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WO2020004200A1 - COMPOSITION CONTENANT DU D-chiro-INOSITOL - Google Patents

COMPOSITION CONTENANT DU D-chiro-INOSITOL Download PDF

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Publication number
WO2020004200A1
WO2020004200A1 PCT/JP2019/024380 JP2019024380W WO2020004200A1 WO 2020004200 A1 WO2020004200 A1 WO 2020004200A1 JP 2019024380 W JP2019024380 W JP 2019024380W WO 2020004200 A1 WO2020004200 A1 WO 2020004200A1
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WO
WIPO (PCT)
Prior art keywords
acid
inositol
chiro
composition
salt
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/JP2019/024380
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English (en)
Japanese (ja)
Inventor
信哉 宅見
公輔 田中
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Kobayashi Pharmaceutical Co Ltd
Original Assignee
Kobayashi Pharmaceutical Co Ltd
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Filing date
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Publication of WO2020004200A1 publication Critical patent/WO2020004200A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/362—Polycarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/365—Hydroxycarboxylic acids; Ketocarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/41—Amines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/45—Derivatives containing from 2 to 10 oxyalkylene groups
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/86—Polyethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth

Definitions

  • the present invention relates to a composition comprising D-chiro-inositol.
  • the present invention also relates to an external preparation containing the composition.
  • Inositol (1,2,3,4,5,6-cyclohexanehexaol) has a structure in which one hydrogen atom on each carbon of cyclohexane is replaced by one hydroxy group, and is known as a vitamin-like active substance. I have. Inositol has nine types of stereoisomers depending on the combination of hydroxy group configurations.
  • Patent Document 1 discloses a hair restorer containing inositol as an active ingredient.
  • “inositol” used in the prior art refers to myo-inositol (cis-1,2,3,5-trans-4) as an additive for pharmaceuticals, quasi-drugs, cosmetics, and the like. , 6-cyclohexanehexaol) (see, for example, Non-Patent Documents 1 to 3).
  • the present inventors have found that among stereoisomers of inositol, chiro-inositol is a compound useful as a hair restorer (see Patent Document 2).
  • D-chiro-inositol is a water-soluble compound among the isomers of inositol.
  • D-chiro-inositol was found to be an inositol stereoisomer as well as in aqueous solution. It has been found that a precipitate tends to be formed.
  • D-chiro-inositol has very low solubility in solvents other than water, and tends to form precipitates more easily in a mixed solution containing a solvent other than water. Further, in particular, D-chiro-inositol tends to remarkably easily form a precipitate due to a change in storage temperature in a mixed solution containing a solvent other than water.
  • an object of the present invention is to provide a composition capable of suppressing the precipitation of D-chiro-inositol.
  • the present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, it has been found that D-chiro-inositol and an organic acid or a salt thereof have a surface activity in an aqueous monoalcohol solution having a specific concentration of 1 to 3 carbon atoms.
  • the composition containing the agent and the polyhydric alcohol is a composition capable of suppressing the precipitation of D-chiro-inositol when the concentration of the surfactant and the concentration of the polyhydric alcohol are each within a predetermined range.
  • the inventors have found that the present invention has been completed.
  • the present invention provides the following inventions.
  • [1] comprising D-chiro-inositol, an organic acid and / or a salt thereof, a surfactant, a monoalcohol having 1 to 3 carbon atoms, a polyhydric alcohol and water, The content of the monoalcohol having 1 to 3 carbon atoms is 40% by mass or more; The content of the surfactant is 1 to 10% by mass, A composition having a polyhydric alcohol content of 1 to 10% by mass.
  • [2] The composition according to [1], wherein the content of D-chiro-inositol is 0.001 to 20% by mass.
  • [3] containing an organic acid The composition according to [1] or [2], wherein the organic acid is a monocarboxylic acid or a polycarboxylic acid.
  • [4] containing a polycarboxylic acid The composition according to [3], wherein the polycarboxylic acid is citric acid or edetic acid.
  • [5] including a salt of an organic acid The composition according to any one of [1] to [4], wherein the salt is one or more selected from the group consisting of a sodium salt, a potassium salt, a calcium salt, and a magnesium salt.
  • the composition according to any one of [1] to [5] comprising an organic acid and a salt of the organic acid.
  • the nonionic surfactant comprises polyoxyethylene hydrogenated castor oil or polyoxyethylene polyoxypropylene alkyl ether.
  • composition capable of suppressing the precipitation of D-chiro-inositol.
  • the composition of the present invention is a composition containing D-chiro-inositol, an organic acid or a salt thereof, a surfactant, a monoalcohol having 1 to 3 carbon atoms, a polyhydric alcohol, and water.
  • D-chiro-inositol examples include, but are not particularly limited to, those extracted from naturally occurring buckwheat, beans, citrus, etc., those extracted and purified from legumes by fermentation, those chemically synthesized, and Commercial products can be mentioned.
  • the extraction method is not particularly limited, and a known extraction method can be used.
  • the content of D-chiro-inositol in the composition of the present invention is not particularly limited, but is preferably 0.001 to 20% by mass, more preferably 0.01 to 20% by mass, and still more preferably 0 to 20% by mass. 0.05 to 15% by mass, more preferably 1 to 10% by mass, still more preferably 3 to 7% by mass.
  • % by mass means the mass percentage of the components contained in the composition with respect to the mass of the entire composition.
  • X to Y means that it is X or more and Y or less.
  • the composition of the present invention can be used as an external preparation.
  • external preparations include, for example, agents for cracks and irrigations, agents for rashes and sores, agents for sea urchin and octopus, agents for dryness and irritations, agents for wrinkles and spots, humectants, hair dyes, hair restorers, shampoos, Rinse, conditioner, lotion, cream, milky lotion, hand cream, medicated soap, pack and the like can be mentioned.
  • the composition of the present invention contains D-chiro-inositol, a composition having a vitamin-like effect and a hair-growth activity can be obtained, and may be used as a hair-growth agent.
  • the hair growth activity is, specifically, an activity relating to hair shaft growth promotion, hair growth, prevention of hair loss, and the like, and preferably an activity relating to hair shaft growth promotion and hair growth.
  • the composition of the present invention contains an organic acid or a salt thereof, and preferably contains an organic acid and a salt of the organic acid.
  • an organic acid or a salt thereof even when the composition further contains a solvent other than water, for example, a monoalcohol having 1 to 3 carbon atoms, the feeling of use in a preparation containing the composition of the present invention can be improved. It becomes. It is presumed that such an effect is attributable to the fact that the organic acid or a salt thereof exerts a chelating effect and functions to reduce the stimulus contributed by a solvent other than water, for example, a monoalcohol having 1 to 3 carbon atoms. (However, the factor is not limited to this.)
  • the organic acid means an organic compound which is acidic alone in water.
  • the organic acid is not particularly limited as long as it is an organic compound exhibiting acidity, and examples thereof include monocarboxylic acids and polycarboxylic acids, and organic sulfonic acids.
  • monocarboxylic acids and organic sulfonic acids are preferable, and organic sulfonic acids are more preferable, from the viewpoint of suppressing the precipitation of D-chiro-inositol.
  • the monocarboxylic acid means an organic compound having one carboxylic acid in the molecule
  • the polyvalent carboxylic acid means an organic compound having two or more carboxylic acids in the molecule
  • the organic sulfonic acid means an organic compound having at least one sulfonic acid in a molecule.
  • a monocarboxylic acid For example, Formic acid, acetic acid, propionic acid, and valeric acid are mentioned.
  • polyvalent carboxylic acid examples include, but are not particularly limited to, dicarboxylic acid, tricarboxylic acid, and tetracarboxylic acid, and include, for example, citric acid, edetic acid, phthalic acid, isophthalic acid, terephthalic acid, succinic acid, fumaric acid, and maleic acid. Acids, malic acid, and tartaric acid. Among these, citric acid and edetic acid are preferred.
  • Organic sulfonic acids include, but are not limited to, methanesulfonic acid, benzenesulfonic acid, and taurine.
  • the salt in the organic acid salt is not particularly limited, and includes, for example, a sodium salt, a potassium salt, a calcium salt, and a magnesium salt. Of these, sodium salts are preferred.
  • the organic acids or salts thereof may be used alone or in combination of two or more. When two or more kinds are used in combination, a combination of two or more kinds of organic acids or a combination of two or more kinds of salts of organic acids may be used. These may be used in combination. When an organic acid and a salt of the organic acid are used, the organic acid and the organic acid of the salt of the organic acid may be the same or different, but the organic acid and the salt of the organic acid are used in combination. Is preferred.
  • the content of the organic acid or a salt thereof in the composition of the present invention is not particularly limited, but is usually 0.001 to 5% by mass, preferably 0.01 to 3% by mass, more preferably 0.03% by mass. To 1% by mass, more preferably 0.05 to 1% by mass.
  • the composition of the present invention contains a surfactant.
  • a surfactant By including a surfactant, it becomes possible to suppress the precipitation of D-chiro-inositol in an aqueous solution containing D-chiro-inositol.
  • a surfactant in the composition of the present invention it becomes possible to improve the feeling of use in a preparation containing the composition of the present invention. It is presumed that the factor that exerts such effects is due to the fact that the surfactant improves the solubility of D-chiro-inositol in an aqueous solution (however, the factor is not limited to this).
  • the surfactant examples include, but are not particularly limited to, a nonionic surfactant, a cationic surfactant, an anionic surfactant, and an amphoteric surfactant.
  • nonionic surfactants are preferable from the viewpoint that a good feeling in use is obtained, particularly, from the viewpoint of excellent permeability into pores.
  • One type of surfactant may be used alone, or two or more types may be used in combination.
  • the HLB value of the surfactant is not particularly limited, but is preferably 2 to 17, more preferably 6 to 17, and even more preferably 12 to 17.
  • HLB is an abbreviation for hydrophile-lipophile balance, and is one of the indices indicating the effect of a surfactant.
  • the HLB value when two or more surfactants are contained is a weighted average of the HLB values of each surfactant.
  • the nonionic surfactant means a surfactant that does not exhibit ionicity in an aqueous solution.
  • Nonionic surfactants include, but are not particularly limited to, for example, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene sorbitan oleate, monoesters of oleic acid and glycerin, and oleic acid. Esters of diglycerin.
  • polyoxyethylene-hardened castor oil and polyoxyethylene poly-polyethylene are preferred from the viewpoint of suppressing the precipitation of D-chiro-inositol and obtaining a good feeling in use, particularly from the viewpoint of excellent permeability into pores.
  • Oxypropylene alkyl ethers are preferred.
  • the cationic surfactant and the anionic surfactant mean a surfactant that becomes a cation and an anion when dissociated in an aqueous solution, respectively, and the amphoteric surfactant has a pH of the aqueous solution in the aqueous solution.
  • Means a surfactant that becomes one of a cation, an anion, and a zwitterion depending on the Examples of the cationic surfactant include, but are not particularly limited to, alkyldimethylamine, alkyltrimethylammonium salt, and dialkyldimethylammonium salt.
  • the anionic surfactant include, but are not particularly limited to, fatty acid salts and alkyl sulfates.
  • Examples of the amphoteric surfactant include, but are not particularly limited to, alkylamino fatty acid salts, alkyl betaines, and alkylamine oxides.
  • the content of the surfactant in the composition of the present invention is 1 to 10% by mass, preferably 1 to 7% by mass, and more preferably 1 to 5% by mass.
  • the content of the surfactant is in such a range, it becomes possible to suppress the precipitation of D-chiro-inositol in the aqueous solution containing D-chiro-inositol.
  • the usability can be improved.
  • the content of the monoalcohol having 1 to 3 carbon atoms is 40% by mass or more.
  • Precipitation of D-chiro-inositol by dissolving D-chiro-inositol, an organic acid or a salt thereof, a surfactant and a polyhydric alcohol in an aqueous solution of mono-alcohol having 1 to 3 carbon atoms of 40% by mass or more. Can be suppressed.
  • water examples include pure water such as ion-exchanged water, ultrafiltration water, reverse osmosis water, and distilled water, and water from which ionic impurities such as ultrapure water have been removed as much as possible.
  • the content of the monoalcohol having 1 to 3 carbon atoms in the composition of the present invention is within the range of 40% by mass or more, usually 80% by mass or less, preferably 50% by mass or less, more preferably 45% by mass or less. % Or less.
  • the monoalcohol having 1 to 3 carbon atoms is methanol, ethanol, n-propanol and isopropanol, preferably ethanol and isopropanol, and more preferably ethanol.
  • the monoalcohol having 1 to 3 carbon atoms may be used alone or in combination of two or more.
  • the composition of the present invention contains a polyhydric alcohol.
  • a polyhydric alcohol By containing a polyhydric alcohol, it becomes possible to suppress the precipitation of D-chiro-inositol in an aqueous solution containing D-chiro-inositol, and it is possible to improve the feeling of use in a preparation containing the composition of the present invention. It becomes.
  • a composition having antibacterial properties and moisture retention properties can be obtained by containing a polyhydric alcohol.
  • a surfactant and a polyhydric alcohol it is possible to suppress the precipitation of D-chiro-inositol in an aqueous solution containing D-chiro-inositol and an organic acid or a salt thereof.
  • the monoalcohol having 1 to 3 carbon atoms is methanol, ethanol, n-propanol and isopropanol, preferably ethanol and isopropanol, and more preferably ethanol.
  • the polyhydric alcohol means an alcohol having two or more hydroxyl groups in a molecule.
  • glycerin ethylene glycol, diethylene glycol, triethylene glycol, propylene glycol (1,2-propanediol), dipropylene glycol, trimethylolpropane, 1,3-propylene glycol ( 1,3-propanediol), isobutylene glycol (2-methyl-1,2-propanediol), 1,2-butanediol, 1,3-butyleneglycol (1,3-butanediol), 1,4-butane Diol, 2-butene-1,4-diol, 1,2-pentanediol, 1,5-pentanediol, 2-methyl-2,4-pentanediol, 1,2-hexanediol, 1,6-hexanediol , 2-ethyl-1,3-hexanediol, 1, - heptanediol
  • the content of the polyhydric alcohol in the composition of the present invention is 1 to 10% by mass, preferably 2 to 7% by mass.
  • the content of the polyhydric alcohol is in such a range, it is possible to suppress the precipitation of D-chiro-inositol in the aqueous solution containing D-chiro-inositol.
  • the usability can be improved.
  • the composition of the present invention may further include a monoterpene.
  • a monoterpene By containing a monoterpene, there is a tendency that a refreshing feeling can be imparted and a composition excellent in suppressing the precipitation of D-chiro-inositol can be obtained.
  • monoterpene examples include, but are not particularly limited to, monoterpene hydrocarbons such as limonene, pinene, and camphor; monoterpene alcohols such as citronellol, geraniol, linalool, menthol, terpineol, and borneol; monoterpenes such as citronellal, citral, and safranal Aldehydes; monoterpene ketones such as menthone, carbomentone, and yonone; Preferably, it is a monoterpene alcohol, and more preferably, menthol. These monoterpenes may be d-, l-, or dl-form.
  • menthol for example, l-menthol and d-menthol are preferred, and l-menthol is more preferred. It may be used as a mixture of 1-menthol and d-menthol. Monoterpenes may be used alone or in combination of two or more.
  • the content of the monoterpene in the composition of the present invention is not particularly limited, but in addition to imparting a refreshing feeling, suppressing precipitation of D-chiro-inositol, suppressing dripping and irritating feeling (crisp feeling) of the obtained composition. And 0.01 to 10% by mass, more preferably 0.05 to 2% by mass, and still more preferably 0.1 to 1.0% by mass because of excellent suppression of separation of the monoterpene itself. %, And still more preferably 0.7 to 1.0% by mass.
  • composition of the present invention may further contain additives that are generally acceptable in pharmaceuticals, quasi-drugs, cosmetics, and the like.
  • additives include, but are not limited to, excipients, stabilizers, odor correctors, bases, dispersants, diluents, emulsifiers, transdermal absorption enhancers, preservatives, coloring agents, oils (oils, fats, minerals, Oil, etc.), thickeners, polymers, film-forming agents, ultraviolet absorbers, cell activators, antioxidants, preservatives, fresheners, deodorants, pigments, dyes, fragrances, sugars, amino acids, vitamins, Organic acids, organic amines, plant extracts and the like can be mentioned.
  • the composition of the present invention is not particularly limited, and can be produced by mixing components contained in the present invention.
  • the order of mixing the components is not particularly limited.
  • the conditions for mixing are not particularly limited, and the composition of the present invention can be obtained according to a conventionally known method.
  • the composition of the present invention when used as an external preparation, it can be used as a drug, a quasi-drug, a cosmetic or the like.
  • it can be used as an external preparation for skin, an external preparation for hair, and an external preparation for scalp, and more specifically, a dermatological drug, a hair drug and a scalp drug, a quasi-drug for skin, and a hair
  • It can be used for quasi-drugs and quasi-drugs, as well as skin cosmetics, hair cosmetics and scalp cosmetics. More specifically, it can be in the form of an ointment, cataplasm, liniment, lotion, topical solution, dusting agent, cream, gel, emulsion, hair tonic, hair spray.
  • the “external preparation for hair” and the “external preparation for scalp” may be the same or different in the form and usage as the external preparation. Or scalp.
  • “external preparation for skin” is a concept including “external preparation for scalp” and means an external preparation that acts directly on the skin without being limited to the scalp.
  • the method of the invention comprises the step of administering a composition of the invention to a subject.
  • the dose of D-chiro-inositol per administration to a subject is not particularly limited, but is preferably 0.005 to 200 mg, more preferably 0.05 to 100 mg, and still more preferably 0.5 to 100 mg. 10 mg.
  • the frequency of administration of the composition of the present invention to a subject is not particularly limited, but is preferably 1 to 6 times per day, more preferably 1 to 3 times per day, and still more preferably 1 to 3 times per day. ⁇ 2 times.
  • composition of the present invention is administered is not particularly limited, and includes, for example, humans, animals such as domestic animals and pets.
  • D-chiro-inositol D-chiro-inositol (manufactured by Wako Pure Chemical Industries, Ltd .; hereinafter abbreviated as "DCI”) [Organic acid or salt thereof] Citric acid (Showa Kako) Sodium citrate (Showa Kako Co., Ltd .; hereinafter abbreviated as "Na citrate”) Sodium edetate (manufactured by Junsei Chemical Co., Ltd .; hereinafter, abbreviated as “Na edetate”) Acetic acid (Wako Pure Chemical Industries, Ltd.) Isophthalic acid (Wako Pure Chemical Industries, Ltd.) Taurine (Mitsui Chemicals) [Surfactant] HCO-10 (polyoxyethylene (10) hydrogenated castor oil, HLB value: 6.5, manufactured by Nikko Chemicals) HCO-20 (polyoxyethylene (20) hydrogenated castor oil, HLB value: 10.
  • DCI D-chiro-inos
  • Example 1 A solution prepared by dissolving DCI and an organic acid and / or a salt thereof in purified water, adding a mixture of EtOH and a surfactant to purified water so that each component has the composition shown in Table 1 below, and adding the remaining volume to purified water , And each composition was prepared as a preparation.
  • Formulation stability test The obtained preparation was evaluated for the precipitation of DCI in each composition by the following method. Formulations of each composition were prepared in 3 lots, and DCI precipitation was induced by a low-temperature cycle (12 hours 5 ° C incubation, 12 hours -20 ° C repeated for 14 days), and visually evaluated based on the following indices did. The evaluation results are shown in Table 1 (the number of N is 3). In all lots, no precipitation of crystals was observed " ⁇ " Even with 1Lot, slight precipitation of crystalline material was observed " ⁇ " Even with 1 Lot, a small number of crystals were precipitated. Even with 1 Lot, many crystals precipitated

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
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Abstract

L'invention a pour objectif d'obtenir une composition permettant d'empêcher la précipitation du D-chiro-inositol. Plus spécifiquement, l'invention concerne une composition contenant: du D-chiro-inositol, un acide organique et/ou un sel de celui-ci, un agent tensio-actif, un monoalcool C1-3, un alcool polyvalent et de l'eau. La teneur en monoalcool C1-3 est supérieure ou égale à 40% en poids, la teneur en agent tensio-actif est comprise entre 1 et 10 % en poids, et la teneur en alcool polyvalent est comprise entre 1 à 10% en poids de cette composition.
PCT/JP2019/024380 2018-06-29 2019-06-19 COMPOSITION CONTENANT DU D-chiro-INOSITOL Ceased WO2020004200A1 (fr)

Applications Claiming Priority (2)

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JP2018-125193 2018-06-29
JP2018125193A JP7203522B2 (ja) 2018-06-29 2018-06-29 Ｄ－ｃｈｉｒｏ－イノシトールを含む組成物

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WO2020004200A1 true WO2020004200A1 (fr) 2020-01-02

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Publication number Priority date Publication date Assignee Title
JP2020147541A (ja) * 2019-03-14 2020-09-17 小林製薬株式会社 外用組成物

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JP2006028026A (ja) * 2004-07-12 2006-02-02 Doctor Program Kk 育毛剤
JP2008169185A (ja) * 2007-01-15 2008-07-24 Hoyu Co Ltd 毛髪処理剤組成物及び毛髪処理方法
JP2009108023A (ja) * 2007-10-11 2009-05-21 Rohto Pharmaceut Co Ltd 育毛剤
WO2017188393A1 (fr) * 2016-04-27 2017-11-02 小林製薬株式会社 Agent de croissance capillaire
JP2019085342A (ja) * 2017-11-01 2019-06-06 小林製薬株式会社 Ｄ−ｃｈｉｒｏ−イノシトールを含む組成物
JP2019085339A (ja) * 2017-11-01 2019-06-06 小林製薬株式会社 Ｄ−ｃｈｉｒｏ−イノシトールを含む組成物

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Publication number Priority date Publication date Assignee Title
JP2006028026A (ja) * 2004-07-12 2006-02-02 Doctor Program Kk 育毛剤
JP2008169185A (ja) * 2007-01-15 2008-07-24 Hoyu Co Ltd 毛髪処理剤組成物及び毛髪処理方法
JP2009108023A (ja) * 2007-10-11 2009-05-21 Rohto Pharmaceut Co Ltd 育毛剤
WO2017188393A1 (fr) * 2016-04-27 2017-11-02 小林製薬株式会社 Agent de croissance capillaire
JP2019085342A (ja) * 2017-11-01 2019-06-06 小林製薬株式会社 Ｄ−ｃｈｉｒｏ−イノシトールを含む組成物
JP2019085339A (ja) * 2017-11-01 2019-06-06 小林製薬株式会社 Ｄ−ｃｈｉｒｏ−イノシトールを含む組成物

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020147541A (ja) * 2019-03-14 2020-09-17 小林製薬株式会社 外用組成物
JP7350498B2 (ja) 2019-03-14 2023-09-26 小林製薬株式会社 外用組成物
JP7570469B2 (ja) 2019-03-14 2024-10-21 小林製薬株式会社 外用組成物

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