylhydroxysulfobetaine and alkyldimethyltaurine; sulfate-type betaines such as alkyldimethylaminoethanol sulfate; alkyldimethylaminoethanol Known betaine compounds such as phosphate-type betaines such as phosphate esters can be used as amphoteric surfactants.
As the betaine compound, sulfate-type betaine is preferable.
Examples of the betaine compounds include phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, phosphatidylglycerol, diphosphatidylglycerol (cardiolipin), phosphatidic acid and other glycerophospholipids; lysophosphatidylcholine (lysolecithin), lysophosphatidylethanolamine, Examples thereof include lysoglycerophospholipids such as serine, lysophosphatidylinositol, lysophosphatidylglycerol, and lysophosphatidic acid; sphingophospholipids such as sphingomyelin; and hydrogenated products thereof. These phospholipids may be derived from animals and plants such as soybeans and egg yolks, or may be synthesized by a chemical or enzymatic method.
Among the betaine compounds, preferably lauryldimethylaminoacetic acid betaine, lauric acid amidopropyl betaine, lauryl hydroxysulfobetaine, stearyl betaine, lysophosphatidylcholine (lysolecithin), lysophosphatidylethanolamine, lysophosphatidylserine, lysophosphatidylinositol, lyso Examples include phosphatidylglycerol and lysophosphatidic acid, and more preferably lauryl hydroxysulfobetaine.

 上記エチレングリコールアルキルエーテルとしては、ポリオキシエチレンアルキルエーテル、ポリオキシエチレンラウリルエーテル、ポリオキシエチレンパルミトイルエーテル、ポリオキシエチレンステアリルエーテル等が挙げられるが、ポリオキシエチレンラウリルエーテルが好ましい。
 またエチレングリコールアルキルエーテルは市販品も使用し得、そのような製品としては、例えば花王(株)のエマルゲン(登録商標)シリーズ及びエマノーン(登録商標)シリーズのうち、エマルゲン102KG、エマルゲン103、エマルゲン104P、エマルゲン105、エマルゲン106、エマルゲン108、エマルゲン109P、エマルゲン120、エマルゲン123P、エマルゲン130K、エマルゲン147、エマルゲン150、エマルゲン210P、エマルゲン220、エマルゲン306P、エマルゲン320P、エマルゲン350、エマルゲン404、エマルゲン408、エマルゲン409PV、エマルゲン420、エマルゲン430、エマルゲン705、エマルゲン707、エマルゲン709、エマルゲン1108、エマルゲン1118S-70、エマルゲン1135S-70、エマルゲン1150S-60、エマルゲン4085、エマルゲン2020G-HA、エマルゲン2025G、エマノーン1112、エマノーン3199V、エマノーン3299V、エマノーン3299RV、エマノーン4110が挙げられる。より好ましくは、花王(株)のエマルゲン103、エマルゲン104P、エマルゲン105、エマルゲン106、エマルゲン108、エマルゲン109P、エマルゲン210P、エマルゲン306P、エマルゲン320P、エマルゲン404、エマルゲン408、エマルゲン409PV、エマルゲン420、エマルゲン705、エマルゲン707、エマルゲン709、エマルゲン1108、エマルゲン2020G-HA、エマノーン1112、エマノーン4110が挙げられる。さらに好ましくは、花王(株)のエマルゲン104P、エマルゲン105、エマルゲン106、エマルゲン108、エマルゲン210P、エマルゲン306P、エマルゲン408、エマルゲン409PV、エマルゲン705、エマルゲン707、エマルゲン709、エマルゲン1108、エマルゲン2020G-HA、エマノーン1112、エマノーン4110が挙げられる。これの他、日光ケミカルズ(株)のNIKKOL(登録商標)シリーズからも適宜選択し得る。例えば、NIKKOL BT-5、NIKKOL BT-7、NIKKOL BT-9、NIKKOL BT-12、NIKKOL BL-2、NIKKOL BL-4.2、NIKKOL BL-9EX等が挙げられ、最も好ましくは、NIKKOL BL-9EXが挙げられる。
Examples of the ethylene glycol alkyl ether include polyoxyethylene alkyl ether, polyoxyethylene lauryl ether, polyoxyethylene palmitoyl ether, and polyoxyethylene stearyl ether. Polyoxyethylene lauryl ether is preferable.
Also, commercially available ethylene glycol alkyl ethers can be used. Examples of such products include Emulgen 102KG, Emargen 103, and Emulgen 104P in Kao's Emulgen (registered trademark) series and Emanon (registered trademark) series. Emulgen 105, Emulgen 106, Emulgen 108, Emulgen 109P, Emulgen 120P, Emulgen 123P, Emulgen 130K, Emulgen 147, Emulgen 150, Emulgen 210P, Emulgen 220, Emulgen 306P, Emulgen 320P, Emulgen 350, Emulgen 404, Emulgen 408, Emulgen 409PV, Emulgen 420, Emulgen 430, Emulgen 705, Emulgen 707, Emulgen 709, Emulgen 1108, Emulgen 1118S-70, Emulgen 1135S-70, Emulgen 1150S-60, Emulgen 4085, Emulgen 2020G-HA, Emulgen 2025G, Emanon 1112, Emanor 3199V, Emanon 3299V, Emanon 3299RV, include the Emanon 4110. More preferably, Kao's Emulgen 103, Emulgen 104P, Emulgen 105, Emulgen 106, Emulgen 108, Emulgen 109P, Emulgen 210P, Emulgen 306P, Emulgen 320P, Emulgen 404, Emulgen 408, Emulgen 409PV, Emulgen 420, Emulgen 705 , Emulgen 707, Emulgen 709, Emulgen 1108, Emulgen 2020G-HA, Emanon 1112, Emanon 4110. More preferably, Kao's Emulgen 104P, Emulgen 105, Emulgen 106, Emulgen 108, Emulgen 210P, Emulgen 306P, Emulgen 408, Emulgen 409PV, Emulgen 705, Emulgen 707, Emulgen 709, Emulgen 1108, Emulgen 2020G-HA, Emanon 1112, Emanon 4110. In addition to this, it can be appropriately selected from the NIKKOL (registered trademark) series of Nikko Chemicals. For example, NIKKOL BT-5, NIKKOL BT-7, NIKKOL BT-9, NIKKOL BT-12, NIKKOL BL-2, NIKKOL BL-4.2, NIKKOL BL-9EX, etc., most preferably NIKOL BL-9EX 9EX.

 また本発明において使用する界面活性剤として、そのHLB(Hydrophile-Lipophile Balance)値が8乃至20であるものを好適に使用することができる。より好ましくは、HLB値が8乃至14である。 In addition, as the surfactant used in the present invention, those having an HLB (Hydrophile-Lipophile Balance) value of 8 to 20 can be suitably used. More preferably, the HLB value is 8 to 14.

 本発明において、界面活性剤の配合量は、得られるスティック状基材の総質量に対して、例えば0.1乃至20質量%、好ましくは、0.1乃至10質量%である。
 尚、界面活性剤として、エチレングリコールアルキルエーテルを用いる場合は、得られるスティック状基材の総質量に対して、例えば0.1乃至3質量%が好ましく、ベタイン系化合物を用いる場合は、得られるスティック状基材の総質量に対して、例えば0.5乃至10質量%が好ましい。
 なお本発明において用いられる界面活性剤は、上述の界面活性剤群の少なくとも一種であり、これら界面活性剤を一種単独で、或いは二種以上を組み合わせて用いることができる。
In the present invention, the compounding amount of the surfactant is, for example, 0.1 to 20% by mass, preferably 0.1 to 10% by mass with respect to the total mass of the stick-like substrate to be obtained.
In addition, when ethylene glycol alkyl ether is used as the surfactant, for example, 0.1 to 3% by mass is preferable with respect to the total mass of the obtained stick-like substrate, and when a betaine compound is used, it is obtained. For example, 0.5 to 10% by mass is preferable with respect to the total mass of the stick-shaped substrate.
The surfactant used in the present invention is at least one of the above-mentioned surfactant group, and these surfactants can be used alone or in combination of two or more.

[1,2-アルカンジオールまたは1,3-アルカンジオール]
 本発明のスティック状基材において使用する1,2-アルカンジオールまたは1,3-アルカンジオールは、前記脂質ペプチド型化合物の溶解性を促進させる働きをもつ。
 1,3-アルカンジオールが好ましい。
 前記1,2-アルカンジオールの具体例としては、1,2-ペンタンジオール、1,2-ヘキサンジオール、1,2-オクタンジオール及び1,2-デカンジオールなどが挙げられる。好ましくは、1,2-ペンタンジオール、1,2-ヘキサンジオール、1,2-オクタンジオールが挙げられる。さらに好ましくは、1,2-ペンタンジオール又は1,2-ヘキサンジオールである。本発明で使用する1,2-アルカンジオールは上述の1,2-アルカンジオール群の少なくとも一種である。
 前記1,3-アルカンジオールの具体例としては、1,3-プロパンジオール、2-メチル-1,3-プロパンジオール、1,3-ブタンジオール、3-メチル-1,3-ブタンジオール、1,3-ペンタンジオール、1,3-ヘキサンジオール、2-エチル-1,3-ヘキサンジオール、2-エチル-1,3-オクタンジオール及び1,3-デカンジオールなどが挙げられる。好ましくは、1,3-ペンタンジオール、1,3-ヘキサンジオール、2-エチル-1,3-ヘキサンジオール、2-エチル-1,3-オクタンジオールが挙げられる。さらに好ましくは、2-エチル-1,3-ヘキサンジオール、2-エチル-1,3-オクタンジオールである。本発明で使用する1,3-アルカンジオールは上述の1,3-アルカンジオール群の少なくとも一種である。
 1,3-アルカンジオールとして、例えば、1,3-ブタンジオールが好ましい。
 これら1,2-アルカンジオールまたは1,3-アルカンジオールを一種単独で、或いは二種以上を組み合わせて用いることができる。
[1,2-alkanediol or 1,3-alkanediol]
The 1,2-alkanediol or 1,3-alkanediol used in the stick-like substrate of the present invention has a function of promoting the solubility of the lipid peptide type compound.
1,3-alkanediol is preferred.
Specific examples of the 1,2-alkanediol include 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol, and the like. Preferred are 1,2-pentanediol, 1,2-hexanediol, and 1,2-octanediol. More preferred is 1,2-pentanediol or 1,2-hexanediol. The 1,2-alkanediol used in the present invention is at least one of the aforementioned 1,2-alkanediol group.
Specific examples of the 1,3-alkanediol include 1,3-propanediol, 2-methyl-1,3-propanediol, 1,3-butanediol, 3-methyl-1,3-butanediol, , 3-pentanediol, 1,3-hexanediol, 2-ethyl-1,3-hexanediol, 2-ethyl-1,3-octanediol, 1,3-decanediol, and the like. Preferred are 1,3-pentanediol, 1,3-hexanediol, 2-ethyl-1,3-hexanediol, and 2-ethyl-1,3-octanediol. More preferred are 2-ethyl-1,3-hexanediol and 2-ethyl-1,3-octanediol. The 1,3-alkanediol used in the present invention is at least one of the aforementioned 1,3-alkanediol group.
As the 1,3-alkanediol, for example, 1,3-butanediol is preferable.
These 1,2-alkanediols or 1,3-alkanediols can be used alone or in combination of two or more.

 本発明において、1,2-アルカンジオール又はまたは1,3-アルカンジオールの配合量は、得られるスティック状基材の総質量に対して、例えば0.5乃至20質量%、好ましくは、1乃至10質量%、より好ましくは2乃至8質量%である。 In the present invention, the blending amount of 1,2-alkanediol or 1,3-alkanediol is, for example, 0.5 to 20% by mass, preferably 1 to 1% by mass with respect to the total mass of the obtained stick-like substrate. It is 10% by mass, more preferably 2 to 8% by mass.

[炭素原子数8乃至30の少なくとも一種の飽和又は不飽和の一価アルコール]
 本発明のスティック状基材には、炭素原子数8乃至30の少なくとも一種の飽和又は不飽和の一価アルコールを配合することにより、基材の安定性の向上、具体的には基材表面の“汗かき”と称される離油現象を抑制できる。なお本明細書において、炭素原子数8乃至30の少なくとも一種の飽和又は不飽和の一価アルコールを単に「高級アルコール」とも称する。
 これら高級アルコールは、誘導体を含め多くの原料が市販されたり合成されたりしているが、本発明のスティック状基材中には、好ましくはアルキル基の炭素原子数が8乃至30である少なくとも一種の飽和又は不飽和の一価アルコールが使用され得、より好ましくは12乃至22である飽和の一価アルコールが用いられ得、中でも、ミリスチルアルコール(炭素原子数14)、セタノール(炭素原子数16)、ステアリルアルコール(炭素原子数18)、ベヘニルアルコール(炭素原子数22)が特に汎用性が高く、また前述の“汗かき”の抑制効果が高い観点から好適である。
 本発明において、高級アルコールの配合量は、得られるスティック状基材の総質量に対して、例えば0.001乃至1質量%、好ましくは、0.01乃至0.5質量%、より好ましくは0.03乃至0.3質量%である。
 なお本発明において用いられる上記高級アルコールは上述の高級アルコール群の少なくとも一種であり、これらを一種単独で、或いは二種以上を組み合わせて用いることができる。
[At least one saturated or unsaturated monohydric alcohol having 8 to 30 carbon atoms]
By adding at least one saturated or unsaturated monohydric alcohol having 8 to 30 carbon atoms to the stick-shaped substrate of the present invention, the stability of the substrate is improved, specifically the surface of the substrate. The oil release phenomenon called “sweat” can be suppressed. In the present specification, at least one saturated or unsaturated monohydric alcohol having 8 to 30 carbon atoms is also simply referred to as “higher alcohol”.
These higher alcohols are commercially available or synthesized many raw materials including derivatives, but in the stick-like base material of the present invention, preferably at least one kind of alkyl group having 8 to 30 carbon atoms. Saturated or unsaturated monohydric alcohols can be used, more preferably 12 to 22 saturated monohydric alcohols, among which myristyl alcohol (14 carbon atoms), cetanol (16 carbon atoms). Stearyl alcohol (18 carbon atoms) and behenyl alcohol (22 carbon atoms) are particularly preferred because of their high versatility and high “sweat” -suppressing effect.
In the present invention, the compounding amount of the higher alcohol is, for example, 0.001 to 1% by mass, preferably 0.01 to 0.5% by mass, and more preferably 0% with respect to the total mass of the stick-like substrate to be obtained. 0.03 to 0.3% by mass.
In addition, the said higher alcohol used in this invention is at least 1 type of the above-mentioned higher alcohol group, These can be used individually by 1 type or in combination of 2 or more types.

[増粘剤]
 本発明のスティック状基材において使用する増粘剤としては、アルギン酸誘導体及びカラギーナンが挙げられる。
 本発明のスティック状基材において使用するアルギン酸誘導体としては、アルギン酸、アルギン酸の塩(ナトリウム塩、カリウム塩、カルシウム塩等)、アルギン酸エステル等が挙げられるが、アルギン酸エステルが好ましく、特に、アルギン酸多価アルコールエステルが好ましい。
 アルギン酸多価アルコールエステルとしては、アルギン酸エチレングリコール、アルギン酸プロピレングリコール等が挙げられるが、アルギン酸プロピレングリコールが好ましい。
 本発明において、使用される増粘剤の配合量は、得られるスティック状基材の総質量に対して、例えば0.3乃至1.0質量%、好ましくは0.3乃至0.7質量%である。
 なお本発明において用いられる増粘剤は、上記から選択される増粘剤の少なくとも1種であり、これら増粘剤を一種単独で、或いは二種以上を組み合わせて用いることができる。
[Thickener]
Examples of the thickener used in the stick-shaped substrate of the present invention include alginic acid derivatives and carrageenan.
Examples of the alginic acid derivative used in the stick-shaped substrate of the present invention include alginic acid, alginic acid salts (sodium salt, potassium salt, calcium salt, etc.), alginic acid ester, and the like. Alcohol esters are preferred.
Examples of the alginic acid polyhydric alcohol ester include ethylene glycol alginate and propylene glycol alginate, and propylene glycol alginate is preferable.
In the present invention, the blending amount of the thickener used is, for example, 0.3 to 1.0% by mass, preferably 0.3 to 0.7% by mass, based on the total mass of the stick-like substrate to be obtained. It is.
In addition, the thickener used in this invention is at least 1 sort (s) of the thickener selected from the above, These thickeners can be used individually by 1 type or in combination of 2 or more types.

 本発明のスティック状基材は、上記の成分及び水に加えて、脂肪酸、油性基剤、顔料、有機酸、多価アルコール並びにその他添加剤も含み得る。
 各成分につき以下に説明する。
In addition to the above components and water, the stick-like substrate of the present invention can also contain fatty acids, oily bases, pigments, organic acids, polyhydric alcohols, and other additives.
Each component will be described below.

[脂肪酸]
 本発明のスティック状基材において使用し得る脂肪酸としては、好ましくは炭素原子数10乃至20の飽和脂肪酸及び不飽和脂肪酸並びにそれら脂肪酸の塩からなる群から選択される少なくとも1種であり、例えば脂肪酸としてはカプリン酸、ウンデカン酸、ラウリン酸、トリデカン酸、ミリスチン酸、ペンタデカン酸、パルミチン酸、マルガリン酸、ステアリン酸が挙げられる。さらに好ましくは、カプリン酸、ラウリン酸、ミリスチン酸、パルミチン酸、ステアリン酸が挙げられ、なかでもステアリン酸が好ましい。
 本発明において、脂肪酸を使用する場合の配合量は、得られるスティック状基材の総質量に対して、例えば0.1乃至2.0質量%、好ましくは0.2乃至1.0質量%である。
 なお本発明において使用し得る脂肪酸は、上記脂肪酸群から選択される少なくとも1種であり、これら脂肪酸を一種単独で、或いは二種以上を組み合わせて用いることができる。
[fatty acid]
The fatty acid that can be used in the stick-shaped substrate of the present invention is preferably at least one selected from the group consisting of saturated fatty acids having 10 to 20 carbon atoms and unsaturated fatty acids and salts of these fatty acids. Examples include capric acid, undecanoic acid, lauric acid, tridecanoic acid, myristic acid, pentadecanoic acid, palmitic acid, margaric acid, and stearic acid. More preferably, capric acid, lauric acid, myristic acid, palmitic acid, and stearic acid are mentioned, and stearic acid is particularly preferable.
In the present invention, the amount of the fatty acid used is, for example, 0.1 to 2.0% by mass, preferably 0.2 to 1.0% by mass, based on the total mass of the stick-like substrate to be obtained. is there.
In addition, the fatty acid which can be used in this invention is at least 1 sort (s) selected from the said fatty acid group, These fatty acids can be used individually by 1 type or in combination of 2 or more types.

[油性基剤]
 本発明のスティック状基材において使用し得る油性基剤としては特に限定されず、例えば以下の油性基剤を挙げることができる:オレイルアルコール、ホホバアルコール、キミルアルコール、セラキルアルコール、バチルアルコール、ヘキシルデカノール、イソステアリルアルコール、2-オクチルドデカノール、ダイマージオール等の高級(多価)アルコール類;ベンジルアルコール等のアラルキルアルコール及びその誘導体;イソステアリン酸、ベヘン酸、ウンデシレン酸、12-ヒドロキシステアリン酸、パルミトオレイン酸、オレイン酸、リノール酸、リノレイン酸、エルカ酸、ドコサヘキサエン酸、エイコサペンタエン酸、イソヘキサデカン酸、アンテイソヘンイコサン酸、長鎖分岐脂肪酸、ダイマー酸、水素添加ダイマー酸等;流動パラフィン(ミネラルオイル)、重質流動イソパラフィン、軽質流動イソパラフィン、α-オレフィンオリゴマー、ポリイソブテン、水添ポリイソブテン、ポリブテン、スクワラン、オリーブ由来スクワラン、スクワレン、ワセリン、固形パラフィン等の炭化水素類;キャンデリラワックス、カルナウバワックス、ライスワックス、木ろう、みつろう、モンタンワックス、オゾケライト、セレシン、パラフィンワックス、マイクロクリスタリンワックス、ペトロラタム、フィッシャートロプシュワックス、ポリエチレンワックス、エチレン・プロピレンコポリマー等のワックス類;ヤシ油、パーム油、パーム核油、サフラワー油、オリーブ油、ヒマシ油、アボカド油、ゴマ油、茶油、月見草油、小麦胚芽油、マカデミアナッツ油、ヘーゼルナッツ油、ククイナッツ油、ローズヒップ油、メドウフォーム油、パーシック油、ティートリー油、ハッカ油、トウモロコシ油、ナタネ油、ヒマワリ油、小麦胚芽油、アマニ油、綿実油、大豆油、落花生油、コメヌカ油、カカオ脂、シア脂、水素添加ヤシ油、水素添加ヒマシ油、ホホバ油、水素添加ホホバ油、グレープシード油、アプリコット油(杏仁油)、ツバキ油等の植物油脂類;牛脂、乳脂、馬脂、卵黄油、ミンク油、タートル油等の動物性油脂類;鯨ロウ、ラノリン、オレンジラッフィー油等の動物性ロウ類;液状ラノリン、還元ラノリン、吸着精製ラノリン、酢酸ラノリン、酢酸液状ラノリン、ヒドロキシラノリン、ポリオキシエチレンラノリン、ラノリン脂肪酸、硬質ラノリン脂肪酸、ラノリンアルコール、酢酸ラノリンアルコール、酢酸(セチル・ラノリル)エステル等のラノリン類;コレステロール、ジヒドロコレステロール、ラノステロール、ジヒドロラノステロール、フィトステロール、コール酸等のステロール類;サポゲニン類;サポニン類;酢酸コレステリル、ノナン酸コレステリル、ステアリン酸コレステリル、イソステアリン酸コレステリル、オレイン酸コレステリル、N-ラウロイル-L-グルタミン酸ジ(コレステリル/ベヘニル/オクチルドデシル)、N-ラウロイル-L-グルタミン酸ジ(コレステリル/オクチルドデシル)、N-ラウロイル-L-グルタミン酸ジ(フィトステリル/ベヘニル/オクチルドデシル)、N-ラウロイル-L-グルタミン酸ジ(フィトステリル/オクチルドデシル)、N-ラウロイルサルコシンイソプロピル等のアシルサルコシンアルキルエステル、12-ヒドロキシステアリン酸コレステリル、マカデミアナッツ油脂肪酸コレステリル、マカデミアナッツ油脂肪酸フィトステリル、イソステアリン酸フィトステリル、軟質ラノリン脂肪酸コレステリル、硬質ラノリン脂肪酸コレステリル、長鎖分岐脂肪酸コレステリル、長鎖α-ヒドロキシ脂肪酸コレステリル等のステロールエステル類;リン脂質・コレステロール複合体、リン脂質・フィトステロール複合体等の脂質複合体;ミリスチン酸オクチルドデシル、ミリスチン酸ヘキシルデシル、イソステアリン酸オクチルドデシル、パルミチン酸セチル、パルミチン酸オクチルドデシル、オクタン酸セチル、オクタン酸ヘキシルデシル、イソノナン酸イソトリデシル、イソノナン酸イソノニル、イソノナン酸オクチル、イソノナン酸イソトリデシル、ネオペンタン酸イソデシル、ネオペンタン酸イソトリデシル、ネオペンタン酸イソステアリル、ネオデカン酸オクチルドデシル、オレイン酸オレイル、オレイン酸オクチルドデシル、リシノレイン酸オクチルドデシル、ラノリン脂肪酸オクチルドデシル、ジメチルオクタン酸ヘキシルデシル、エルカ酸オクチルドデシル、イソステアリン酸硬化ヒマシ油、オレイン酸エチル、アボカド油脂肪酸エチル、ミリスチン酸イソプロピル、パルミチン酸イソプロピル、パルミチン酸オクチル、イソステアリン酸イソプロピル、ラノリン脂肪酸イソプロピル、セバチン酸ジエチル、セバチン酸ジイソプロピル、セバチン酸ジオクチル、アジピン酸ジイソプロピル、セバチン酸ジブチルオクチル、アジピン酸ジイソブチル、コハク酸ジオクチル、クエン酸トリエチル等のモノアルコールカルボン酸エステル類;乳酸セチル、リンゴ酸ジイソステアリル、モノイソステアリン酸水添ヒマシ油等のオキシ酸エステル類;トリオクタン酸グリセリル(トリ2-エチルヘキサン酸グリセリル)、トリオレイン酸グリセリル、トリイソステアリン酸グリセリル、ジイソステアリン酸グリセリル、トリ(カプリル酸/カプリン酸)グリセリル、トリ(カプリル酸/カプリン酸/ミリスチン酸/ステアリン酸)グリセリル、水添ロジントリグリセリド(水素添加エステルガム)、ロジントリグリセリド(エステルガム)、ベヘン酸エイコサン二酸グリセリル、トリオクタン酸トリメチロールプロパン、トリイソステアリン酸トリメチロールプロパン、ジオクタン酸ネオペンチルグリコール、ジカプリン酸ネオペンチルグリコール、ジオクタン酸2-ブチル-2-エチル-1,3-プロパンジオール、ジオレイン酸プロピレングリコール、テトラオクタン酸ペンタエリスリチル、水素添加ロジンペンタエリスリチル、トリエチルヘキサン酸ジトリメチロールプロパン、(イソステアリン酸/セバシン酸)ジトリメチロールプロパン、トリエチルヘキサン酸ペンタエリスリチル、(ヒドロキシステアリン酸/ステアリン酸/ロジン酸)ジペンタエリスリチル、ジイソステアリン酸ジグリセリル、テトライソステアリン酸ポリグリセリル、ノナイソステアリン酸ポリグリセリル-10、デカ(エルカ酸/イソステアリン酸/リシノレイン酸)ポリグリセリル-8、(ヘキシルデカン酸/セバシン酸)ジグリセリルオリゴエステル、ジステアリン酸グリコール(ジステアリン酸エチレングリコール)、ジネオペンタン酸3-メチル-1,5-ペンタンジオール、ジネオペンタン酸2,4-ジエチル-1,5-ペンタンジオール等の多価アルコール脂肪酸エステル類;ダイマージリノール酸ジイソプロピル、ダイマージリノール酸ジイソステアリル、ダイマージリノール酸ジ(イソステアリル/フィトステリル)、ダイマージリノール酸(フィトステリル/ベヘニル)、ダイマージリノール酸(フィトステリル/イソステアリル/セチル/ステアリル/ベヘニル)、ダイマージリノール酸ダイマージリノレイル、ジイソステアリン酸ダイマージリノレイル、ダイマージリノレイル水添ロジン縮合物、ダイマージリノール酸硬化ヒマシ油、ヒドロキシアルキルダイマージリノレイルエーテル等のダイマー酸若しくはダイマージオールの誘導体;ヤシ油脂肪酸モノエタノールアミド(コカミドMEA)、ヤシ油脂肪酸ジエタノールアミド(コカミドDEA)、ラウリン酸モノエタノールアミド(ラウラミドMEA)、ラウリン酸ジエタノールアミド(ラウラミドDEA)、ラウリン酸モノイソプロパノールアミド(ラウラミドMIPA)、パルミチン酸モノエタノールアミド(パルタミドMEA)、パルミチン酸ジエタノールアミド(パルタミドDEA)、ヤシ油脂肪酸メチルエタノールアミド(コカミドメチルMEA)等の脂肪酸アルカノールアミド類;ジメチコン(ジメチルポリシロキサン)、高重合ジメチコン(高重合ジメチルポリシロキサン)、シクロメチコン(環状ジメチルシロキサン、デカメチルシクロペンタシロキサン(単にシクロペンタシロキサンとも))、フェニルトリメチコン、ジフェニルジメチコン、フェニルジメチコン、ステアロキシプロピルジメチルアミン、(アミノエチルアミノプロピルメチコン/ジメチコン)コポリマー、ジメチコノール、ジメチコノールクロスポリマー、シリコーン樹脂、シリコーンゴム、アミノプロピルジメチコン及びアモジメチコン等のアミノ変性シリコーン、カチオン変性シリコーン、ジメチコンコポリオール等のポリエーテル変性シリコーン、ポリグリセリン変性シリコーン、糖変性シリコーン、カルボン酸変性シリコーン、リン酸変性シリコーン、硫酸変性シリコーン、アルキル変性シリコーン、脂肪酸変性シリコーン、アルキルエーテル変性シリコーン、アミノ酸変性シリコーン、ペプチド変性シリコーン、フッ素変性シリコーン、カチオン変性及びポリエーテル変性シリコーン、アミノ変性及びポリエーテル変性シリコーン、アルキル変性及びポリエーテル変性シリコーン、ポリシロキサン・オキシアルキレン共重合体等のシリコーン類;パーフルオロデカン、パーフルオロオクタン、パーフルオロポリエーテル等のフッ素系油剤類が、好ましいものとして挙げられる。
[Oil base]
The oily base that can be used in the stick-like substrate of the present invention is not particularly limited, and examples thereof include the following oily bases: oleyl alcohol, jojoba alcohol, chimyl alcohol, seraalkyl alcohol, batyl alcohol, Higher (polyhydric) alcohols such as hexyldecanol, isostearyl alcohol, 2-octyldodecanol, dimer diol; aralkyl alcohols such as benzyl alcohol and derivatives thereof; isostearic acid, behenic acid, undecylenic acid, 12-hydroxystearic acid, palmi Tooleic acid, oleic acid, linoleic acid, linolenic acid, erucic acid, docosahexaenoic acid, eicosapentaenoic acid, isohexadecanoic acid, antiisohenicosanoic acid, long-chain branched fatty acid, dimer acid, hydrogenated dimer acid, etc .; Hydrocarbons such as animal paraffin (mineral oil), heavy liquid isoparaffin, light liquid isoparaffin, α-olefin oligomer, polyisobutene, hydrogenated polyisobutene, polybutene, squalane, olive-derived squalane, squalene, petrolatum, solid paraffin; candelilla wax , Carnauba wax, rice wax, wax, beeswax, montan wax, ozokerite, ceresin, paraffin wax, microcrystalline wax, petrolatum, Fischer-Tropsch wax, polyethylene wax, ethylene / propylene copolymer, etc .; palm oil, palm oil , Palm kernel oil, safflower oil, olive oil, castor oil, avocado oil, sesame oil, tea oil, evening primrose oil, wheat germ oil, macadamia nut oil, hazel Nut oil, cucumber oil, rosehip oil, meadow foam oil, persic oil, tea tree oil, mint oil, corn oil, rapeseed oil, sunflower oil, wheat germ oil, linseed oil, cottonseed oil, soybean oil, peanut oil, rice bran oil, Vegetable oils such as cacao butter, shea butter, hydrogenated coconut oil, hydrogenated castor oil, jojoba oil, hydrogenated jojoba oil, grape seed oil, apricot oil (apricot oil), camellia oil; beef fat, milk fat, horse fat, Animal fats and oils such as egg yolk oil, mink oil and turtle oil; animal waxes such as whale wax, lanolin and orange luffy oil; liquid lanolin, reduced lanolin, adsorbed purified lanolin, lanolin acetate, lanolin acetate, hydroxy lanolin , Polyoxyethylene lanolin, lanolin fatty acid, hard lanolin fatty acid, lanolin alcohol, lanolin acetate And lanolins such as acetic acid (cetyl lanolyl) ester; sterols such as cholesterol, dihydrocholesterol, lanosterol, dihydrolanosterol, phytosterol, cholic acid; sapogenins; saponins; cholesteryl acetate, cholesteryl nonate, cholesteryl stearate, Cholesteryl isostearate, cholesteryl oleate, N-lauroyl-L-glutamate di (cholesteryl / behenyl / octyldodecyl), N-lauroyl-L-glutamate di (cholesteryl / octyldodecyl), N-lauroyl-L-glutamate di (phytosteryl) / Behenyl / octyldodecyl), N-lauroyl-L-glutamate di (phytosteryl / octyldodecyl), N-lauroyl sarcosine isopropyl, etc. Acyl sarcosine alkyl ester, cholesteryl 12-hydroxystearate, macadamia nut oil fatty acid cholesteryl, macadamia nut oil fatty acid phytosteryl, phytosteryl isostearate, soft lanolin fatty acid cholesteryl, hard lanolin fatty acid cholesteryl, long chain branched fatty acid cholesteryl, long chain α-hydroxy fatty acid cholesteryl, etc. Sterol esters of phospholipid / cholesterol complex, phospholipid / phytosterol complex, etc .; octyldodecyl myristate, hexyldecyl myristate, octyldodecyl isostearate, cetyl palmitate, octyldodecyl palmitate, octanoic acid Cetyl, hexyldecyl octoate, isotridecyl isononanoate, isononyl isononanoate, isononona Octyl acid, isotridecyl isononanoate, isodecyl neopentanoate, isotridecyl neopentanoate, isostearyl neopentanoate, octyldodecyl neodecanoate, oleyl oleate, octyldodecyl oleate, octyldodecyl ricinoleate, lanolin fatty acid octyldodecyl, hexyldecyl dimethyloctanoate, Octyldodecyl erucate, isostearic acid hydrogenated castor oil, ethyl oleate, avocado oil fatty acid ethyl, isopropyl myristate, isopropyl palmitate, octyl palmitate, isopropyl isostearate, lanolin fatty acid isopropyl, diethyl sebacate, diisopropyl sebacate, sebacic acid Dioctyl, diisopropyl adipate, dibutyloctyl sebacate, adipic acid Monoalcohol carboxylates such as isobutyl, dioctyl succinate, triethyl citrate; oxyesters such as cetyl lactate, diisostearyl malate, hydrogenated castor oil monoisostearate; glyceryl trioctanoate (tri-2-ethylhexane) Glyceryl acid), glyceryl trioleate, glyceryl triisostearate, glyceryl diisostearate, glyceryl tri (caprylic acid / capric acid), tri (caprylic acid / capric acid / myristic acid / stearic acid) glyceryl, hydrogenated rosin triglyceride (hydrogen Ester gum added), rosin triglyceride (ester gum), glyceryl behenate, trimethylolpropane trioctanoate, trimethylolpropane triisostearate, dioctanoic acid Opentyl glycol, neopentyl glycol dicaprate, 2-butyl-2-ethyl-1,3-propanediol dioctanoate, propylene glycol dioleate, pentaerythrityl tetraoctanoate, hydrogenated rosin pentaerythrityl, ditritrihexanoate Methylolpropane, (isostearic acid / sebacic acid) ditrimethylolpropane, pentaerythrityl triethylhexanoate, (hydroxystearic acid / stearic acid / rosinic acid) dipentaerythrityl, diglyceryl diisostearate, polyglyceryl tetraisostearate, polyglyceryl nonaisostearate-10 , Deca (erucic acid / isostearic acid / ricinoleic acid) polyglyceryl-8, (hexyldecanoic acid / sebacic acid) diglyceryl Polyhydric alcohol fatty acid esters such as ligoester, glycol distearate (ethylene glycol distearate), dineopentanoic acid 3-methyl-1,5-pentanediol, dineopentanoic acid 2,4-diethyl-1,5-pentanediol; Diisopropyl linoleate, diisostearyl dimerinolinoleate, dimerinolinoleate di (isostearyl / phytosteryl), dimerlinoleic acid (phytosteryl / behenyl), dimerlinoleic acid (phytosteryl / isostearyl / cetyl / stearyl / behenyl) , Dimer dilinoleic acid dimer dilinoleyl, diisostearic acid dimer dilinoleyl, dimer dilinoleyl hydrogenated rosin condensate, dimer dilinoleic acid hydrogenated castor oil, hydroxyalkyl Dimer acid or dimer diol derivative such as imazyl linoleyl ether; coconut oil fatty acid monoethanolamide (cocamide MEA), coconut oil fatty acid diethanolamide (cocamide DEA), lauric acid monoethanolamide (lauramide MEA), lauric acid diethanolamide ( Fatty acid alkanolamides such as lauramide DEA), lauric acid monoisopropanolamide (lauramide MIPA), palmitic acid monoethanolamide (partamide MEA), palmitic acid diethanolamide (partamide DEA), coconut oil fatty acid methylethanolamide (cocamidomethyl MEA); Dimethicone (dimethylpolysiloxane), highly polymerized dimethicone (highly polymerized dimethylpolysiloxane), cyclomethicone (cyclic dimethylsiloxane, deca Methylcyclopentasiloxane (also simply cyclopentasiloxane), phenyltrimethicone, diphenyldimethicone, phenyldimethicone, stearoxypropyldimethylamine, (aminoethylaminopropylmethicone / dimethicone) copolymer, dimethiconol, dimethiconol crosspolymer, silicone resin, silicone Amino-modified silicone such as rubber, aminopropyl dimethicone and amodimethicone, polyether-modified silicone such as cation-modified silicone and dimethicone copolyol, polyglycerin-modified silicone, sugar-modified silicone, carboxylic acid-modified silicone, phosphoric acid-modified silicone, sulfuric acid-modified silicone , Alkyl modified silicone, fatty acid modified silicone, alkyl ether modified silicone, amino acid modified silicone , Silicones such as peptide-modified silicone, fluorine-modified silicone, cation-modified and polyether-modified silicone, amino-modified and polyether-modified silicone, alkyl-modified and polyether-modified silicone, polysiloxane-oxyalkylene copolymer; perfluorodecane, Fluorine-based oils such as perfluorooctane and perfluoropolyether are preferred.

 本発明において、油性基剤を使用する場合の配合量は、得られるスティック状基材の総質量に対して、例えば1乃至50質量%、好ましくは、5乃至50質量%、より好ましくは5乃至20質量%、特に好ましくは10乃至20質量%である。
 なお本発明において用いられ得る上記油性基剤は上述の油性基剤群の少なくとも一種であり、これら油性基剤を一種単独で、或いは二種以上を組み合わせて用いてもよい。
In the present invention, the blending amount when the oily base is used is, for example, 1 to 50% by mass, preferably 5 to 50% by mass, more preferably 5 to 5% by mass with respect to the total mass of the stick-like substrate to be obtained. It is 20% by mass, particularly preferably 10 to 20% by mass.
The oily base that can be used in the present invention is at least one of the above-mentioned oily base group, and these oily bases may be used alone or in combination of two or more.

[顔料]
 本発明のスティック状基材には、さらに顔料を含み得る。配合され得る顔料としては特に限定されるものではないが、例えば、二酸化チタン、酸化亜鉛等の無機白色顔料;赤酸化鉄(ベンガラ)、チタン酸鉄等の無機赤色系顔料;γ-酸化鉄等の無機褐色系顔料;黄酸化鉄、黄土等の無機黄色系顔料;黒酸化鉄、低次酸化チタン等の無機黒色系顔料;マンゴバイオレット、コバルトバイオレット等の無機紫色系顔料;酸化クロム、水酸化クロム、チタン酸コバルト等の無機緑色系顔料;群青、紺青等の無機青色系顔料;酸化チタンコーテッドマイカ、酸化チタンコーテッドオキシ塩化ビスマス、酸化チタンコーテッドタルク、着色酸化チタンコーテッドマイカ、オキシ塩化ビスマス、魚鱗箔等のパール顔料;タルク、セリサイト、マイカ、カオリン、炭酸カルシウム、炭酸マグネシウム、無水ケイ酸、硫酸バリウム、水酸化アルミニウム等の体質顔料;アルミニウムパウダー、カッパーパウダー、金等の金属粉末顔料;表面処理無機及び金属粉末顔料;ジルコニウム、バリウム又はアルミニウムレーキ等の有機顔料;表面処理有機顔料等が挙げられる。
 本発明において、顔料を配合する場合、その配合量は、得られるスティック状基材の総質量に対して、例えば1乃至50質量%、好ましくは、5乃至50質量%、より好ましくは6乃至20質量%、特に好ましくは10乃至20質量%である。
 なお本発明において用いられる上記顔料は、上述の顔料群の少なくとも一種であり、これら顔料を一種単独で、或いは二種以上を組み合わせて用いられ得る。
[Pigment]
The stick-like substrate of the present invention may further contain a pigment. The pigment that can be blended is not particularly limited. For example, inorganic white pigments such as titanium dioxide and zinc oxide; inorganic red pigments such as red iron oxide (bengala) and iron titanate; γ-iron oxide and the like Inorganic yellow pigments such as yellow iron oxide and loess; inorganic black pigments such as black iron oxide and low-order titanium oxide; inorganic purple pigments such as mango violet and cobalt violet; chromium oxide and hydroxide Inorganic green pigments such as chromium and cobalt titanate; inorganic blue pigments such as ultramarine and bitumen; titanium oxide coated mica, titanium oxide coated bismuth oxychloride, titanium oxide coated talc, colored titanium oxide coated mica, bismuth oxychloride, fish scale Pearl pigments such as foil; talc, sericite, mica, kaolin, calcium carbonate, magnesium carbonate, silicic anhydride Body pigments such as barium sulfate and aluminum hydroxide; metal powder pigments such as aluminum powder, copper powder and gold; surface-treated inorganic and metal powder pigments; organic pigments such as zirconium, barium and aluminum lakes; surface-treated organic pigments and the like It is done.
In the present invention, when a pigment is blended, the blending amount is, for example, 1 to 50% by mass, preferably 5 to 50% by mass, and more preferably 6 to 20%, based on the total mass of the stick-like substrate to be obtained. % By mass, particularly preferably 10 to 20% by mass.
In addition, the said pigment used in this invention is at least 1 type of the above-mentioned pigment group, These pigments can be used individually by 1 type or in combination of 2 or more types.

[有機酸]
 本発明のスティック状基材はさらに有機酸を含み得る。
 上記有機酸としては、アスコルビン酸、クエン酸、乳酸、グリコール酸、コハク酸、酢酸、リンゴ酸、酒石酸、フマル酸等が挙げられる。中でも好ましくはアスコルビン酸、クエン酸、乳酸が挙げられ、特にアスコルビン酸、クエン酸が挙げられる。
 本発明において、有機酸を使用する場合の配合量は、得られるスティック状基材の総質量に対して、例えば1乃至20質量%、好ましくは、1乃至10質量%である。
[Organic acid]
The stick-like substrate of the present invention may further contain an organic acid.
Examples of the organic acid include ascorbic acid, citric acid, lactic acid, glycolic acid, succinic acid, acetic acid, malic acid, tartaric acid, and fumaric acid. Among them, ascorbic acid, citric acid, and lactic acid are preferable, and ascorbic acid and citric acid are particularly preferable.
In this invention, the compounding quantity in the case of using an organic acid is 1-20 mass% with respect to the total mass of the stick-shaped base material obtained, Preferably it is 1-10 mass%.

[多価アルコール]
 本発明のスティック状基材は、さらに多価アルコールを含み得る。前記多価アルコールは、先に挙げた1,2-アルカンジオール又は1,3-アルカンジオールとは異なる多価アルコールであり、その具体例としてはグリセリン、プロピレングリコール及びポリエチレングリコール等が挙げられる。多価アルコールを含むことにより、スティック状基材の経時安定性を向上させることができる。なお上記ポリエチレングリコールとしては、例えば平均分子量1,000乃至4,000のものを好適に使用できる。
 本発明において、多価アルコールを使用する場合の配合量は、得られるスティック状基材の総質量に対して、例えば1乃至80質量%、好ましくは、1乃至60質量%とすることができる。
[Polyhydric alcohol]
The stick-like substrate of the present invention may further contain a polyhydric alcohol. The polyhydric alcohol is a polyhydric alcohol different from the 1,2-alkanediol or 1,3-alkanediol listed above, and specific examples thereof include glycerin, propylene glycol, and polyethylene glycol. By including the polyhydric alcohol, the temporal stability of the stick-like substrate can be improved. For example, polyethylene glycol having an average molecular weight of 1,000 to 4,000 can be preferably used.
In the present invention, when polyhydric alcohol is used, the blending amount can be, for example, 1 to 80% by mass, preferably 1 to 60% by mass, based on the total mass of the stick-like substrate to be obtained.

[その他添加剤]
 本発明のスティック状基材には、必要に応じて一般的に化粧品用添加剤や、医薬部外品用添加剤及び医薬用添加剤として使用可能な添加剤を配合することができる。化粧品、医薬部外品又は医薬等の皮膚外用剤に配合される生理活性物質及び機能性物質等の添加成分としては、例えば保湿剤、感触向上剤、上記以外の界面活性剤、溶剤、酸化防止剤、還元剤、酸化剤、防腐剤、抗菌剤、殺菌剤、キレート剤、pH調整剤、酸、アルカリ、粉体、無機塩、紫外線吸収剤、美白剤、ビタミン類及びその誘導体類、育毛用薬剤、血行促進剤、刺激剤、ホルモン類、抗しわ剤、抗老化剤、ひきしめ剤、冷感剤、温感剤、創傷治癒促進剤、刺激緩和剤、鎮痛剤、細胞賦活剤、植物・動物・微生物エキス、鎮痒剤、角質剥離・溶解剤、制汗剤、清涼剤、収れん剤、酵素、核酸、香料、色素、着色剤、染料、消炎剤、抗炎症剤、抗喘息、抗慢性閉塞性肺疾患、抗アレルギー、免疫調整剤、抗感染症剤及び抗真菌剤等が挙げられる。
 これらその他添加剤の配合量は、その種類によって種々変化し得るが、得られるスティック状基材の総質量に対して、例えば0.1乃至20質量%、あるいは0.5乃至10質量%程度とすることができる。
[Other additives]
The stick-like substrate of the present invention can be blended with additives that can generally be used as cosmetic additives, quasi-drug additives, and pharmaceutical additives as necessary. Examples of additive components such as physiologically active substances and functional substances that are blended in cosmetics, quasi-drugs, or pharmaceutical external preparations for skin include moisturizers, feel-improving agents, surfactants other than the above, solvents, and antioxidants. Agent, reducing agent, oxidizing agent, preservative, antibacterial agent, bactericidal agent, chelating agent, pH adjuster, acid, alkali, powder, inorganic salt, UV absorber, whitening agent, vitamins and derivatives thereof, for hair growth Drug, Blood circulation promoter, Stimulant, Hormones, Anti-wrinkle agent, Anti-aging agent, Tightening agent, Cool sensation agent, Warm sensation agent, Wound healing promoter, Stimulation mitigation agent, Analgesic agent, Cell activator, Plant / Animal・ Microbial extract, antipruritic agent, exfoliating / dissolving agent, antiperspirant, refreshing agent, astringent, enzyme, nucleic acid, fragrance, pigment, colorant, dye, anti-inflammatory agent, anti-inflammatory agent, anti-asthma, anti-chronic obstructive Examples include pulmonary diseases, antiallergies, immune regulators, antiinfectives and antifungals It is.
The blending amount of these other additives may vary depending on the type of the additive, but is, for example, about 0.1 to 20% by mass, or about 0.5 to 10% by mass with respect to the total mass of the obtained stick-shaped substrate. can do.

 保湿剤・感触向上剤としては、グリセリン、トリメチロールプロパン、ペンタエリスリトール、ヘキシレングリコール、ジグリセリン、ポリグリセリン、ジエチレングリコール、ジプロピレングリコール、ポリプロピレングリコール、エチレングリコール・プロピレングリコール共重合体等のポリオール類及びその重合体;ジエチレングリコールモノエチルエーテル(エトキシジグリコール)、エチレングリコールモノエチルエーテル、エチレングリコールモノブチルエーテル、ジエチレングリコールジブチルエーテル等のグリコールアルキルエーテル類;(エイコサン二酸/テトラデカン二酸)ポリグリセリル-10、テトラデカン二酸ポリグリセリル-10等の水溶性エステル類;ソルビトール、キシリトール、エリスリトール、マンニトール、マルチトール等の糖アルコール類;グルコース、フルクトース、ガラクトース、マンノース、トレオース、キシロース、アラビノース、フコース、リボース、デオキシリボース、マルトース、トレハロース、ラクトース、ラフィノース、グルコン酸、グルクロン酸、シクロデキストリン類(α-、β-、γ-シクロデキストリン、及び、マルトシル化、ヒドロキシアルキル化等の修飾シクロデキストリン)、β-グルカン、キチン、キトサン、ヘパリン及び誘導体、ペクチン、アラビノガラクタン、デキストリン、デキストラン、グリコーゲン、エチルグルコシド、メタクリル酸グルコシルエチル重合物若しくは共重合物等の糖類及びその誘導体類;ヒアルロン酸、ヒアルロン酸ナトリウム;コンドロイチン硫酸ナトリウム;ムコイチン硫酸、カロニン硫酸、ケラト硫酸、デルマタン硫酸;シロキクラゲ抽出物、シロキクラゲ多糖体;フコイダン;チューベロース多糖体又は天然由来多糖体;クエン酸、酒石酸、乳酸等の有機酸及びその塩;尿素及びその誘導体;2-ピロリドン-5-カルボン酸及びそのナトリウム等の塩;ベタイン(トリメチルグリシン)、プロリン、ヒドロキシプロリン、アルギニン、リジン、セリン、グリシン、アラニン、フェニルアラニン、チロシン、β-アラニン、スレオニン、グルタミン酸、グルタミン、アスパラギン、アスパラギン酸、システイン、シスチン、メチオニン、ロイシン、イソロイシン、バリン、トリプトファン、ヒスチジン、タウリン等のアミノ酸類及びその塩;コラーゲン、魚由来コラーゲン、アテロコラーゲン、ゼラチン、エラスチン、コラーゲン分解ペプチド、加水分解コラーゲン、塩化ヒドロキシプロピルアンモニウム加水分解コラーゲン、エラスチン分解ペプチド、ケラチン分解ペプチド、加水分解ケラチン、コンキオリン分解ペプチド、加水分解コンキオリン、シルク蛋白分解ペプチド、加水分解シルク、ラウロイル加水分解シルクナトリウム、大豆蛋白分解ペプチド、小麦蛋白分解ペプチド、加水分解小麦蛋白、カゼイン分解ペプチド、アシル化ペプチド等の蛋白ペプチド類及びその誘導体;パルミトイルオリゴペプチド、パルミトイルペンタペプチド、パルミトイルテトラペプチド等のアシル化ペプチド類;シリル化ペプチド類;乳酸菌培養液、酵母抽出液、卵殻膜タンパク、牛顎下腺ムチン、ヒポタウリン、ゴマリグナン配糖体、グルタチオン、アルブミン、乳清;塩化コリン、ホスホリルコリン;胎盤抽出液、エアラスチン、コラーゲン、アロエ抽出物、ハマメリス水、ヘチマ水、カモミラエキス、カンゾウエキス、コンフリーエキス、シルクエキス、イザヨイバラエキス、セイヨウノコギリソウエキス、ユーカリエキス、メリロートエキス等の動物・植物抽出成分、天然型セラミド(タイプ1、2、3、4、5、6)、ヒドロキシセラミド、疑似セラミド、スフィンゴ糖脂質、セラミド及び糖セラミド含有エキス等のセラミド類が好ましいものとして挙げられる。 Examples of moisturizers / feel improvers include glycerin, trimethylolpropane, pentaerythritol, hexylene glycol, diglycerin, polyglycerin, diethylene glycol, dipropylene glycol, polypropylene glycol, ethylene glycol / propylene glycol copolymer and the like polyols and Polymers; glycol alkyl ethers such as diethylene glycol monoethyl ether (ethoxydiglycol), ethylene glycol monoethyl ether, ethylene glycol monobutyl ether, diethylene glycol dibutyl ether; (eicosane diacid / tetradecanedioic acid) polyglyceryl-10, tetradecane Water-soluble esters such as polyglyceryl-10; sorbitol, xylitol, erythritol, man Sugar alcohols such as tol and maltitol; glucose, fructose, galactose, mannose, threose, xylose, arabinose, fucose, ribose, deoxyribose, maltose, trehalose, lactose, raffinose, gluconic acid, glucuronic acid, cyclodextrins (α -, Β-, γ-cyclodextrin and modified cyclodextrins such as maltosylation, hydroxyalkylation, etc.), β-glucan, chitin, chitosan, heparin and derivatives, pectin, arabinogalactan, dextrin, dextran, glycogen, ethyl Sugars such as glucoside, glucosylethyl methacrylate polymer or copolymer, and derivatives thereof; hyaluronic acid, sodium hyaluronate; chondroitin sulfate sodium; mucoichi Sulfate, caronine sulfate, keratosulfate, dermatan sulfate; white jellyfish extract, white jellyfish polysaccharide; fucoidan; tuberose polysaccharide or naturally derived polysaccharide; organic acids such as citric acid, tartaric acid, lactic acid and their salts; urea and its derivatives; 2-pyrrolidone-5-carboxylic acid and salts thereof such as sodium; betaine (trimethylglycine), proline, hydroxyproline, arginine, lysine, serine, glycine, alanine, phenylalanine, tyrosine, β-alanine, threonine, glutamic acid, glutamine, Amino acids and their salts such as asparagine, aspartic acid, cysteine, cystine, methionine, leucine, isoleucine, valine, tryptophan, histidine, taurine; collagen, fish-derived collagen, atelocollagen, gelatin Elastin, collagen degrading peptide, hydrolyzed collagen, hydroxypropylammonium chloride hydrolyzed collagen, elastin degrading peptide, keratin degrading peptide, hydrolyzed keratin, conchiolin degrading peptide, hydrolyzed conchiolin, silk proteolytic peptide, hydrolyzed silk, lauroyl hydrolyzing Protein peptides such as silk sodium, soybean proteolytic peptide, wheat proteolytic peptide, hydrolyzed wheat protein, casein degrading peptide, acylated peptide and derivatives thereof; acylated peptides such as palmitoyl oligopeptide, palmitoyl pentapeptide, palmitoyl tetrapeptide Silylated peptides: Lactic acid bacteria culture solution, yeast extract, eggshell membrane protein, bovine submandibular gland mucin, hypotaurine, sesameignan glycoside, glutathione, a Lubumin, whey; choline chloride, phosphorylcholine; placenta extract, aerostin, collagen, aloe extract, hamamelis water, loofah water, chamomile extract, licorice extract, comfrey extract, silk extract, Izayoi rose extract, yarrow extract, eucalyptus extract Ceramides, such as animal and plant extract components such as merirot extract, natural ceramide (types 1, 2, 3, 4, 5, 6), hydroxyceramide, pseudoceramide, glycosphingolipid, ceramide and sugar ceramide-containing extract It is mentioned as preferable.

 界面活性剤としては、陰イオン性界面活性剤、非イオン性界面活性剤、陽イオン性界面活性剤、両性界面活性剤、高分子界面活性剤等が好ましいものとして挙げられる。界面活性剤として好ましいものを例示すると、陰イオン性界面活性剤としては、ラウリン酸カリウム、ミリスチン酸カリウム等の脂肪酸塩;ラウリル硫酸ナトリウム、ラウリル硫酸トリエタノールアミン、ラウリル硫酸アンモニウム等のアルキル硫酸エステル塩;ラウレス硫酸ナトリウム、ラウレス硫酸トリエタノールアミン等のポリオキシエチレンアルキル硫酸塩;ココイルメチルタウリンナトリウム、ココイルメチルタウリンカリウム、ラウロイルメチルタウリンナトリウム、ミリストイルメチルタウリンナトリウム、ラウロイルメチルアラニンナトリウム、ラウロイルサルコシンナトリウム、ラウロイルサルコシントリエタノールアミン、ラウロイルグルタミン酸メチルアラニンナトリウム等のアシルN-メチルアミノ酸塩;ココイルグルタミン酸ナトリウム、ココイルグルタミン酸トリエタノールアミン、ラウロイルグルタミン酸ナトリウム、ミリストイルグルタミン酸ナトリウム、ステアロイルグルタミン酸ナトリウム、パルミトイルアスパラギン酸ジトリエタノールアミン、ココイルアラニントリエタノールアミン等のアシルアミノ酸塩;ラウレス酢酸ナトリウム等のポリオキシエチレンアルキルエーテル酢酸塩;ラウロイルモノエタノールアミドコハク酸ナトリウム等のコハク酸エステル塩;脂肪酸アルカノールアミドエーテルカルボン酸塩;アシル乳酸塩;ポリオキシエチレン脂肪アミン硫酸塩;脂肪酸アルカノールアミド硫酸塩;硬化ヤシ油脂肪酸グリセリン硫酸ナトリウム等の脂肪酸グリセリド硫酸塩;アルキルベンゼンポリオキシエチレン硫酸塩;α-オレフィンスルホン酸ナトリウム等のオレフィンスルホン酸塩;スルホコハク酸ラウリル2ナトリウム、スルホコハク酸ジオクチルナトリウム等のアルキルスルホコハク酸塩;スルホコハク酸ラウレス2ナトリウム、モノラウロイルモノエタノールアミドポリオキシエチレンスルホコハク酸ナトリウム、ラウリルポリプロピレングリコールスルホコハク酸ナトリウム等のアルキルエーテルスルホコハク酸塩;テトラデシルベンゼンスルホン酸ナトリウム、テトラデシルベンゼンスルホン酸トリエタノールアミン等のアルキルベンゼンスルホン酸塩;アルキルナフタレンスルホン酸塩;アルカンスルホン酸塩;α-スルホ脂肪酸メチルエステル塩;アシルイセチオン酸塩;アルキルグリシジルエーテルスルホン酸塩;アルキルスルホ酢酸塩;ラウレスリン酸ナトリウム、ジラウレスリン酸ナトリウム、トリラウレスリン酸ナトリウム、モノオレスリン酸ナトリウム等のアルキルエーテルリン酸エステル塩;ラウリルリン酸カリウム等のアルキルリン酸エステル塩;カゼインナトリウム;アルキルアリールエーテルリン酸塩;脂肪酸アミドエーテルリン酸塩;ホスファチジルグリセロール、ホスファチジルイノシトール、ホスファチジン酸等のリン脂質類;カルボン酸変性シリコーン、リン酸変性シリコーン、硫酸変性シリコーン等のシリコーン系陰イオン性界面活性剤等;非イオン性界面活性剤としては、ラウレス(ポリオキシエチレンラウリルエーテル)類、セテス(ポリオキシエチレンセチルエーテル)類、ステアレス(ポリオキシエチレンステアリルエーテル)類、ベヘネス(ポリオキシエチレンベヘニルエーテル)類、イソステアレス(ポリオキシエチレンイソステアリルエーテル)類、オクチルドデセス(ポリオキシエチレンオクチルドデシルエーテル)類等の種々のポリオキシエチレン付加数のポリオキシエチレンアルキルエーテル類;ポリオキシエチレンアルキルフェニルエーテル;ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンヒマシ油、ポリオキシエチレン硬化ヒマシ油モノイソステアレート、ポリオキシエチレン硬化ヒマシ油トリイソステアレート、ポリオキシエチレン硬化ヒマシ油モノピログルタミン酸モノイソステアリン酸ジエステル、ポリオキシエチレン硬化ヒマシ油マレイン酸等のヒマシ油及び硬化ヒマシ油誘導体;ポリオキシエチレンフィトステロール;ポリオキシエチレンコレステロール;ポリオキシエチレンコレスタノール;ポリオキシエチレンラノリン;ポリオキシエチレン還元ラノリン;ポリオキシエチレン・ポリオキシプロピレンセチルエーテル、ポリオキシエチレン・ポリオキシプロピレン2-デシルテトラデシルエーテル、ポリオキシエチレン・ポリオキシプロピレンモノブチルエーテル、ポリオキシエチレン・ポリオキシプロピレン水添ラノリン、ポリオキシエチレン・ポリオキシプロピレングリセリンエーテル等のポリオキシエチレン・ポリオキシプロピレンアルキルエーテル;ポリオキシエチレン・ポリオキシプロピレングリコール;PPG-9ジグリセリル等の(ポリ)グリセリンポリオキシプロピレングリコール;ステアリン酸グリセリル、イソステアリン酸グリセリル、パルミチン酸グリセリル、ミリスチン酸グリセリル、オレイン酸グリセリル、ヤシ油脂肪酸グリセリル、モノ綿実油脂肪酸グリセリン、モノエルカ酸グリセリン、セスキオレイン酸グリセリン、α,α’-オレイン酸ピログルタミン酸グリセリン、モノステアリン酸グリセリンリンゴ酸等のグリセリン脂肪酸部分エステル類;ステアリン酸ポリグリセリル-2、同3、同4、同5、同6、同8、同10、ジステアリン酸ポリグリセリル-6、同10、トリステアリン酸ポリグリセリル-2、デカステアリン酸ポリグリセリル-10、イソステアリン酸ポリグリセリル-2、同3、同4、同5、同6、同8、同10、ジイソステアリン酸ポリグリセリル-2(ジイソステアリン酸ジグリセリル)、同3、同10、トリイソステアリン酸ポリグリセリル-2、テトライソステアリン酸ポリグリセリル-2、デカイソステアリン酸ポリグリセリル-10、オレイン酸ポリグリセリル-2、同3、同4、同5、同6、同8、同10、ジオレイン酸ポリグリセリル-6、トリオレイン酸ポリグリセリル-2、デカオレイン酸ポリグリセリル-10等のポリグリセリン脂肪酸エステル;モノステアリン酸エチレングリコール等のエチレングリコールモノ脂肪酸エステル;モノステアリン酸プロピレングリコール等のプロピレングリコールモノ脂肪酸エステル;ペンタエリスリトール部分脂肪酸エステル;ソルビトール部分脂肪酸エステル;マルチトール部分脂肪酸エステル;マルチトールエーテル;ソルビタンモノオレエート、ソルビタンモノイソステアレート、ソルビタンモノラウレート、ソルビタンモノパルミテート、ソルビタンモノステアレート、ソルビタンセスキオレエート、ソルビタントリオレエート、ペンタ-2-エチルヘキシル酸ジグリセロールソルビタン、テトラ-2-エチルヘキシル酸ジグリセロールソルビタン等のソルビタン脂肪酸エステル;ショ糖脂肪酸エステル、メチルグルコシド脂肪酸エステル、ウンデシレン酸トレハロース等の糖誘導体部分エステル;カプリリルグルコシド等のアルキルグルコシド;アルキルポリグリコシド;ラノリンアルコール;還元ラノリン;ポリオキシエチレンジステアレート、ポリチレングリコールジイソステアレート、ポリオキシエチレンモノオレエート、ポリオキシエチレンジオレエート等のポリオキシエチレン脂肪酸モノ及びジエステル;ポリオキシエチレン・プロピレングリコール脂肪酸エステル;ポリオキシエチレングリセリンモノステアレート、ポリオキシエチレングリセリンモノイソステアレート、ポリオキシエチレングリセリントリイソステアレート等のポリオキシエチレンモノオレエート等のポリオキシエチレングリセリン脂肪酸エステル;ポリオキシエチレンソルビタンモノオレエート、ポリオキシエチレンソルビタンモノステアレート、ポリオキシエチレンソルビタンモノオレート、ポリオキシエチレンソルビタンテトラオレエート等のポリオキシエチレンソルビタン脂肪酸エステル;ポリオキシエチレンソルビトールモノラウレート、ポリオキシエチレンソルビトールモノオレエート、ポリオキシエチレンソルビトールペンタオレエート、ポリオキシエチレンソルビトールモノステアレート等のポリオキシエチレンソルビトール脂肪酸エステル;ポリオキシエチレンメチルグルコシド脂肪酸エステル;ポリオキシエチレンアルキルエーテル脂肪酸エステル;ポリオキシエチレンソルビトールミツロウ等のポリオキシエチレン動植物油脂類;イソステアリルグリセリルエーテル、キミルアルコール、セラキルアルコール、バチルアルコール等のアルキルグリセリルエーテル類;多価アルコールアルキルエーテル;ポリオキシエチレンアルキルアミン;テトラポリオキシエチレン・テトラポリオキシプロピレン-エチレンジアミン縮合物類;サポニン、ソホロリピッド等の天然系界面活性剤;ポリオキシエチレン脂肪酸アミド;ヤシ油脂肪酸モノエタノールアミド(コカミドMEA)、ヤシ油脂肪酸ジエタノールアミド(コカミドDEA)、ラウリン酸モノエタノールアミド(ラウラミドMEA)、ラウリン酸ジエタノールアミド(ラウラミドDEA)、ラウリン酸モノイソプロパノールアミド(ラウラミドMIPA)、パルミチン酸モノエタノールアミド(パルタミドMEA)、パルミチン酸ジエタノールアミド(パルタミドDEA)、ヤシ油脂肪酸メチルエタノールアミド(コカミドメチルMEA)等の脂肪酸アルカノールアミド類;ラウラミンオキシド、コカミンオキシド、ステアラミンオキシド、ベヘナミンオキシド等のアルキルジメチルアミンオキシド;アルキルエトキシジメチルアミンオキシド;ポリオキシエチレンアルキルメルカプタン;ジメチコンコポリオール等のポリエーテル変性シリコーン、ポリシロキサン・オキシアルキレン共重合体、ポリグリセリン変性シリコーン、糖変性シリコーン等のシリコーン系非イオン性界面活性剤等;陽イオン性界面活性剤としては、ベヘントリモニウムクロリド、ステアルトリモニウムクロリド、セトリモニウムクロリド、ラウリルトリモニウムクロリド等のアルキルトリメチルアンモニウムクロリド;ステアリルトリモニウムブロミド等のアルキルトリメチルアンモニウムブロミド;ジステアリルジモニウムクロリド、ジココジモニウムクロリド等のジアルキルジメチルアンモニウムクロリド;ステアラミドプロピルジメチルアミン、ステアラミドエチルジエチルアミン等の脂肪酸アミドアミン及びその塩;ステアロキシプロピルジメチルアミン等のアルキルエーテルアミン及びその塩又は四級塩;エチル硫酸長鎖分岐脂肪酸(12~31)アミノプロピルエチルジメチルアンモニウム、エチル硫酸ラノリン脂肪酸アミノプロピルエチルジメチルアンモニウム等の脂肪酸アミド型四級アンモニウム塩;ポリオキシエチレンアルキルアミン及びその塩又は四級塩;アルキルアミン塩;脂肪酸アミドグアニジウム塩;アルキルエーテルアミンモニウム塩;アルキルトリアルキレングリコールアンモニウム塩;ベンザルコニウム塩;ベンゼトニウム塩;塩化セチルピリジニウム等のピリジニウム塩;イミダゾリニウム塩;アルキルイソキノリニウム塩;ジアルキルモリホニウム塩;ポリアミン脂肪酸誘導体;アミノプロピルジメチコン及びアモジメチコン等のアミノ変性シリコーン、カチオン変性シリコーン、カチオン変性及びポリエーテル変性シリコーン、アミノ変性及びポリエーテル変性シリコーン等のシリコーン系陽イオン性界面活性剤等;両性界面活性剤としては、
ラウリルベタイン(ラウリルジメチルアミノ酢酸ベタイン)等のN-アルキル-N,N-ジメチルアミノ酸ベタイン;コカミドプロピルベタイン、ラウラミドプロピルベタイン等の脂肪酸アミドアルキル-N,N-ジメチルアミノ酸ベタイン;ココアンホ酢酸ナトリウム、ラウロアンホ酢酸ナトリウム等のイミダゾリン型ベタイン;アルキルジメチルタウリン等のアルキルスルホベタイン;アルキルジメチルアミノエタノール硫酸エステル等の硫酸型ベタイン;アルキルジメチルアミノエタノールリン酸エステル等のリン酸型ベタイン;ホスファチジルコリン、ホスファチジルエタノールアミン、ホスファチジルセリン、スフィンゴミエリン等のスフィンゴリン脂質、リゾレシチン、水素添加大豆リン脂質、部分水素添加大豆リン脂質、水素添加卵黄リン脂質、部分水素添加卵黄リン脂質、水酸化レシチン等のリン脂質類;シリコーン系両性界面活性剤等;高分子界面活性剤としては、ポリビニルアルコール、アルギン酸ナトリウム、デンプン誘導体、トラガントガム、アクリル酸・メタアクリル酸アルキル共重合体;シリコーン系各種界面活性剤が好ましいものとして挙げられる。
Preferred examples of the surfactant include an anionic surfactant, a nonionic surfactant, a cationic surfactant, an amphoteric surfactant, and a polymer surfactant. Examples of preferable surfactants include fatty acid salts such as potassium laurate and potassium myristate; alkyl sulfate esters such as sodium lauryl sulfate, triethanolamine lauryl sulfate, and ammonium lauryl sulfate; Polyoxyethylene alkyl sulfates such as sodium laureth sulfate and triethanolamine laureth sulfate; cocoyl methyl taurine sodium, cocoyl methyl taurine potassium, lauroyl methyl taurine sodium, myristoyl methyl taurine sodium, lauroyl methyl alanine sodium, lauroyl sarcosine sodium, lauroyl sarcosine tri Acyl N-methyl amino acid salts such as ethanolamine and sodium methylalanine lauroylglutamate; cocoyl Acyl amino acid salts such as sodium glutamate, triethanolamine cocoyl glutamate, sodium lauroyl glutamate, sodium myristoyl glutamate, sodium stearoyl glutamate, ditriethanolamine palmitoyl aspartate, cocoylalanine triethanolamine; polyoxyethylene alkyl ethers such as sodium laureth acetate Acetic acid salt; Succinic acid ester salt such as sodium lauroyl monoethanolamide succinate; Fatty acid alkanolamide ether carboxylate; Acyl lactate; Polyoxyethylene fatty amine sulfate; Fatty acid alkanolamide sulfate; Hardened coconut oil fatty acid sodium glyceryl sulfate Fatty acid glyceride sulfate such as alkylbenzene polyoxyethylene sulfate; α-olefin Olefin sulfonates such as sodium sulfonic acid sulfonate; Alkyl sulfosuccinates such as disodium lauryl sulfosuccinate and dioctyl sodium sulfosuccinate; disodium laureth sulfosuccinate, monolauroyl monoethanolamide polyoxyethylene sodium sodium sulfosuccinate, lauryl polypropylene glycol sulfosuccinic acid Alkyl ether sulfosuccinates such as sodium; alkylbenzene sulfonates such as sodium tetradecylbenzenesulfonate and triethanolamine tetradecylbenzenesulfonate; alkylnaphthalenesulfonates; alkanesulfonates; α-sulfo fatty acid methyl ester salts; Acyl isethionate; alkyl glycidyl ether sulfonate; alkyl sulfoacetate; laureth Alkyl ether phosphate salts such as sodium phosphate, sodium dilaureth phosphate, sodium trilaureth phosphate, sodium monooles phosphate; alkyl phosphate ester salts such as potassium lauryl phosphate; sodium caseinate; alkyl aryl ether phosphate; fatty acid amide Ether phosphates; Phospholipids such as phosphatidylglycerol, phosphatidylinositol, and phosphatidic acid; Silicone anionic surfactants such as carboxylic acid-modified silicone, phosphoric acid-modified silicone, and sulfuric acid-modified silicone; Nonionic surfactants These include laureth (polyoxyethylene lauryl ether), ceteth (polyoxyethylene cetyl ether), steareth (polyoxyethylene stearyl ether), behenez (polyoxy). Polyoxyethylene alkyl ethers with various polyoxyethylene addition numbers such as silethylene behenyl ethers), isosteares (polyoxyethylene isostearyl ether) s, octyldecesses (polyoxyethylene octyldodecyl ethers); Ether: Polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil monoisostearate, polyoxyethylene hydrogenated castor oil triisostearate, polyoxyethylene hydrogenated castor oil monopyroglutamic acid monoisostearic acid diester Castor oil and hardened castor oil derivatives such as polyoxyethylene hydrogenated castor oil maleic acid; polyoxyethylene phytosterol; polyoxyethylene cholesterol Polyoxyethylene cholestanol; polyoxyethylene lanolin; polyoxyethylene reduced lanolin; polyoxyethylene / polyoxypropylene cetyl ether, polyoxyethylene / polyoxypropylene 2-decyltetradecyl ether, polyoxyethylene / polyoxypropylene monobutyl ether Polyoxyethylene / polyoxypropylene hydrogenated lanolin, polyoxyethylene / polyoxypropylene glycerin ether and other polyoxyethylene / polyoxypropylene alkyl ethers; polyoxyethylene / polyoxypropylene glycol; PPG-9 diglyceryl and the like ( Poly) glycerin polyoxypropylene glycol; glyceryl stearate, glyceryl isostearate, glyceryl palmitate, milli Glyceryl fatty acid partial esters such as glyceryl tinate, glyceryl oleate, glyceryl coconut oil fatty acid glyceryl, mono-cotton oil fatty acid glycerin, glyceryl monoerucate, glyceryl sesquioleate, glycerin α, α'-oleic acid pyroglutamate, glyceryl monostearate Polyglyceryl stearate-2, 3, 4, 5, 6, 8, 10, 10 polyglyceryl-6 distearate, 10, polyglyceryl tristearate, polyglyceryl decastearate-10, isostearin Polyglyceryl-2, 3, 4, 5, 6, 8, 10, diisostearate polyglyceryl-2 (diglyceryl diisostearate), 3, 10, polyglyceryl-2 triisostearate, tetraisostearate Polyglyceryl-2, polyglyceryl-10 decaisostearate, polyglyceryl-2 oleate, 3, 4, 5, 6, 8, 10, dioleate polyglyceryl-6, trioleate polyglyceryl-2, dekaoleic acid Polyglyceryl fatty acid esters such as polyglyceryl-10; ethylene glycol monofatty acid esters such as ethylene glycol monostearate; propylene glycol monofatty acid esters such as propylene glycol monostearate; pentaerythritol partial fatty acid esters; sorbitol partial fatty acid esters; maltitol moieties Fatty acid ester; maltitol ether; sorbitan monooleate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbi Monostearate, sorbitan sesquioleate, sorbitan trioleate, penta-2-ethylhexyl diglycerol sorbitan, tetra-2-ethylhexyl diglycerol sorbitan, etc .; sucrose fatty acid ester, methyl glucoside fatty acid ester, undecylene Sugar derivative partial ester such as acid trehalose; alkyl glucoside such as caprylyl glucoside; alkyl polyglycoside; lanolin alcohol; reduced lanolin; polyoxyethylene distearate, polytylene glycol diisostearate, polyoxyethylene monooleate, poly Polyoxyethylene fatty acid mono- and diesters such as oxyethylene dioleate; polyoxyethylene propylene glycol fatty acid ester; Polyoxyethylene glycerol fatty acid esters such as polyoxyethylene monooleate such as xylethylene glycerol monostearate, polyoxyethylene glycerol monoisostearate, polyoxyethylene glycerol triisostearate; polyoxyethylene sorbitan monooleate, poly Polyoxyethylene sorbitan fatty acid esters such as oxyethylene sorbitan monostearate, polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan tetraoleate; polyoxyethylene sorbitol monolaurate, polyoxyethylene sorbitol monooleate, polyoxyethylene sorbitol Polyoxyethylene sorbitol such as pentaoleate and polyoxyethylene sorbitol monostearate Fatty acid ester; Polyoxyethylene methyl glucoside fatty acid ester; Polyoxyethylene alkyl ether fatty acid ester; Polyoxyethylene animal and vegetable fats and oils such as polyoxyethylene sorbitol beeswax; Isostearyl glyceryl ether, Kimyl alcohol, Serakyl alcohol, Batyl alcohol, etc. Polyglyceryl ethers; polyoxyethylene alkylamines; tetrapolyoxyethylene / tetrapolyoxypropylene-ethylenediamine condensates; natural surfactants such as saponins and sophorolipids; polyoxyethylene fatty acid amides; Palm oil fatty acid monoethanolamide (cocamide MEA), palm oil fatty acid diethanolamide (cocamide DEA), lauric acid monoethanolamide (Lauramide MEA), lauric acid diethanolamide (lauramide DEA), lauric acid monoisopropanolamide (lauramide MIPA), palmitic acid monoethanolamide (partamide MEA), palmitic acid diethanolamide (partamide DEA), palm oil fatty acid methylethanolamide ( Fatty acid alkanolamides such as cocamidomethyl MEA); alkyldimethylamine oxides such as lauramine oxide, cocamamine oxide, stearamine oxide, and behenamine oxide; alkylethoxydimethylamine oxide; polyoxyethylene alkyl mercaptan; dimethicone copolyol, etc. Polyether-modified silicone, polysiloxane / oxyalkylene copolymer, polyglycerin-modified silicone, sugar-modified silicone, etc. Nonionic surfactants of silicone, etc .; cationic surfactants include alkyltrimethylammonium chlorides such as behentrimonium chloride, steartrimonium chloride, cetrimonium chloride, lauryltrimonium chloride; stearyltrimonium bromide, etc. Alkyltrimethylammonium bromides; dialkyldimethylammonium chlorides such as distearyldimonium chloride and dicocodimonium chloride; fatty acid amidoamines and salts thereof such as stearamidepropyldimethylamine and stearamideethyldiethylamine; alkyl ethers such as stearoxypropyldimethylamine Amines and salts or quaternary salts thereof; ethyl sulfate long chain branched fatty acid (12-31) aminopropylethyldimethylammonium Fatty acid amide type quaternary ammonium salts such as lanolin fatty acid aminopropylethyldimethylammonium; polyoxyethylene alkylamines and salts or quaternary salts thereof; alkylamine salts; fatty acid amidoguanidinium salts; alkyl etheraminemonium salts; Benzalkonium salts; benzethonium salts; pyridinium salts such as cetylpyridinium chloride; imidazolinium salts; alkylisoquinolinium salts; dialkyl morpholinium salts; polyamine fatty acid derivatives; aminopropyl dimethicone and amodimethicone, etc. Silicone-based cationic surfactants such as amino-modified silicone, cation-modified silicone, cation-modified and polyether-modified silicone, amino-modified and polyether-modified silicone Examples of the amphoteric surfactant; etc
N-alkyl-N, N-dimethylamino acid betaines such as lauryl betaine (lauryldimethylaminoacetic acid betaine); fatty acid amide alkyl-N, N-dimethylamino acid betaines such as cocamidopropyl betaine and lauramidopropyl betaine; sodium cocoamphoacetate; Imidazoline-type betaines such as sodium lauroamphoacetate; alkylsulfobetaines such as alkyldimethyltaurine; sulfate-type betaines such as alkyldimethylaminoethanol sulfate; phosphate-type betaines such as alkyldimethylaminoethanol phosphate; phosphatidylcholine, phosphatidylethanolamine, Sphingophospholipids such as phosphatidylserine and sphingomyelin, lysolecithin, hydrogenated soybean phospholipid, partially hydrogenated soybean phospholipid, hydrogen Egg yolk phospholipids, partially hydrogenated egg yolk phospholipids, phospholipids such as hydroxylated lecithin; silicone-based amphoteric surfactants; polymer surfactants include polyvinyl alcohol, sodium alginate, starch derivatives, tragacanth gum, acrylic acid -Alkyl methacrylate copolymers; various silicone surfactants are preferred.

 溶剤としては、エタノール、2-プロパノール(イソプロピルアルコール)、ブタノール、イソブチルアルコール等の低級アルコール類;プロピレングリコール、ジエチレングリコール、ジプロピレングリコール、イソペンチルジオール等のグリコール類;ジエチレングリコールモノエチルエーテル(エトキシジグリコール)、エチレングリコールモノエチルエーテル、エチレングリコールモノブチルエーテル、トリエチレングリコールモノエチルエーテル、ジエチレングリコールジエチルエーテル、ジエチレングリコールジブチルエーテル、プロピレングリコールモノエチルエーテル、ジプロピレングリコールモノエチルエーテル等のグリコールエーテル類;エチレングリコールモノエチルエーテルアセテート、ジエチレングリコールモノエチルエーテルアセテート、プロピレングリコールモノエチルエーテルアセテート等のグリコールエーテルエステル類;コハク酸ジエトキシエチル、エチレングリコールジサクシネート等のグリコールエステル類;ベンジルアルコール、ベンジルオキシエタノール、炭酸プロピレン、炭酸ジアルキル、アセトン、酢酸エチル、N-メチルピロリドン;トルエン等が好ましいものとして挙げられる。 Solvents include lower alcohols such as ethanol, 2-propanol (isopropyl alcohol), butanol and isobutyl alcohol; glycols such as propylene glycol, diethylene glycol, dipropylene glycol and isopentyl diol; diethylene glycol monoethyl ether (ethoxydiglycol) , Glycol ethers such as ethylene glycol monoethyl ether, ethylene glycol monobutyl ether, triethylene glycol monoethyl ether, diethylene glycol diethyl ether, diethylene glycol dibutyl ether, propylene glycol monoethyl ether, dipropylene glycol monoethyl ether; ethylene glycol monoethyl ether Acetate, diethylene glycol Glycol ether esters such as ethyl ether acetate and propylene glycol monoethyl ether acetate; glycol esters such as diethoxyethyl succinate and ethylene glycol disuccinate; benzyl alcohol, benzyloxyethanol, propylene carbonate, dialkyl carbonate, acetone, acetic acid Preferred examples include ethyl, N-methylpyrrolidone and toluene.

 酸化防止剤としては、トコフェロール(ビタミンE)、酢酸トコフェロール等のトコフェロール誘導体;BHT、BHA;没食子酸プロピル等の没食子酸誘導体;ビタミンC(アスコルビン酸)及び/又はその誘導体;エリソルビン酸及びその誘導体;亜硫酸ナトリウム等の亜硫酸塩;亜硫酸水素ナトリウム等の亜硫酸水素塩;チオ硫酸ナトリウム等のチオ硫酸塩;メタ亜硫酸水素塩;チオタウリン、ヒポタウリン;チオグリセロール、チオ尿素、チオグリコール酸、システイン塩酸塩が好ましいものとして挙げられる。 Antioxidants include tocopherol derivatives such as tocopherol (vitamin E) and tocopherol acetate; BHT, BHA; gallic acid derivatives such as propyl gallate; vitamin C (ascorbic acid) and / or derivatives thereof; erythorbic acid and derivatives thereof; Preferred are sulfites such as sodium sulfite; bisulfites such as sodium bisulfite; thiosulfates such as sodium thiosulfate; metabisulfites; thiotaurine, hypotaurine; thioglycerol, thiourea, thioglycolic acid, cysteine hydrochloride As mentioned.

 還元剤としては、チオグリコール酸、システイン、システアミン等が好ましいものとして挙げられる。 Preferred examples of the reducing agent include thioglycolic acid, cysteine, cysteamine and the like.

 酸化剤としては、過酸化水素水、過硫酸アンモニウム、臭素酸ナトリウム、過炭酸等が好ましいものとして挙げられる。 Preferred examples of the oxidizing agent include hydrogen peroxide water, ammonium persulfate, sodium bromate, percarbonate, and the like.

 防腐剤・抗菌剤・殺菌剤としては、メチルパラベン、エチルパラベン、プロピルパラベン、ブチルパラベン等のヒドロキシ安息香酸及びその塩若しくはそのエステル;サリチル酸;安息香酸ナトリウム;フェノキシエタノール;メチルクロロイソチアゾリノン、メチルイソチアゾリノン等のイソチアゾリンオン誘導体;イミダゾリニウムウレア;デヒドロ酢酸及びその塩;フェノール類;トリクロサン等のハロゲン化ビスフェノール類、酸アミド類、四級アンモニウム塩類;トリクロロカルバニド、ジンクピリチオン、塩化ベンザルコニウム、塩化ベンゼトニウム、ソルビン酸、クロルヘキシジン、グルコン酸クロルヘキシジン、ハロカルバン、ヘキサクロロフェン、ヒノキチオール;フェノール、イソプロピルフェノール、クレゾール、チモール、パラクロロフェノール、フェニルフェノール、フェニルフェノールナトリウム等のその他フェノール類;フェニルエチルアルコール、感光素類、抗菌性ゼオライト、銀イオンが好ましいものとして挙げられる。 Examples of preservatives, antibacterial agents, and bactericides include hydroxybenzoic acid such as methylparaben, ethylparaben, propylparaben, and butylparaben, and salts or esters thereof; salicylic acid; sodium benzoate; phenoxyethanol; methylchloroisothiazolinone, methylisothiazo Isothiazolinone derivatives such as linone; imidazolinium urea; dehydroacetic acid and its salts; phenols; halogenated bisphenols such as triclosan, acid amides, quaternary ammonium salts; trichlorocarbanide, zinc pyrithione, benzalkonium chloride, chloride Benzethonium, sorbic acid, chlorhexidine, chlorhexidine gluconate, halocarban, hexachlorophene, hinokitiol; phenol, isopropylphenol, cresol, Mall, para chlorophenol, phenylphenol, other phenols such as phenylphenol sodium; phenylethyl alcohol, photosensitive Motorui, be mentioned as antibacterial zeolite, silver ion.

 キレート剤としては、EDTA、EDTA2Na、EDTA3Na、EDTA4Na等のエデト酸塩(エチレンジアミン四酢酸塩);HEDTA3Na等のヒドロキシエチルエチレンジアミン三酢酸塩;ペンテト酸塩(ジエチレントリアミン五酢酸塩);フィチン酸;エチドロン酸等のホスホン酸及びそのナトリウム塩等の塩類;ポリアスパラギン酸、ポリグルタミン酸等のポリアミノ酸類;ポリリン酸ナトリウム、メタリン酸ナトリウム、リン酸;クエン酸ナトリウム、クエン酸、アラニン、ジヒドロキシエチルグリシン、グルコン酸、アスコルビン酸、コハク酸、酒石酸が好ましいものとして挙げられる。 Examples of chelating agents include edetate (ethylenediaminetetraacetate) such as EDTA, EDTA2Na, EDTA3Na, and EDTA4Na; hydroxyethylethylenediaminetriacetate such as HEDTA3Na; pentetate (diethylenetriaminepentaacetate); phytic acid; Phosphonic acid and its sodium salt; polyamino acids such as polyaspartic acid and polyglutamic acid; sodium polyphosphate, sodium metaphosphate, phosphoric acid; sodium citrate, citric acid, alanine, dihydroxyethylglycine, gluconic acid, Ascorbic acid, succinic acid and tartaric acid are preferred.

 pH調整剤・酸・アルカリとしては、クエン酸、クエン酸ナトリウム、乳酸、乳酸ナトリウム、乳酸カリウム、グリコール酸、コハク酸、酢酸、酢酸ナトリウム、リンゴ酸、酒石酸、フマル酸、リン酸、塩酸、硫酸、モノエタノールアミン、ジエタノールアミン、トリエタノールアミン、イソプロパノールアミン、トリイソプロパノールアミン、2-アミノ-2-メチル-1,3-プロパンジオール、2-アミノ-2-ヒドロキシメチル-1,3-プロパンジオール、アルギニン、水酸化ナトリウム、水酸化カリウム、アンモニア水、炭酸グアニジン、炭酸アンモニウムが好ましいものとして挙げられる。 pH adjusters / acids / alkalis include citric acid, sodium citrate, lactic acid, sodium lactate, potassium lactate, glycolic acid, succinic acid, acetic acid, sodium acetate, malic acid, tartaric acid, fumaric acid, phosphoric acid, hydrochloric acid, sulfuric acid , Monoethanolamine, diethanolamine, triethanolamine, isopropanolamine, triisopropanolamine, 2-amino-2-methyl-1,3-propanediol, 2-amino-2-hydroxymethyl-1,3-propanediol, arginine Sodium hydroxide, potassium hydroxide, aqueous ammonia, guanidine carbonate, and ammonium carbonate are preferable.

 粉体としては、マイカ、タルク、カオリン、セリサイト、モンモリロナイト、カオリナイト、雲母、白雲母、金雲母、合成雲母、紅雲母、黒雲母、パーミキュライト、炭酸マグネシウム、炭酸カルシウム、ケイ酸アルミニウム、ケイ酸バリウム、ケイ酸カルシウム、ケイ酸マグネシウム、ケイ酸ストロンチウム、タングステン酸金属塩、マグネシウム、ゼオライト、硫酸バリウム、焼成硫酸カルシウム、リン酸カルシウム、弗素アパタイト、ヒドロキシアパタイト、セラミックパウダー、ベントナイト、スメクタイト、粘土、泥、金属石鹸(例えば、ミリスチン酸亜鉛、パルミチン酸カルシウム、ステアリン酸アルミニウム)、炭酸カルシウム、ベンガラ、黄酸化鉄、黒酸化鉄、群青、紺青、カーボンブラック、酸化チタン、微粒子及び超微粒子酸化チタン、酸化亜鉛、微粒子及び超微粒子酸化亜鉛、アルミナ、シリカ、煙霧状シリカ(超微粒子無水ケイ酸)、雲母チタン、魚鱗箔、窒化ホウ素、ホトクロミック顔料、合成フッ素金雲母、微粒子複合粉体、金、アルミニウム等の各種の大きさ・形状の無機粉体、及び、これらをハイドロジェンシリコーン、環状ハイドロジェンシリコーン等のシリコーン若しくはその他のシラン若しくはチタンカップリング剤等の各種表面処理剤で処理を行って疎水化若しくは親水化した粉体等の無機粉体;デンプン、セルロース、ナイロンパウダー、ポリエチレン末、ポリメタクリル酸メチル末、ポリスチレン末、スチレンとアクリル酸の共重合体樹脂粉末、ポリエステル末、ベンゾグアナミン樹脂粉末、ポリエチレンテレフタレート・ポリメチルメタクリレート積層末、ポリエチレンテレフタレート・アルミニウム・エポキシ積層末等、ウレタン粉末、シリコーン粉末、テフロン(登録商標)粉末等の各種の大きさ・形状の有機系粉体及び表面処理粉体、有機無機複合粉体が好ましいものとして挙げられる。 Examples of powders include mica, talc, kaolin, sericite, montmorillonite, kaolinite, mica, muscovite, phlogopite, synthetic mica, saucite, biotite, permiculite, magnesium carbonate, calcium carbonate, aluminum silicate, and silicic acid. Barium, calcium silicate, magnesium silicate, strontium silicate, metal tungstate, magnesium, zeolite, barium sulfate, calcined calcium sulfate, calcium phosphate, fluorine apatite, hydroxyapatite, ceramic powder, bentonite, smectite, clay, mud, metal Soap (eg, zinc myristate, calcium palmitate, aluminum stearate), calcium carbonate, bengara, yellow iron oxide, black iron oxide, ultramarine, bitumen, carbon black, titanium oxide, fine particles and super Titanium oxide, zinc oxide, fine and ultrafine zinc oxide, alumina, silica, fumed silica (ultrafine silica), mica titanium, fish scale foil, boron nitride, photochromic pigment, synthetic fluorophlogopite, fine particle composite powder Body, gold, aluminum, etc., various sizes and shapes of inorganic powders, and these are treated with various surface treatment agents such as hydrogen silicone, cyclic hydrogen silicone, or other silane or titanium coupling agents Inorganic powders such as hydrophobized or hydrophilized powders; starch, cellulose, nylon powder, polyethylene powder, polymethyl methacrylate powder, polystyrene powder, copolymer resin powder of styrene and acrylic acid, polyester powder, Benzoguanamine resin powder, polyethylene terephthalate polymer Organic powders and surface-treated powders of various sizes and shapes, such as polyurethane powder, polyethylene terephthalate / aluminum / epoxy powder, urethane powder, silicone powder, Teflon (registered trademark) powder, organic-inorganic composite powder The body is preferred.

 無機塩類としては、食塩、並塩、岩塩、海塩、天然塩等の塩化ナトリウム含有塩類;塩化カリウム、塩化アルミニウム、塩化カルシウム、塩化マグネシウム、にがり、塩化亜鉛、塩化アンモニウム;硫酸ナトリウム、硫酸アルミニウム、硫酸アルミニウム・カリウム(ミョウバン)、硫酸アルミニウム・アンモニウム、硫酸バリウム、硫酸カルシウム、硫酸カリウム、硫酸マグネシウム、硫酸亜鉛、硫酸鉄、硫酸銅;リン酸1Na・2Na・3Na等のリン酸ナトリウム類、リン酸カリウム類、リン酸カルシウム類、リン酸マグネシウム類が好ましいものとして挙げられる。 Inorganic salts include sodium chloride-containing salts such as salt, common salt, rock salt, sea salt, natural salt; potassium chloride, aluminum chloride, calcium chloride, magnesium chloride, bittern, zinc chloride, ammonium chloride; sodium sulfate, aluminum sulfate, Aluminum sulfate / potassium sulfate (alum), aluminum sulfate / ammonium sulfate, barium sulfate, calcium sulfate, potassium sulfate, magnesium sulfate, zinc sulfate, iron sulfate, copper sulfate; sodium phosphates such as 1Na, 2Na and 3Na phosphates, phosphoric acid Potassium, calcium phosphates and magnesium phosphates are preferred.

 紫外線吸収剤としては、パラアミノ安息香酸、パラアミノ安息香酸モノグリセリンエステル、N,N-ジプロポキシパラアミノ安息香酸エチルエステル、N,N-ジエトキシパラアミノ安息香酸エチルエステル、N,N-ジメチルパラアミノ安息香酸エチルエステル、N,N-ジメチルパラアミノ安息香酸ブチルエステル、N,N-ジメチルパラアミノ安息香酸メチルエステル等の安息香酸系紫外線吸収剤;ホモメンチル-N-アセチルアントラニレート等のアントラニル酸系紫外線吸収剤;サリチル酸及びそのナトリウム塩、アミルサリシレート、メンチルサリシレート、ホモメンチルサリシレート、オクチルサリシレート、フェニルサリシレート、ベンジルサリシレート、p-イソプロパノールフェニルサリシレート等のサリチル酸系紫外線吸収剤;オクチルシンナメート、エチル-4-イソプロピルシンナメート、メチル-2,5-ジイソプロピルシンナメート、エチル-2,4-ジイソプロピルシンナメート、メチル-2,4-ジイソプロピルシンナメート、プロピル-p-メトキシシンナメート、イソプロピル-p-メトキシシンナメート、イソアミル-p-メトキシシンナメート、2-エチルヘキシル-p-メトキシシンナメート(パラメトキシケイヒ酸オクチル)、2-エトキシエチル-p-メトキシシンナメート(シノキサート)、シクロヘキシル-p-メトキシシンナメート、エチル-α-シアノ-β-フェニルシンナメート、2-エチルヘキシル-α-シアノ-β-フェニルシンナメート(オクトクリン)、グリセリルモノ-2-エチルヘキサノイル-ジパラメトキシシンナメート、フェルラ酸及びその誘導体等の桂皮酸系紫外線吸収剤;2,4-ジヒドロキシベンゾフェノン、2,2’-ジヒドロキシ-4-メトキシベンゾフェノン、2,2’-ジヒドロキシ-4,4’-ジメトキシベンゾフェノン、2,2’,4,4’-テトラヒドロキシベンゾフェノン、2-ヒドロキシ-4-メトキシベンゾフェノン(オキシベンゾン-3)、2-ヒドロキシ-4-メトキシ-4’-メチルベンゾフェノン、2-ヒドロキシ-4-メトキシベンゾフェノン-5-スルホン酸塩、4-フェニルベンゾフェノン、2-エチルヘキシル-4’-フェニル-ベンゾフェノン-2-カルボキシレート、2-ヒドロキシ-4-n-オクトキシベンゾフェノン、4-ヒドロキシ-3-カルボキシベンゾフェノン等のベンゾフェノン系紫外線吸収剤;3-(4’-メチルベンジリデン)-d,l-カンフル、3-ベンジリデン-d,l-カンフル;2-フェニル-5-メチルベンゾキサゾール;2,2’-ヒドロキシ-5-メチルフェニルベンゾトリアゾール;2-(2’-ヒドロキシ-5’-t-オクチルフェニル)ベンゾトリアゾール;2-(2’-ヒドロキシ-5’-メチルフェニルベンゾトリアゾール;ジベンザラジン;ジアニソイルメタン;5-(3,3-ジメチル-2-ノルボルニリデン)-3-ペンタン-2-オン;4-t-ブチルメトキシジベンゾイルメタン等のジベンゾイルメタン誘導体;オクチルトリアゾン;ウロカニン酸及びウロカニン酸エチル等のウロカニン酸誘導体;2-(2’-ヒドロキシ-5’-メチルフェニル)ベンゾトリアゾール、1-(3,4-ジメトキシフェニル)-4,4-ジメチル-1,3-ペンタンジオン、ジメトキシベンジリデンジオキソイミダゾリジンプロピオン酸2-エチルヘキシル等のヒダントイン誘導体、フェニルベンズイミダソゾールスルホン酸、テレフタリリデンジカンフルスルホン酸、ドロメトリゾールトリシロキサン、アントラニル酸メチル、ルチン及びその誘導体、オリザノール及びその誘導体が好ましいものとして挙げられる。 Examples of ultraviolet absorbers include paraaminobenzoic acid, paraaminobenzoic acid monoglycerin ester, N, N-dipropoxyparaaminobenzoic acid ethyl ester, N, N-diethoxyparaaminobenzoic acid ethyl ester, and N, N-dimethylparaaminobenzoic acid ethyl ester. Benzoic acid ultraviolet absorbers such as esters, N, N-dimethylparaaminobenzoic acid butyl ester, N, N-dimethylparaaminobenzoic acid methyl ester; Anthranilic acid ultraviolet absorbers such as homomenthyl-N-acetylanthranilate; Salicylic acid And salicylic acid systems such as sodium salt, amyl salicylate, menthyl salicylate, homomenthyl salicylate, octyl salicylate, phenyl salicylate, benzyl salicylate, p-isopropanol phenyl salicylate External line absorbent: octyl cinnamate, ethyl-4-isopropyl cinnamate, methyl-2,5-diisopropyl cinnamate, ethyl-2,4-diisopropyl cinnamate, methyl-2,4-diisopropyl cinnamate, propyl-p- Methoxycinnamate, isopropyl-p-methoxycinnamate, isoamyl-p-methoxycinnamate, 2-ethylhexyl-p-methoxycinnamate (octyl paramethoxycinnamate), 2-ethoxyethyl-p-methoxycinnamate (sinoxate) Cyclohexyl-p-methoxycinnamate, ethyl-α-cyano-β-phenylcinnamate, 2-ethylhexyl-α-cyano-β-phenylcinnamate (octocrine), glyceryl mono-2-ethylhexanoyl-diparame Cinnamic acid UV absorbers such as toxicinnamate, ferulic acid and derivatives thereof; 2,4-dihydroxybenzophenone, 2,2′-dihydroxy-4-methoxybenzophenone, 2,2′-dihydroxy-4,4′-dimethoxy Benzophenone, 2,2 ′, 4,4′-tetrahydroxybenzophenone, 2-hydroxy-4-methoxybenzophenone (oxybenzone-3), 2-hydroxy-4-methoxy-4′-methylbenzophenone, 2-hydroxy-4- Methoxybenzophenone-5-sulfonate, 4-phenylbenzophenone, 2-ethylhexyl-4′-phenyl-benzophenone-2-carboxylate, 2-hydroxy-4-n-octoxybenzophenone, 4-hydroxy-3-carboxybenzophenone Benzofe etc. UV absorbers; 3- (4′-methylbenzylidene) -d, l-camphor, 3-benzylidene-d, l-camphor; 2-phenyl-5-methylbenzoxazole; 2,2′-hydroxy- 2- (2′-hydroxy-5′-t-octylphenyl) benzotriazole; 2- (2′-hydroxy-5′-methylphenylbenzotriazole; dibenzalazine; dianisoylmethane; 5- (3,3-dimethyl-2-norbornylidene) -3-pentan-2-one; dibenzoylmethane derivatives such as 4-t-butylmethoxydibenzoylmethane; octyl triazone; urocanic acid such as urocanic acid and ethyl urocanate Derivatives; 2- (2′-hydroxy-5′-methylphenyl) benzotriazole Hydantoin derivatives such as 1- (3,4-dimethoxyphenyl) -4,4-dimethyl-1,3-pentanedione, dimethoxybenzylidenedioxoimidazolidinepropionate 2-ethylhexyl, phenylbenzimidazolazolesulfonic acid, terephthalate Preference is given to liridene dicamphorsulfonic acid, drometrizol trisiloxane, methyl anthranilate, rutin and its derivatives, oryzanol and its derivatives.

 美白剤としては、アルブチン、α-アルブチン等のヒドロキノン配糖体及びそのエステル類;アスコルビン酸、アスコルビン酸リン酸エステルナトリウム塩及びアスコルビン酸リン酸エステルマグネシウム塩等のアスコルビン酸リン酸エステル塩、アスコルビン酸テトライソパルミチン酸エステル等のアスコルビン酸脂肪酸エステル、アスコルビン酸エチルエーテル等のアスコルビン酸アルキルエーテル、アスコルビン酸-2-グルコシド等のアスコルビン酸グルコシド及びその脂肪酸エステル類、アスコルビン酸硫酸エステル、リン酸トコフェリルアスコルビル等のアスコルビン酸誘導体;コウジ酸、エラグ酸、トラネキサム酸及びその誘導体、フェルラ酸及びその誘導体、プラセンタエキス、グルタチオン、オリザノール、ブチルレゾルシノール、油溶性カモミラエキス、油溶性カンゾウエキス、西河柳エキス、ユキノシタエキス等植物エキスが好ましいものとして挙げられる。 Examples of whitening agents include hydroquinone glycosides such as arbutin and α-arbutin and their esters; ascorbic acid phosphates such as ascorbic acid, sodium ascorbic acid phosphate and magnesium ascorbic acid phosphate, ascorbic acid Ascorbic acid fatty acid esters such as tetraisopalmitic acid ester, ascorbic acid alkyl ethers such as ascorbic acid ethyl ether, ascorbic acid glucosides such as ascorbic acid-2-glucoside and fatty acid esters thereof, ascorbic acid sulfate ester, tocopheryl ascorbyl phosphate Ascorbic acid derivatives such as kojic acid, ellagic acid, tranexamic acid and its derivatives, ferulic acid and its derivatives, placenta extract, glutathione, oryzanol, butylreso Shinoru, oil-soluble Kamomiraekisu, oil-soluble licorice extract, Nishikawa willow extract, be mentioned as saxifrage extract, and the like plant extracts are preferred.

 ビタミン類及びその誘導体類としては、レチノール、酢酸レチノール、パルミチン酸レチノール等のビタミンA類;チアミン塩酸塩、チアミン硫酸塩、リボフラビン、酢酸リボフラビン、塩酸ピリドキシン、ピリドキシンジオクタノエート、ピリドキシンジパルミテート、フラビンアデニンジヌクレオチド、シアノコバラミン、葉酸類、ニコチン酸アミド・ニコチン酸ベンジル等のニコチン酸類、コリン類等のビタミンB群類;アスコルビン酸及びそのナトリウム等の塩等のビタミンC類;ビタミンD;α、β、γ、δ-トコフェロール等のビタミンE類;パントテン酸、ビオチン等のその他ビタミン類;アスコルビン酸リン酸エステルナトリウム塩及びアスコルビン酸リン酸エステルマグネシウム塩等のアスコルビン酸リン酸エステル塩、アスコルビン酸テトライソパルミチン酸エステル・ステアリン酸アスコルビル・パルミチン酸アスコルビル・ジパルミチン酸アスコルビル等のアスコルビン酸脂肪酸エステル、アスコルビン酸エチルエーテル等のアスコルビン酸アルキルエーテル、アスコルビン酸-2-グルコシド等のアスコルビン酸グルコシド及びその脂肪酸エステル、リン酸トコフェリルアスコルビル等のアスコルビン酸誘導体;ニコチン酸トコフェロール、酢酸トコフェロール、リノール酸トコフェロール、フェルラ酸トコフェロール、トコフェロールリン酸エステル等のトコフェロール誘導体等のビタミン誘導体、トコトリエノール、その他各種ビタミン誘導体類が好ましいものとして挙げられる。 Vitamins and their derivatives include vitamin A such as retinol, retinol acetate, retinol palmitate; thiamine hydrochloride, thiamine sulfate, riboflavin, riboflavin acetate, pyridoxine hydrochloride, pyridoxine dioctanoate, pyridoxine dipalmitate, Flavin adenine dinucleotide, cyanocobalamin, folic acid, nicotinic acid such as nicotinic acid amide / benzyl nicotinate, vitamin B group such as choline; vitamin C such as ascorbic acid and its sodium salt; vitamin D; α, Vitamin E such as β, γ, and δ-tocopherol; other vitamins such as pantothenic acid and biotin; ascorbic acid phosphates such as ascorbic acid phosphate sodium salt and ascorbic acid phosphate magnesium salt, Ascorbic acid fatty acid esters such as ascorbyl tetraisopalmitate, ascorbyl stearate, ascorbyl palmitate and ascorbyl dipalmitate, ascorbic acid alkyl ethers such as ascorbic acid ethyl ether, ascorbic acid glucosides such as ascorbic acid-2-glucoside and Ascorbic acid derivatives such as fatty acid esters and tocopheryl phosphate ascorbyl; vitamin derivatives such as tocopherol nicotinate, tocopherol acetate, tocopherol acetate, tocopherol linoleate, tocopherol phosphate, tocopherol phosphate etc., tocotrienol, and other various vitamin derivatives Is preferable.

 育毛用薬剤・血行促進剤・刺激剤としては、センブリエキス、トウガラシチンキ、ショウキョウチンキ、ショウキョウエキス、カンタリスチンキ等の植物エキス・チンキ類;カプサイシン、ノニル酸ワニリルアミド、ジンゲロン、イクタモール、タンニン酸、ボルネオール、シクランデレート、シンナリジン、トラゾリン、アセチルコリン、ベラパミル、セファランチン、γ-オリザノール、ビタミンE及びニコチン酸トコフェロール・酢酸トコフェロール等の誘導体、ニコチン酸及びニコチン酸アミド・ニコチン酸ベンジルエステル・イノシトールヘキサニコチネート、ニコチンアルコール等の誘導体、アラントイン、感光素301、感光素401、塩化カプロニウム、ペンタデカン酸モノグリセリド、フラバノノール誘導体、スチグマステロール又はスチグマスタノール及びその配糖体、ミノキシジルが好ましいものとして挙げられる。 Plant extracts and tinctures such as assembly extract, red pepper tincture, ginger tincture, ginger extract, cantalis tincture; capsaicin, nonylic acid vanillylamide, gingeron, ictamol, tannic acid Borneol, cyclandrate, cinnarizine, trazoline, acetylcholine, verapamil, cephalanthin, γ-oryzanol, vitamin E and derivatives such as nicotinic acid tocopherol / acetic acid tocopherol, nicotinic acid and nicotinic acid amide / nicotinic acid benzyl ester / inositol hexanicotinate Derivatives of nicotine alcohol, allantoin, photosensitive element 301, photosensitive element 401, capronium chloride, pentadecanoic acid monoglyceride, flavonol derivative, stigma Terol or stigmastanol and glycosides thereof, and the like as minoxidil are preferred.

 ホルモン類としては、エストラジオール、エストロン、エチニルエストラジオール、コルチゾン、ヒドロコルチゾン、プレドニゾン等が好ましいものとして挙げられる。抗しわ剤、抗老化剤、ひきしめ剤、冷感剤、温感剤、創傷治癒促進剤、刺激緩和剤、鎮痛剤、細胞賦活剤等のその他の薬効剤としては、レチノール類、レチノイン酸類、レチノイン酸トコフェリル;乳酸、グリコール酸、グルコン酸、フルーツ酸、サリチル酸及びその配糖体・エステル化物等の誘導体、ヒドロキシカプリン酸、長鎖α-ヒドロキシ脂肪酸、長鎖α-ヒドロキシ脂肪酸コレステリル等のα-又はβ-ヒドロキシ酸類及びその誘導体類;γ-アミノ酪酸、γ-アミノ-β-ヒドロキシ酪酸;カルニチン;カルノシン;クレアチン;セラミド類、スフィンゴシン類;カフェイン、キサンチン等及びその誘導体;コエンザイムQ10、カロチン、リコピン、アスタキサンチン、ルテイン、α-リポ酸、白金ナノコロイド、フラーレン類等の抗酸化・活性酸素消去剤;カテキン類;ケルセチン等のフラボン類;イソフラボン類;没食子酸及びエステル糖誘導体;タンニン、セサミン、プロトアントシアニジン、クロロゲン酸、リンゴポリフェノール等のポリフェノール類;ルチン及び配糖体等の誘導体;ヘスペリジン及び配糖体等の誘導体;リグナン配糖体;グラブリジン、グラブレン、リクイリチン、イソリクイリチン等のカンゾウエキス関連物質;ラクトフェリン;ショウガオール、ジンゲロール;メントール、セドロール等の香料物質及びその誘導体;カプサイシン、バニリン等及び誘導体;ジエチルトルアミド等の昆虫忌避剤;生理活性物質とシクロデキストリン類との複合体が好ましいものとして挙げられる。 Preferred examples of hormones include estradiol, estrone, ethinyl estradiol, cortisone, hydrocortisone, prednisone and the like. Other remedies such as anti-wrinkle agents, anti-aging agents, squeeze agents, cooling sensations, warming sensation agents, wound healing promoters, irritation relievers, analgesics, cell activators include retinols, retinoic acids, retinoin Acid tocopheryl; derivatives such as lactic acid, glycolic acid, gluconic acid, fruit acid, salicylic acid and glycosides / esterified products thereof, α- or such as hydroxycapric acid, long chain α-hydroxy fatty acid, long chain α-hydroxy fatty acid cholesteryl β-hydroxy acids and derivatives thereof; γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid; carnitine; carnosine; creatine; ceramides, sphingosines; caffeine, xanthine and the like; coenzyme Q10, carotene, lycopene , Astaxanthin, lutein, α-lipoic acid, platinum nanocolloid, fullerenes, etc. Antioxidant / active oxygen scavengers; catechins; flavones such as quercetin; isoflavones; gallic acid and ester sugar derivatives; polyphenols such as tannin, sesamin, protoanthocyanidin, chlorogenic acid, apple polyphenol; rutin and glycosides, etc. Derivatives of hesperidin and glycosides; lignan glycosides; licorice extract-related substances such as grabrizine, glabrene, liquiritin, and isoliquiritin; lactoferrin; shogaol, gingerol; and fragrance substances such as menthol and cedrol; And insecticides such as diethyl toluamide; complexes of physiologically active substances and cyclodextrins are preferred.

 植物・動物・微生物エキス類としては、アイリスエキス、アシタバエキス、アスナロエキス、アスパラガスエキス、アボカドエキス、アマチャエキス、アーモンドエキス、アルテアエキス、アルニカエキス、アロエエキス、アンズエキス、アンズ核エキス、イチョウエキス、インチンコウエキス、ウイキョウエキス、ウコンエキス、ウーロン茶エキス、ウワウルシエキス、エイジツエキス、エチナシ葉エキス、エンメイソウエキス、オウゴンエキス、オウバクエキス、オウレンエキス、オオムギエキス、オタネニンジンエキス、オトギリソウエキス、オドリコソウエキス、オノニスエキス、オランダカラシエキス、オレンジエキス、海水乾燥物、海藻エキス、カキ葉エキス、カキョクエキス、加水分解エラスチン、加水分解コムギ末、加水分解シルク、カッコンエキス、カモミラエキス、油溶性カモミラエキス、カロットエキス、カワラヨモギエキス、カラスムギエキス、カルカデエキス、カンゾウエキス、油溶性カンゾウエキス、キウイエキス、キオウエキス、キクラゲエキス、キナエキス、キューカンバーエキス、キリ葉エキス、グアノシン、グアバエキス、クジンエキス、クチナシエキス、クマザサエキス、クララエキス、クルミエキス、クリエキス、グレープフルーツエキス、クレマティスエキス、黒米エキス、黒砂糖抽出物、黒酢、クロレラエキス、クワエキス、ゲンチアナエキス、ゲンノショウコエキス、紅茶エキス、酵母エキス、コウボクエキス、コーヒーエキス、ゴボウエキス、コメエキス、コメ発酵エキス、コメヌカ発酵エキス、コメ胚芽油、コンフリーエキス、コラーゲン、コケモモエキス、サイシンエキス、サイコエキス、サイタイ抽出液、サフランエキス、サルビアエキス、サボンソウエキス、ササエキス、サンザシエキス、サンシャエキス、サンショウエキス、シイタケエキス、ジオウエキス、シコンエキス、シソエキス、シナノキエキス、シモツケソウエキス、ジャトバエキス、シャクヤクエキス、ショウキュウエキス、ショウブ根エキス、シラカバエキス、白キクラゲエキス、スギナエキス、ステビアエキス、ステビア発酵物、西河柳エキス、セイヨウキズタエキス、セイヨウサンザシエキス、セイヨウニワトコエキス、セイヨウノコギリソウエキス、セイヨウハッカエキス、セージエキス、ゼニアオイエキス、センキュウエキス、センブリエキス、ソウハクヒエキス、ダイオウエキス、ダイズエキス、タイソウエキス、タイムエキス、タンポポエキス、地衣類エキス、茶エキス、チョウジエキス、チガヤエキス、チンピエキス、ティートリー油、甜茶エキス、トウガラシエキス、トウキエキス、トウキンセンカエキス、トウニンエキス、トウヒエキス、ドクダミエキス、トマトエキス、納豆エキス、ニンジンエキス、ニンニクエキス、ノバラエキス、ハイビスカスエキス、バクモンドウエキス、ハスエキス、パセリエキス、バーチエキス、蜂蜜、ハマメリスエキス、パリエタリアエキス、ヒキオコシエキス、ビサボロール、ヒノキエキス、ビフィズス菌エキス、ビワエキス、フキタンポポエキス、フキノトウエキス、ブクリョウエキス、ブッチャーブルームエキス、ブドウエキス、ブドウ種子エキス、プロポリス、ヘチマエキス、ベニバナエキス、ペパーミントエキス、ボダイジュエキス、ボタンエキス、ホップエキス、マイカイカエキス、マツエキス、マロニエエキス、ミズバショウエキス、ムクロジエキス、メリッサエキス、モズクエキス、モモエキス、ヤグルマギクエキス、ユーカリエキス、ユキノシタエキス、ユズエキス、ユリエキス、ヨクイニンエキス、ヨモギエキス、ラベンダーエキス、緑茶エキス、卵殻膜エキス、リンゴエキス、ルイボス茶エキス、レイシエキス、レタスエキス、レモンエキス、レンギョウエキス、レンゲソウエキス、ローズエキス、ローズマリーエキス、ローマカミツレエキス、ローヤルゼリーエキス、ワレモコウエキス等のエキスが好ましいものとして挙げられる。 Plant / animal / microbe extracts include iris extract, ashitaba extract, asunalo extract, asparagus extract, avocado extract, achacha extract, almond extract, altea extract, arnica extract, aloe extract, apricot extract, apricot kernel extract, ginkgo biloba extract , Carrot extract, fennel extract, turmeric extract, oolong tea extract, walrus extract, ages extract, echinacea leaf extract, enmeo extract, peony extract, duckweed extract, lauren extract, barley extract, ginseng extract, hypericum extract, licorice extract, Onionis extract, Dutch mustard extract, orange extract, dried seawater, seaweed extract, oyster leaf extract, oyster extract, hydrolyzed elastin, hydrolyzed wheat powder, water Denatured silk, cocoon extract, chamomile extract, oil-soluble chamomile extract, carrot extract, kawarayomigi extract, oat extract, calcade extract, licorice extract, oil-soluble licorice extract, kiwi extract, kiou extract, jellyfish extract, quina extract, cucumber extract, giraffe leaf extract , Guanosine, guava extract, kudin extract, gardenia extract, kumazasa extract, clara extract, walnut extract, chestnut extract, grapefruit extract, clematis extract, black rice extract, brown sugar extract, black vinegar, chlorella extract, mulberry extract, gentian extract, gentian pepper extract, Black tea extract, yeast extract, kokuboku extract, coffee extract, burdock extract, rice extract, rice fermented extract, rice bran fermented extract, rice germ oil, comfrey exhaust Collagen extract Citrus extract, jatoba extract, peonies extract, ginger cucumber extract, ginger root extract, white birch extract, white jellyfish extract, horsetail extract, stevia extract, stevia fermented product, Nishikawa willow extract, Atlantic kizuta extract, hawthorn extract, elderberry extract, yarrow Extract, mint extract, sage extract, mallow extract, nematode extract, assembly extract, Sakuhakuhi extract, Diou extract, Soybean extract, tiso extract, thyme extract, dandelion extract, lichen extract, tea extract, clove extract, chigaya extract, chimpi extract, tea tree oil, strawberry tea extract, red pepper extract, suzuki extract, eucalyptus extract, tonin extract, spruce extract, dokudami extract, tomato Extract, natto extract, carrot extract, garlic extract, wild rose extract, hibiscus extract, bacmond extract, lotus extract, parsley extract, birch extract, honey, hamamelis extract, parietalia extract, hyacinth extract, bisabolol, cypress extract, bifidobacteria extract, Loquat extract, dandelion extract, burdock extract, bukkuri extract, butcher bloom extract, grape extract, grape seed extract, propolis, loofah , Safflower extract, peppermint extract, body extract, button extract, hop extract, squid extract, pine extract, maroni extract, citrus extract, mugwort extract, melissa extract, mozuku extract, peach extract, cornflower extract, eucalyptus extract, yukinoshita extract, yuzu extract, Lily extract, Yokuinin extract, Artemisia extract, Lavender extract, Green tea extract, Egg shell membrane extract, Apple extract, Rooibos tea extract, Ganoderma extract, Lettuce extract, Lemon extract, Forsythia extract, Forsythia extract, Rose extract, Rosemary extract, Roman chamomile extract Extracts such as royal jelly extract and walnut extract are preferred.

 鎮痒剤としては、塩酸ジフェンヒドラミン、マレイン酸クロルフェニラミン、カンフル、サブスタンス-P阻害剤等が挙げられる。 Examples of antipruritic agents include diphenhydramine hydrochloride, chlorpheniramine maleate, camphor, substance-P inhibitor, and the like.

 角質剥離・溶解剤としては、サリチル酸、イオウ、レゾルシン、硫化セレン、ピリドキシン等が挙げられる。 Examples of the exfoliating / dissolving agent include salicylic acid, sulfur, resorcin, selenium sulfide, pyridoxine and the like.

 制汗剤としては、クロルヒドロキシアルミニウム、塩化アルミニウム、酸化亜鉛、パラフェノールスルホン酸亜鉛等が挙げられる。 Examples of antiperspirants include chlorohydroxyaluminum, aluminum chloride, zinc oxide, zinc paraphenol sulfonate, and the like.

 清涼剤としては、メントール、サリチル酸メチル等が挙げられる。 Examples of the refreshing agent include menthol and methyl salicylate.

 収れん剤としては、クエン酸、酒石酸、乳酸、硫酸アルミニウム・カリウム、タンニン酸等が挙げられる。 Examples of astringents include citric acid, tartaric acid, lactic acid, aluminum sulfate / potassium, and tannic acid.

 酵素類としては、スーパーオキサイドディスムターゼ、カタラーゼ、塩化リゾチーム、リパーゼ、パパイン、パンクレアチン、プロテアーゼ等が挙げられる。 Enzymes include superoxide dismutase, catalase, lysozyme chloride, lipase, papain, pancreatin, protease, and the like.

 核酸類としては、リボ核酸及びその塩、デオキシリボ核酸及びその塩、アデノシン三リン酸二ナトリウムが好ましいものとして挙げられる。 Preferred nucleic acids include ribonucleic acid and its salts, deoxyribonucleic acid and its salts, and adenosine triphosphate disodium.

 香料としては、アセチルセドレン、アミルシンナムアルデヒド、アリルアミルグリコレート、β-イオノン、イソイースーパー、イソブチルキノリン、イリス油、イロン、インドール、イランイラン油、ウンデカナール、ウンデセナール、γ-ウンデカラクトン、エストラゴール、オイゲノール、オークモス、オポポナックスレジノイド、オレンジ油、オイゲノール、オーランチオール、ガラクソリッド、カルバクロール、L-カルボン、カンフル、キャノン、キャロットシード油、クローブ油、ケイヒ酸メチル、ゲラニオール、ゲラニルニトリル、酢酸イソボルニル、酢酸ゲラニル、酢酸ジメチルベンジルカルビニル、酢酸スチラリル、酢酸セドリル、酢酸テレピネル、酢酸p-t-ブチルシクロヘキシル、酢酸ベチベリル、酢酸ベンジル、酢酸リナリル、サリチル酸イソペンチル、サリチル酸ベンジル、サンダルウッド油、サンタロール、シクラメンアルデヒド、シクロペンタデカノリド、ジヒドロジャスモン酸メチル、ジヒドロミルセノール、ジャスミンアブソリュート、ジャスミンラクトン、cis-ジャスモン、シトラール、シトロネノール、シトロネラール、シナモンバーク油、1,8-シネオール、シンナムアルデヒド、スチラックスレジノイド、セダーウッド油、セドレン、セドロール、セロリシード油、タイム油、ダマスコン、ダマセノン、チモール、チュベローズアブソリュート、デカナール、デカラクトン、テルピネオール、γ-テルピネン、トリプラール、ネロール、ノナナール、2,6-ノナジエノール、ノナラクトン、パチョリアルコール、バニラアブソリュート、バニリン、バジル油、パチョリ油、ヒドロキシシトロネラール、α-ピネン、ピペリトン、フェネチルアルコール、フェニルアセトアルデヒド、プチグレン油、ヘキシルシンナムアルデヒド、cis-3-ヘキセノール、ペルーバルサム、ベチバー油、ベチベロール、ペパーミント油、ペパー油、ヘリオトロピン、ベルガモット油、ベンジルベンゾエート、ボルネオール、ミルレジノイド、ムスクケトン、メチルノニルアセトアルデヒド、γ-メチルヨノン、メントール、L-メントール、L-メントン、ユーカリ油、β-ヨノン、ライム油、ラベンダー油、D-リモネン、リナロール、リラール、リリアール、レモン油、ローズアブソリュート、ローズオキシド、ローズ油、ローズマリー油、各種精油等の合成香料及び天然香料並びに各種調合香料が好ましいものとして挙げられる。 As perfumes, acetyl cedrene, amylcinnamaldehyde, allyl amyl glycolate, β-ionone, iso-Esuper, isobutyl quinoline, Iris oil, Iron, indole, ylang ylang oil, undecanal, undecenal, γ-undecalactone, Estragole, eugenol, oak moss, opoponax resinoid, orange oil, eugenol, auranthiol, galac solid, carvacrol, L-carvone, camphor, cannon, carrot seed oil, clove oil, methyl cinnamate, geraniol, geranyl nitrile , Isobornyl acetate, geranyl acetate, dimethylbenzyl carvinyl acetate, styraryl acetate, cedolyl acetate, terpinel acetate, pt-butylcyclohexyl acetate, vetiberyl acetate, benzyl acetate Linalyl acetate, isopentyl salicylate, benzyl salicylate, sandalwood oil, santalol, cyclamenaldehyde, cyclopentadecanolide, methyl dihydrojasmonate, dihydromyrsenol, jasmine absolute, jasmine lactone, cis-jasmon, citral, citronenol, Citronellal, cinnamon bark oil, 1,8-cineole, cinnamaldehyde, stylus resinoid, cedarwood oil, cedrene, cedrol, celery seed oil, thyme oil, damascon, damasenone, thymol, tuberose absolute, decanal, decalactone, terpineol, γ- Terpinene, triplar, nerol, nonanal, 2,6-nonadienol, nonalactone, patchouli alcohol, vanilla Solute, vanillin, basil oil, patchouli oil, hydroxycitronellal, α-pinene, piperitone, phenethyl alcohol, phenylacetaldehyde, petitglen oil, hexylcinnamaldehyde, cis-3-hexenol, perubalsum, vetiver oil, vetiverol, peppermint oil , Pepper oil, heliotropin, bergamot oil, benzylbenzoate, borneol, milresinoid, musk ketone, methylnonylacetaldehyde, γ-methylyonone, menthol, L-menthol, L-menton, eucalyptus oil, β-yonone, lime oil, lavender oil Synthetic and natural flavors such as D-limonene, linalool, linal, rillial, lemon oil, rose absolute, rose oxide, rose oil, rosemary oil, and various essential oils In addition, various kinds of blended fragrances are preferable.

 色素・着色剤・染料としては、褐色201号、黒色401号、紫色201号、紫色401号、青色1号、青色2号、青色201号、青色202号、青色203号、青色204号、青色205号、青色403号、青色404号、緑色201号、緑色202号、緑色204号、緑色205号、緑色3号、緑色401号、緑色402号、赤色102号、赤色104-1号、赤色105-1号、赤色106号、赤色2号、赤色201号、赤色202号、赤色203号、赤色204号、赤色205号、赤色206号、赤色207号、赤色208号、赤色213号、赤色214号、赤色215号、赤色218号、赤色219号、赤色220号、赤色221号、赤色223号、赤色225号、赤色226号、赤色227号、赤色228号、赤色230-1号、赤色230-2号、赤色231号、赤色232号、赤色3号、赤色401号、赤色404号、赤色405号、赤色501号、赤色502号、赤色503号、赤色504号、赤色505号、赤色506号、橙色201号、橙色203号、橙色204号、橙色205号、橙色206号、橙色207号、橙色401号、橙色402号、橙色403号、黄色201号、黄色202-1号、黄色202-2号、黄色203号、黄色204号、黄色205号、黄色4号、黄色401号、黄色402号、黄色403-1号、黄色404号、黄色405号、黄色406号、黄色407号、黄色5号等の法定色素;Acid Red 14等のその他酸性染料;Arianor Sienna Brown、Arianor Madder Red、Arianor Steel Blue、Arianor Straw Yellow等の塩基染料;HC Yellow 2、HC Yellow 5、HC Red 3、4-hydoxypropylamino-3-nitrophenol、N,N’-bis(2-hydroxyethyl)-2-nitro-p-phenylenediamine、HC Blue 2、Basic Blue 26等のニトロ染料;分散染料;アスタキサンチン、アリザリン等のアントラキノン類、アントシアニジン、β-カロチン、カテナール、カプサンチン、カルコン、カルサミン、クエルセチン、クロシン、クロロフィル、クルクミン、コチニール、シコニン等のナフトキノン類、ビキシン、フラボン類、ベタシアニジン、ヘナ、ヘモグロビン、リコピン、リボフラビン、ルチン等の天然色素・染料;p-フェニレンジアミン、トルエン-2,5-ジアミン、o-,m-,若しくはp-アミノフェノール、m-フェニレンジアミン、5-アミノ-2-メチルフェノール、レゾルシン、1-ナフトール、2,6-ジアミノピリジン等及びその塩等の酸化染料中間体及びカップラー;インドリン等の自動酸化型染料;ジヒドロキシアセトンが好ましいものとして挙げられる。 As pigments / colorants / dyes, brown 201, black 401, purple 201, purple 401, blue 1, blue 2, blue 201, blue 202, blue 203, blue 204, blue 205, Blue 403, Blue 404, Green 201, Green 202, Green 204, Green 205, Green 3, Green 401, Green 402, Red 102, Red 104-1, Red 105-1, Red 106, Red 2, Red 201, Red 202, Red 203, Red 204, Red 205, Red 206, Red 207, Red 208, Red 213, Red 214, Red 215, Red 218, Red 219, Red 220, Red 221, Red 223, Red 225, Red 226, Red 227, Red 228, Red 230-1 Red 230-2, Red 231, Red 232, Red 3, Red 401, Red 404, Red 404, Red 405, Red 501, Red 502, Red 503, Red 504, Red 505 Red No. 506, Orange No. 201, Orange No. 203, Orange No. 204, Orange No. 205, Orange No. 206, Orange No. 207, Orange No. 401, Orange No. 402, Orange No. 403, Yellow No. 201, Yellow No. 202-1 Yellow 202-2, Yellow 203, Yellow 204, Yellow 205, Yellow 4, Yellow 401, Yellow 402, Yellow 403-1, Yellow 404, Yellow 405, Yellow 406, Yellow Legal pigments such as No. 407 and Yellow No. 5; Other acidic dyes such as Acid Red 14; Aryanor Sienna Brown, Aryanor Madder Red, Ari Basic dyes such as nor Steel Blue, Aryanor Straw Yellow, etc .; HC Yellow 2, HC Yellow 5, HC Red 3, 4-hydroxypropylamino-3-Ntrobisphenol, N, N'-bis (2-hydroxyethyl-2) Nitro dyes such as phenylenediamine, HC Blue 2, Basic Blue 26; disperse dyes; anthraquinones such as astaxanthin and alizarin, anthocyanidins, β-carotene, catenal, capsanthin, chalcone, calsamine, quercetin, crocin, chlorophyll, curcumin, cochineal, cochineal Naphthoquinones such as bixin, flavones, betacyanidine, henna, hemoglobin Natural pigments and dyes such as glycine, lycopene, riboflavin and rutin; p-phenylenediamine, toluene-2,5-diamine, o-, m-, or p-aminophenol, m-phenylenediamine, 5-amino-2- Preferable examples include oxidative dye intermediates and couplers such as methylphenol, resorcin, 1-naphthol, 2,6-diaminopyridine, and salts thereof; auto-oxidative dyes such as indoline; and dihydroxyacetone.

 消炎剤・抗炎症剤としては、グリチルリチン酸及びその誘導体、グリチルレチン酸誘導体、サリチル酸誘導体、ヒノキチオール、グアイアズレン、アラントイン、インドメタシン、ケトプロフェン、イブプロフェン、ジクロフェナク、ロキソプロフェン、セレコシキブ、インフリキシマブ、エタネルセプト、酸化亜鉛、酢酸ヒドロコルチゾン、プレドニゾン、塩酸ジフェドラミン、マレイン酸クロルフェニラミン;桃葉エキス、蓬葉エキス等の植物エキスが好ましいものとして挙げられる。 Anti-inflammatory / anti-inflammatory agents include glycyrrhizic acid and its derivatives, glycyrrhetinic acid derivatives, salicylic acid derivatives, hinokitiol, guaiazulene, allantoin, indomethacin, ketoprofen, ibuprofen, diclofenac, loxoprofen, celecoxib, infliximab, etanercept, zinc oxide, hydroacetic acid, zinc acetate, Preferred examples include prednisone, diphedramine hydrochloride, chlorpheniramine maleate; and plant extracts such as peach leaf extract and persimmon leaf extract.

 抗喘息、抗慢性閉塞性肺疾患、抗アレルギー、免疫調整剤としては、アミノフィリン、テオフィリン類、ステロイド類(フルチカゾン、ベクロメタゾンなど)、ロイコトリエン拮抗薬類、トロンボキサン阻害薬類、インタール、β2刺激薬類(フォルモテロール、サルメテロール、アルブテロール、ツロブテロール、クレンブテロール、エピネフリンなど)、チオトロピウム、イプラトロピウム、デキストロメトルファン、ジメモルファン、ブロムヘキシン、トラニラスト、ケトチフェン、アゼラスチン、セチリジン、クロルフェニラミン、メキタジン、タクロリムス、シクロスポリン、シロリムス、メトトレキサート、サイトカイン調整剤類、インターフェロン、オマリズマブ、タンパク/抗体製剤が好ましいものとして挙げられる。 Anti-asthma, anti-chronic obstructive pulmonary disease, anti-allergy, immunomodulators include aminophylline, theophylline, steroids (fluticasone, beclomethasone, etc.), leukotriene antagonists, thromboxane inhibitors, intal, β2-stimulant (Formoterol, salmeterol, albuterol, tulobuterol, clenbuterol, epinephrine, etc.), tiotropium, ipratropium, dextromethorphan, dimemorphan, bromhexine, tranilast, ketotifen, azelastine, cetirizine, chlorpheniramine, polyquitolsine, Preferred examples include cytokine regulators, interferons, omalizumab, and protein / antibody preparations.

 抗感染症剤、抗真菌剤としては、オセルタミビルとザナミビル、イトラコナゾールが好ましいものとして挙げられる。これらの他、化粧品原料基準、化粧品種別配合成分規格、日本化粧品工業連合会成分表示名称リスト、INCI辞書(The International Cosmetic Ingredient Dictionaryand Handbook)、医薬部外品原料規格、日本薬局方、医薬品添加物規格、食品添加物公定書等に記載されている成分、及び、国際特許分類IPCがA61K7及びA61K8の分類に属する日本国及び諸外国特許公報及び特許公開公報(公表公報・再公表を含む)に記載されている成分等、公知の化粧料成分、医薬品成分、食品成分などを、公知の組み合わせ及び配合比・配合量で含有させることが可能である。 Preferred examples of the anti-infective and antifungal agents include oseltamivir, zanamivir, and itraconazole. In addition to these, cosmetic raw material standards, cosmetic ingredient-specific combination ingredient standards, Japan Cosmetic Industry Association ingredient display name list, INCI dictionary (The International Cosmetic Ingredients and Handbooks), quasi-drug ingredients standards, Japanese pharmacopoeia, pharmaceutical additive standards Ingredients listed in the Food Addendum, etc., and the international patent classification IPC described in Japan and other foreign patent gazettes and patent publications (including publications and republications) belonging to the A61K7 and A61K8 classifications It is possible to contain known cosmetic ingredients, pharmaceutical ingredients, food ingredients, etc., in known combinations, blending ratios and blending amounts.

[スティック状基材の製造方法]
 本発明のスティック状基材は、前記式(1)乃至式(3)で表される化合物又はその薬学的に使用可能な塩のうちの少なくとも一種からなる脂質ペプチド化合物と界面活性剤及び水、1,2-アルカンジオール又は1,3-アルカンジオール、高級アルコール、増粘剤及び所望により油性基剤や、顔料、その他添加剤とを用いて、加熱しながら混合、撹拌した後、静置放冷することによって製造され得る。
[Production method of stick-like substrate]
The stick-like substrate of the present invention comprises a lipid peptide compound comprising at least one of the compounds represented by the formulas (1) to (3) or a pharmaceutically usable salt thereof, a surfactant and water, 1,2-alkanediol or 1,3-alkanediol, higher alcohol, thickener and, if necessary, an oily base, pigment, and other additives, mixed and stirred with heating, then allowed to stand It can be manufactured by cooling.

 例えば本発明のスティック状基材は、一例として、下記工程により製造される。
a)上記脂質ペプチド化合物と、界面活性剤と、水を配合し、加熱して溶解液又は分散液を調製する工程、
b)上記溶解液又は分散液を水に添加し、室温以上100℃未満の温度で加熱する工程、
c)前記加熱工程における温度よりも低い温度になるまで撹拌しながら冷却し、その後静置放冷し、ゲル状の固形物(スティック状基材)を形成する工程。
 ここで、1,2-アルカンジオール又は1,3-アルカンジオール、油性基剤、高級アルコール、増粘剤及び顔料やその他添加剤は、a)工程において溶解液又は分散液の調製工程において添加してもよいし、b)工程において溶解液又は分散液を添加する水に予め添加していてもよい。
 また得られたスティック状基材の総質量に対して、水は20質量%以上99質量%未満であることが好ましい。
 また得られた溶解液又は分散液の総質量に対して、水は30質量%以上80質量%未満であることが好ましい。
For example, the stick-shaped substrate of the present invention is produced by the following process as an example.
a) a step of blending the above-mentioned lipid peptide compound, a surfactant and water, and preparing a solution or dispersion by heating;
b) adding the solution or dispersion to water and heating at a temperature of room temperature to less than 100 ° C .;
c) The process which cools with stirring until it becomes temperature lower than the temperature in the said heating process, and is left still standing to cool, and forms a gel-like solid substance (stick-shaped base material).
Here, 1,2-alkanediol or 1,3-alkanediol, oily base, higher alcohol, thickener, pigment and other additives are added in the step of preparing the solution or dispersion in step a). Alternatively, it may be added in advance to the water to which the solution or dispersion is added in step b).
Moreover, it is preferable that water is 20 mass% or more and less than 99 mass% with respect to the total mass of the obtained stick-shaped base material.
Moreover, it is preferable that water is 30 to 80 mass% with respect to the total mass of the obtained solution or dispersion.

 前記a)工程及びb)工程における加熱温度は好ましくは50℃乃至90℃、より好ましくは60℃乃至90℃、例えば80℃であり、加熱しながら撹拌を行うことが好ましい。この時の夫々の工程における加熱撹拌の時間は、用いる脂質ペプチド化合物や、界面活性剤ほかその他成分の種類、そしてそれらの配合量によって異なるが、通常5分から50分程度で溶解・分散可能である。
 a)、b)工程につづいて、液温がb)工程における温度よりも低い温度になるまで撹拌しながら冷却を行う(c)工程)。ここで冷却温度は例えば室温乃至80℃、室温乃至60℃、或いは室温乃至40℃程度である。
The heating temperature in the step a) and the step b) is preferably 50 ° C. to 90 ° C., more preferably 60 ° C. to 90 ° C., for example 80 ° C., and stirring is preferably performed while heating. The time of heating and stirring in each step at this time varies depending on the type of lipid peptide compound used, the surfactant and other components, and the blending amount thereof, but can usually be dissolved and dispersed in about 5 to 50 minutes. .
Following steps a) and b), cooling is performed with stirring until the liquid temperature is lower than the temperature in step b) (step c). Here, the cooling temperature is, for example, room temperature to 80 ° C., room temperature to 60 ° C., or room temperature to 40 ° C.

 また本発明のスティック状基材はプレミックスである水性組成物を製造した後、該プレミックスに他の配合成分を適宜添加して製造することもできる。
 例えば、プレミックスを経たスティック状基材の製造方法としては、以下が挙げられる。
1)プレミックスを調製する工程
1-1)界面活性剤及び水と、前記式(1)乃至式(3)で表される化合物又はその薬学的に使用可能な塩のうちの少なくとも一種からなる脂質ペプチド型化合物とを含む混合系を室温以上100℃未満の温度に加熱する加熱工程、
1-2)続いて、加熱した前記混合系に、1,2-アルカンジオール又は1,3-アルカンジオール及びその他添加剤を適宜添加する工程、
1-3)前記溶解液又は分散液を冷却し、水性組成物(プレミックス)を得る調製工程、
2)プレミックスを用いてスティック状基材を製造する工程
2-1)室温以上100℃未満の温度に加熱された水相に、室温以上100℃未満の温度に加熱した上記水性組成物(プレミックス)を添加し、混合する、或いは、室温以上100℃未満の温度に加熱した上記水性組成物(プレミックス)に、室温以上100℃未満の温度に加熱された水相を添加し、混合する、混合工程、
2-2)前記混合工程で得られた混合物を冷却し、スティック状基材(ゲル)を形成させる冷却工程。
 上記2-1)工程における水相は水を含み、さらに油性基剤、高級アルコール、増粘剤、顔料を含み得、また1,2-アルカンジオール又は1,3-アルカンジオール、及びその他添加剤を含んでいてもよい。また、2-1)において水性組成物(プレミックス)に顔料やその他添加剤を混合した後、水相とあわせてもよい。
 さらに、前記混合工程において、更に薬剤の溶解液を添加することにより、薬剤を添加したスティック状基材(製剤)を製造することもできる。
Moreover, after manufacturing the aqueous composition which is a premix, the stick-shaped base material of this invention can also be manufactured by adding suitably another compounding component to this premix.
For example, the following is mentioned as a manufacturing method of the stick-shaped base material which passed through the premix.
1) Step of preparing a premix 1-1) A surfactant and water, and at least one of the compounds represented by the formulas (1) to (3) or a pharmaceutically usable salt thereof. A heating step of heating a mixed system containing the lipid peptide type compound to a temperature of room temperature to less than 100 ° C .;
1-2) Subsequently, a step of appropriately adding 1,2-alkanediol or 1,3-alkanediol and other additives to the heated mixed system,
1-3) A preparation step of cooling the solution or dispersion to obtain an aqueous composition (premix),
2) Step of producing stick-like substrate using premix 2-1) The aqueous composition (pre-heated) heated to a temperature of room temperature to less than 100 ° C. in an aqueous phase heated to a temperature of room temperature to less than 100 ° C. (Mix) is added and mixed, or an aqueous phase heated to a temperature of room temperature to less than 100 ° C. is added to and mixed with the aqueous composition (premix) heated to a temperature of room temperature to less than 100 ° C. , Mixing process,
2-2) A cooling step in which the mixture obtained in the mixing step is cooled to form a stick-like substrate (gel).
The aqueous phase in the step 2-1) contains water, and may further contain an oily base, a higher alcohol, a thickener, a pigment, and 1,2-alkanediol or 1,3-alkanediol, and other additives. May be included. Further, in 2-1), a pigment and other additives may be mixed with the aqueous composition (premix) and then combined with the aqueous phase.
Furthermore, in the said mixing process, the stick-shaped base material (formulation) which added the chemical | medical agent can also be manufactured by adding the chemical | medical agent solution.

 前記1-1)工程及び1-2)工程における、混合系(及び水性組成物)の加熱温度は好ましくは50℃乃至90℃、より好ましくは60℃乃至90℃、例えば70℃、或いは80℃である。本工程は撹拌しながら実施することが好ましい。この時の各工程における加熱(撹拌)の時間は、水性組成物に含まれる脂質ペプチド化合物や界面活性剤ほかその他成分の種類、そしてそれらの配合量によって異なるが、通常5分から50分程度である。本工程により水性組成物を均一に溶解させた状態とする。
 また、前記1-3)工程における冷却温度は、例えば室温乃至80℃、室温乃至60℃、或いは室温乃至40℃程度である。この工程において、撹拌しながら冷却し、その後撹拌を停止して、静置することがより好ましい。
 なお1)工程により得られた水性組成物(プレミックス)の総質量に対して、水は30質量%以上80質量%未満であることが好ましい。
The heating temperature of the mixed system (and aqueous composition) in the steps 1-1) and 1-2) is preferably 50 ° C. to 90 ° C., more preferably 60 ° C. to 90 ° C., for example 70 ° C., or 80 ° C. It is. This step is preferably carried out with stirring. The time of heating (stirring) in each step at this time is usually about 5 to 50 minutes, although it varies depending on the type of lipid peptide compound, surfactant and other components contained in the aqueous composition, and their blending amount. . By this step, the aqueous composition is uniformly dissolved.
The cooling temperature in the step 1-3) is, for example, room temperature to 80 ° C., room temperature to 60 ° C., or room temperature to 40 ° C. In this step, it is more preferable to cool with stirring, then stop stirring and leave to stand.
In addition, it is preferable that water is 30 mass% or more and less than 80 mass% with respect to the total mass of the aqueous composition (premix) obtained by the 1) process.

 前記2-1)工程における、水相及び水性組成物(プレミックス)の加熱温度は好ましくは50℃乃至90℃、より好ましくは60℃乃至90℃、例えば70℃、或いは80℃、あるいは90℃である。水相の加熱は、特に油性基剤などその他成分を含むことから撹拌しながら行うことが好ましく、含有する成分が均一に溶解・分散するまで、通常5分から50分程度、加熱(撹拌)を実施することが好ましい。なお、水相の加熱温度は、上記水性組成物(プレミックス)の加熱温度と同じ温度としてもよい。 In the step 2-1), the heating temperature of the aqueous phase and the aqueous composition (premix) is preferably 50 ° C. to 90 ° C., more preferably 60 ° C. to 90 ° C., such as 70 ° C., or 80 ° C., or 90 ° C. It is. The aqueous phase is preferably heated with stirring because it contains other components such as an oily base. Heating (stirring) is usually carried out for about 5 to 50 minutes until the contained components are uniformly dissolved and dispersed. It is preferable to do. The heating temperature of the aqueous phase may be the same as the heating temperature of the aqueous composition (premix).

 続いて、前記2-2)工程において、前工程で得られた混合物を冷却し、ゲル状の固形物(スティック状基材)を形成させるが、このとき、撹拌しながら冷却してもよい。撹拌しながら冷却する場合、例えば冷却温度が室温ないし80℃、室温ないし60℃、例えば60℃程度となるまで撹拌を実施した後、その後撹拌を停止して静置し冷却することが好ましい。特に50℃以下では撹拌を停止し、静置して冷却することが好ましい。 Subsequently, in the step 2-2), the mixture obtained in the previous step is cooled to form a gel-like solid (stick-like substrate). At this time, the mixture may be cooled with stirring. In the case of cooling with stirring, it is preferable to carry out stirring until the cooling temperature reaches room temperature to 80 ° C., room temperature to 60 ° C., for example, about 60 ° C., and then stop the stirring and leave it to cool. In particular, at 50 ° C. or less, it is preferable to stop stirring and leave it to cool.

 こうして水性組成物(プレミックス)を用いた得られたスティック状基材においても、水の配合量は、スティック状基材の総質量に対して、20質量%以上99質量%未満であることが好ましい。 Even in the stick-shaped substrate thus obtained using the aqueous composition (premix), the blending amount of water may be 20% by mass or more and less than 99% by mass with respect to the total mass of the stick-shaped substrate. preferable.

 以下、本発明を実施例及び試験例を例に挙げて詳しく説明するが、本発明がこれらの例に限定されるものではない。 Hereinafter, the present invention will be described in detail by way of examples and test examples, but the present invention is not limited to these examples.

[合成例1:脂質ペプチド(N-パルミトイル-Gly-His)の合成]
 本実施例において用いた脂質ペプチド型化合物を以下に示す方法で合成した。
 500mLの4つ口フラスコに、ヒスチジン14.2g(91.6mmol)、N-パルミトイル-Gly-メチル30.0g(91.6mmol)、トルエン300gを投入し、塩基であるナトリウムメトキサイド 28%メタノール溶液35.3g(183.2mmol)を加え、油浴で60℃に加熱し1時間撹拌を続けた。その後、油浴を外し、25℃まで放冷し、この溶液をアセトン600gで再沈殿させ、ろ取した。ここで得られた固体を、水600gとメタノール750gの混合溶液に溶解し、ここに6規定塩酸30.5ml(183.2mmol)を加えて中和し固体を析出させ、ろ過した。次に、得られた固体をテトラヒドロフラン120gと水30gの混合溶液に60℃で溶解させ、酢酸エチル150gを加え、60℃から30℃まで冷却した。その後、析出した固体をろ過した。さらに得られた固体を、テトラヒドロフラン120gとアセトニトリル60g溶剤中に溶解し、60℃に加熱し、1時間撹拌した後に冷却し、ろ過した。ここで得られた固体を水120gで洗浄し、ろ過後に減圧乾燥を行いN-パルミトイル-Gly-Hisフリー体(以下、単にPal-GHとも称する)の白色の結晶、26.9g(収率65%)を得た。
[Synthesis Example 1: Synthesis of lipid peptide (N-palmitoyl-Gly-His)]
The lipid peptide type compound used in this example was synthesized by the following method.
A 500 mL four-necked flask was charged with 14.2 g (91.6 mmol) of histidine, 30.0 g (91.6 mmol) of N-palmitoyl-Gly-methyl and 300 g of toluene, and a sodium methoxide 28% methanol solution as a base. 35.3 g (183.2 mmol) was added, and the mixture was heated to 60 ° C. in an oil bath and stirred for 1 hour. Thereafter, the oil bath was removed and the mixture was allowed to cool to 25 ° C. This solution was reprecipitated with 600 g of acetone and collected by filtration. The solid obtained here was dissolved in a mixed solution of 600 g of water and 750 g of methanol, and 30.5 ml (183.2 mmol) of 6N hydrochloric acid was added thereto for neutralization to precipitate a solid, followed by filtration. Next, the obtained solid was dissolved in a mixed solution of 120 g of tetrahydrofuran and 30 g of water at 60 ° C., 150 g of ethyl acetate was added, and the mixture was cooled from 60 ° C. to 30 ° C. Thereafter, the precipitated solid was filtered. Further, the obtained solid was dissolved in 120 g of tetrahydrofuran and 60 g of acetonitrile, heated to 60 ° C., stirred for 1 hour, cooled, and filtered. The solid obtained here was washed with 120 g of water, dried under reduced pressure after filtration, and 26.9 g (yield 65) of white crystals of N-palmitoyl-Gly-His free form (hereinafter also simply referred to as “Pal-GH”). %).

[実施例1乃至実施例4、比較例1乃至比較例3]
(プレミックスの調製方法)
 下記表1に従って、各成分をサンプル管No.5に秤量した。秤量した組成物を70℃以上に加熱し、均一に溶解させる事でプレミックスを調製した。

Figure JPOXMLDOC01-appb-T000010
[Examples 1 to 4 and Comparative Examples 1 to 3]
(Premix preparation method)
According to Table 1 below, each component was sample tube No. Weighed to 5. The pre-mix was prepared by heating the weighed composition to 70 ° C. or higher and dissolving it uniformly.
Figure JPOXMLDOC01-appb-T000010

(スティック状基材の調製法)
 下記表2に従って、A相の各成分あるいは前述のプレミックスをサンプル管No.5に秤量した。秤量したA相を70℃以上に加熱し、均一に溶解させた。一方、別のサンプル管No.5にB相である水5.0gを秤量し、70℃以上に加熱した。その後、A相をB相に添加し、加熱した状態で混合し約30秒程度撹拌した後、静置放冷を行った。
(Preparation method of stick-like substrate)
In accordance with the following Table 2, each component of the A phase or the above-mentioned premix is sample tube No. Weighed to 5. The weighed phase A was heated to 70 ° C. or higher and dissolved uniformly. On the other hand, another sample tube No. 5 was weighed 5.0 g of water as B phase and heated to 70 ° C. or higher. Thereafter, the A phase was added to the B phase, mixed in a heated state and stirred for about 30 seconds, and then allowed to stand and cool.

(破断強度測定方法)
 YAMADEN RHEONER II CREEP METER RE2-33005B((株)山電)にて、測定速度:0.5mm/秒、測定歪率:20%、格納ピッチ:0.10秒、治具:30349-3を用いて破断強度測定を行った。
 得られた結果を表2に示す。

Figure JPOXMLDOC01-appb-T000011
(Break strength measurement method)
Using YAMADEN RHEONER II CREEP METER RE2-30005B (Sanden Co., Ltd.), measurement speed: 0.5 mm / second, measurement distortion: 20%, storage pitch: 0.10 second, jig: 30349-3 The breaking strength was measured.
The obtained results are shown in Table 2.
Figure JPOXMLDOC01-appb-T000011

 表1に示すように、実施例1乃至実施例4の皮膚外用固形基材は破断強度:0.4~1.3×105Paを有し、特にスティック状の基材として求められる強度を有していた。 As shown in Table 1, the solid base materials for external application of Examples 1 to 4 have a breaking strength: 0.4 to 1.3 × 10 5 Pa, and have the strength required particularly as a stick-shaped base material. Had.

Claims (8)

ベタイン系化合物及びエチレングリコールアルキルエーテルからなる群より選択される1種以上の界面活性剤と、
水と、
下記式(1)乃至式(3)で表される化合物又はその薬学的に使用可能な塩のうちの少なくとも一種からなる脂質ペプチド型化合物と、
炭素原子数8乃至30の少なくとも一種の飽和又は不飽和の一価アルコールと、
アルギン酸誘導体及びカラギーナンからなる群より選択される1種以上の増粘剤、
を含む、スティック状基材。
Figure JPOXMLDOC01-appb-C000001
(式中、R1は炭素原子数9乃至23の脂肪族基を表し、R2は水素原子、又は炭素原子数1若しくは2の分枝鎖を有し得る炭素原子数1乃至4のアルキル基を表し、R3は-(CH2n-X基を表し、nは1乃至4の数を表し、Xはアミノ基、グアニジノ基、-CONH2基、又は窒素原子を1乃至3個有し得る5員環若しくは6員環又は5員環と6員環から構成される縮合複素環を表す。)
Figure JPOXMLDOC01-appb-C000002
(式中、R4は炭素原子数9乃至23の脂肪族基を表し、R5乃至R7はそれぞれ独立して水素原子、炭素原子数1若しくは2の分枝鎖を有し得る炭素原子数1乃至4のアルキル基、又は-(CH2n-X基を表し、nは1乃至4の数を表し、Xはアミノ基、グアニジノ基、-CONH2基、又は窒素原子を1乃至3個有し得る5員環若しくは6員環又は5員環と6員環から構成される縮合複素環を表す。)
Figure JPOXMLDOC01-appb-C000003
(式中、R8は炭素原子数9乃至23の脂肪族基を表し、R9乃至R12はそれぞれ独立して水素原子、炭素原子数1若しくは2の分枝鎖を有し得る炭素原子数1乃至4のアルキル基、又は-(CH2n-X基を表し、nは1乃至4の数を表し、Xはアミノ基、グアニジノ基、-CONH2基、又は窒素原子を1乃至3個有し得る5員環若しくは6員環又は5員環と6員環から構成される縮合複素環を表す。)
One or more surfactants selected from the group consisting of betaine compounds and ethylene glycol alkyl ethers;
water and,
A lipid peptide type compound comprising at least one of the compounds represented by the following formulas (1) to (3) or a pharmaceutically usable salt thereof;
At least one saturated or unsaturated monohydric alcohol having 8 to 30 carbon atoms;
One or more thickeners selected from the group consisting of alginic acid derivatives and carrageenan,
A stick-like substrate.
Figure JPOXMLDOC01-appb-C000001
(In the formula, R 1 represents an aliphatic group having 9 to 23 carbon atoms, and R 2 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms which may have a branched chain having 1 or 2 carbon atoms. R 3 represents a — (CH 2 ) n —X group, n represents a number of 1 to 4, X represents an amino group, a guanidino group, a —CONH 2 group, or 1 to 3 nitrogen atoms. And represents a condensed heterocyclic ring composed of a 5-membered ring or a 6-membered ring or a 5-membered ring and a 6-membered ring.)
Figure JPOXMLDOC01-appb-C000002
(Wherein R 4 represents an aliphatic group having 9 to 23 carbon atoms, and R 5 to R 7 each independently represents a hydrogen atom or a carbon atom having a branched chain having 1 or 2 carbon atoms. 1 to 4 alkyl groups or — (CH 2 ) n —X group, n represents a number of 1 to 4, and X represents an amino group, a guanidino group, a —CONH 2 group, or a nitrogen atom of 1 to 3 This represents a 5-membered ring or 6-membered ring which may have one or a condensed heterocyclic ring composed of a 5-membered ring and a 6-membered ring.)
Figure JPOXMLDOC01-appb-C000003
(In the formula, R 8 represents an aliphatic group having 9 to 23 carbon atoms, and R 9 to R 12 each independently represents a hydrogen atom, or a carbon atom number that can have a branched chain having 1 or 2 carbon atoms. 1 to 4 alkyl, or - (CH 2) n represents an -X group, n represents a number from 1 to 4, X is an amino group, a guanidino group, -CONH 2 group, or a nitrogen atom and 1 to 3 This represents a 5-membered ring or 6-membered ring which may have one or a condensed heterocyclic ring composed of a 5-membered ring and a 6-membered ring.)
前記界面活性剤が、エチレングリコールアルキルエーテルである請求項1に記載のスティック状基材。 The stick-shaped substrate according to claim 1, wherein the surfactant is ethylene glycol alkyl ether. 更に、1,2-アルカンジオール又は1,3-アルカンジオールを含む、請求項1に記載のスティック状基材。 The stick-like substrate according to claim 1, further comprising 1,2-alkanediol or 1,3-alkanediol. 前記アルギン酸誘導体が、アルギン酸多価アルコールエステルである、請求項3に記載のスティック状基材。 The stick-shaped substrate according to claim 3, wherein the alginic acid derivative is an alginate polyhydric alcohol ester. 前記増粘剤が、スティック状基材の総質量に基いて0.1~1.0質量%の割合にて含まれてなる、請求項1乃至請求項4のうち何れか一項に記載のスティック状基材。 The thickener according to any one of claims 1 to 4, wherein the thickener is contained in a proportion of 0.1 to 1.0% by mass based on the total mass of the stick-like substrate. Stick-like substrate. 前記ベタイン系化合物が、硫酸型ベタインである、請求項3乃至請求項5のうち何れか一項に記載のスティック状基材。 The stick-shaped substrate according to any one of claims 3 to 5, wherein the betaine compound is a sulfuric acid type betaine. 前記一価アルコールが、ミリスチルアルコール、セタノール、ステアリルアルコール及びベヘニルアルコールからなる群から選択される1種以上の化合物である、請求項1乃至請求項6のうち何れか一項に記載のスティック状基材。 The stick-shaped substrate according to any one of claims 1 to 6, wherein the monohydric alcohol is one or more compounds selected from the group consisting of myristyl alcohol, cetanol, stearyl alcohol, and behenyl alcohol. . 前記脂質ペプチド型化合物が、スティック状基材の総質量に基いて0.1~2質量%の割合にて含まれてなる、請求項1乃至請求項7のうち何れか一項に記載のスティック状基材。 The stick according to any one of claims 1 to 7, wherein the lipid peptide-type compound is contained in a proportion of 0.1 to 2% by mass based on the total mass of the stick-like substrate. Substrate.
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