KR20070068288A - Parenting Composition - Google Patents

Abstract

A hair growth stimulating composition is provided to show excellent hair-growing effect by promoting percutaneous absorption of a hair growth stimulating ingredient and promote the improvement of storage stability. The hair growth stimulating composition comprises (A) a hair growth stimulating ingredient such as tocopherol acetate, nicotinic acid amide, pantothenyl alcohol, acetyl pantothenylethylether, hinokitiol, an extract of Swertia pseudo-chinensis, beta-glycyrrhetinic acid, l-menthol, pyroctone olamine and isopropylmethylphenol, (B) a polyhydric alcohol such as polyethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol and isoprene glycol, (C) a fatty acid propylene glycol ester, and (D) 5-50 wt.% of water.

Description

Hair raising composition {HAIR GROWTH STIMULATING COMPOSITION}

1 is a perspective view of a Franz-type diffusion cell used in the test of the present invention.

2 is an explanatory diagram illustrating a test method using a Franz-type diffusion cell.

(Explanation of the sign)

1 Franz diffusion cell

2 donor

3 receptor

4 stirrer

5 back peeling skin

The present invention relates to a parenting agent composition which promotes percutaneous absorption of the parenting active ingredient and is excellent in storage stability of the composition. More specifically, the parenting effect is more effectively exhibited by improving the percutaneous absorption of the parenting active ingredient. It relates to a parenting composition.

As a means of improving the storage stability of the lipophilic parenting hair active ingredient, the method which uses a formulation as an ethanol is common. However, when there is much ethanol, especially a person with sensitive skin feels irritation to a skin, and there are people who care about an ethanol smell. For this reason, when the content of water is increased instead of ethanol, there is a problem that the stability of the parenting active ingredient is deteriorated.

On the other hand, since the epidermis has a structure that prevents foreign substances from entering the body, sufficient transdermal absorption is not obtained by the barrier function of the stratum corneum only by applying an active ingredient on the skin. In the case of the parenting active ingredient, the effect is expressed by penetration into the skin, and in order to enhance the effect of the parenting effective ingredient, it is important to improve the skin permeability of the parenting effective ingredient. On the other hand, in order to improve the skin permeability of the hair raising active ingredient, various transdermal absorption accelerators have been proposed.

As the transdermal absorption accelerators, for example, surfactants, various oil agents, terpenes and the like have been proposed. Specifically, branched fatty acids and alcohols (see Patent Document 1: Japanese Patent Application Laid-Open No. 2-207018) as a penetrating agent of a medicament in an external preparation for skin include polyethylene glycol (Patent Document 2: Japanese Patent Application Laid-Open No. 2001-106621 has been proposed, and mono or diesters of even-carbon long-chain fatty acids have been proposed for improving the water absorption of odd-chain fatty acid glycerides, which are active ingredients of hair growth agents. See G. 4-66516). However, most of these absorption accelerators are lipophilic substances, and when a large amount of water is contained in the hair growth agent composition, precipitation of the parenting active ingredient appears, and it is difficult to secure long-term stability, and the effect of the parenting active ingredient is still sufficiently sufficient. It did not lead to exercise. From the above, while further improving the percutaneous absorption of the parenting hair active ingredient, precipitation of the parenting hair active ingredient, etc. is suppressed in the composition with much water content, and the hair raising agent composition excellent in the storage stability of a composition was desired. Moreover, the following are mentioned as a prior art document concerning this invention.

[Patent Document 1] Japanese Unexamined Patent Publication No. 2-207018

[Patent Document 2] Japanese Patent Application Laid-Open No. 2001-106621

[Patent Document 3] Japanese Unexamined Patent Publication No. 4-66516

[Patent Document 4] Japanese Patent Application Laid-Open No. 10-72321

[Patent Document 5] Japanese Patent Application Laid-Open No. 2003-321330

The present invention has been made in view of the above circumstances, and by external application to the scalp, it promotes percutaneous absorption of parenting hair active ingredients, has hair growth promoting effect and effect of preventing hair loss, and has no irritation and ethanol odor is reduced, Even if the amount of water in the composition is large, it is an object of the present invention to provide a hair raising composition having excellent storage stability by inhibiting precipitation of the hair raising active ingredient.

MEANS TO SOLVE THE PROBLEM As a result of earnestly examining in order to achieve the said objective, the polyhydric alcohol and fatty acid propylene glycol ester as a percutaneous absorption promoter of a parenting hair active ingredient in the parenting composition containing 5-50 mass% of parenting hair active ingredients and water in a composition. When the compound was formulated, it was found that the percutaneous absorption of the parenting active ingredient is promoted, and that the precipitation of the parenting active ingredient at low temperature can be suppressed despite the composition having a large water content, thereby completing the present invention.

Accordingly, the present invention provides the following invention.

[One]. A parenting composition containing (A) parenting hair active ingredient, (B) polyhydric alcohol, (C) fatty acid propylene glycol ester, and (D) 5-50 mass% of water.

[2]. Furthermore, the parenting agent composition as described in [1] containing (E) polyoxyethylene oleyl ether.

[3]. (A) Parenting active ingredient is selected from tocopherol acetate, nicotinic acid amide, pantothenyl alcohol, acetylpantotenylethyl ether, hinokithiol, bittersweet extract, β-glyciletin acid, 1-menthol, pyroctonolamine and isopropylmethylphenol The raising agent composition as described in [1] or [2] which is 1 type, or 2 or more types.

[4]. (B) The parenting agent composition according to any one of [1] to [3], wherein the polyhydric alcohol is one or two or more selected from polyethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, and isoprene glycol. .

(The best form to carry out invention)

(A) component of this invention is a parenting hair effective ingredient. Examples of parenting hair active ingredients include cell activators, vitamins, hormones, vasodilators, amino acids, anti-inflammatory agents, fungicides, and keratin-soluble agents, and can be used alone or in combination of two or more. Can be. Specifically, examples of the cell activator include pentadecanoic acid glycerides, hino chitinol, forskolin, trans-3,4'-dimethyl-3-hydroxyflavanone, and vitamins such as tocopherols such as tocopherol acetate and nicotinic acid. Examples of nicotinic acid amide, palmitic retinol, β-carotene, calciferol, folic acid, biotin, D-pantothenyl alcohol, acetylpantotenylethyl ether, calcium pantothenate, pantothenylethyl ether, ascorbic acid, and hormones include estradiol As vasodilators, such as minoxidil, bitter grass extract, amino acids, such as arginine, aspartic acid, methionine, serine, glycine, glutamic acid, cystine, and the like, as anti-inflammatory agents, β-glyciretinic acid, glycyric acid, pyridoxine hydrochloride, etc. As an isopropyl methyl phenol, a pyroctonolamine etc. are mentioned. As the active ingredient, tocopherol acetate, nicotinic acid amide, pantothenyl alcohol, acetylpantotenylethyl ether, hinokithiol, bittersweet extract, β-glyciletinic acid, 1-menthol, pyroctonolamine and isopropylmethylphenol are preferable.

(A) Although the compounding quantity of the raising parent active ingredient is an effective amount of the raising parent active ingredient mix | blended, it is normally 0.001-10 mass% in a raising agent composition, and 0.005-5 mass% is preferable.

(B) component is polyhydric alcohol, and can be used individually by 1 type or in combination of 2 or more types. Ethylene glycol, diethylene glycol, triethylene glycol, polyethylene glycol, propylene glycol, dipropylene glycol, polypropylene glycol, 1, 3- butylene glycol, isoprene glycol, etc. are mentioned. Among these, polyethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol and isoprene glycol are preferable, and polyethylene glycol is especially preferable.

The range of the preferable average molecular weight of polyethyleneglycol (the average molecular weight test method of polyethylene glycol 200 listed in cosmetic raw material standard) is 200-1000, More preferably, it is 200-400. Specifically, polyethylene glycol 200, 300, 400, 600, 1000 (based on cosmetic raw material standards) are preferable, More preferably, they are 300-600 polyethylene glycol. In this range, the percutaneous absorption promotion of the parenting active ingredient is further improved.

(B) Although the compounding quantity of polyhydric alcohol can be adjusted suitably, 0.001-20 mass% is preferable in a hair raising agent composition, More preferably, it is 0.01-10 mass%. When too small, satisfactory transdermal absorption promoting effect may not be exhibited, and even if it mixes more than 20 mass%, the further effect improvement is not exhibited normally.

(C) component of this invention is fatty acid propylene glycol ester, It can be used individually by 1 type or in combination of 2 or more types. The fatty acid constituting the fatty acid propylene glycol ester may be a saturated fatty acid or an unsaturated fatty acid. In addition, the unsaturated fatty acid may contain one or a plurality of double bonds. The carbon number of the carbon chain is preferably 6 to 22, more preferably 8 to 18, and the carbon chain may be linear or branched. Examples of such fatty acid propylene glycol include propylene glycol octanoate, propylene glycol decanoate, propylene glycol laurate, propylene glycol myristic acid, propylene glycol palmitic acid, propylene glycol oleate, and propylene glycol stearate. Glycol and propylene glycol laurate are particularly preferred.

Although the compounding quantity of (C) fatty acid propylene glycol ester can be prepared suitably, 0.01-20 mass% is preferable in a hair raising agent composition, More preferably, it is 0.1-10 mass%. When too small, satisfactory transdermal absorption promoting effect may not be exhibited, and even if it mixes more than 20 mass%, the effect improvement beyond that is not normally exhibited.

As for the compounding mass ratio ((B) / (C)) of (B) polyhydric alcohol and (C) fatty acid propylene glycol ester, 1/10-100/1 are preferable, More preferably, 1/5-10/1 to be. By setting it as this ratio, the percutaneous absorption promotion of the hair raising active ingredient improves more.

(D) component of this invention is water, and the compounding quantity is 5-50 mass% in the hair raising composition. Even if it is the compounding quantity of water of this range, precipitation of the hair raising active ingredient at low temperature can be suppressed and it is excellent in storage stability. Moreover, even if the compounding quantity of water is in the range of 10-50 mass%, especially 15-40 mass% in a hair raising composition, it can exhibit more effects.

What is necessary is just to mix | blend (E) polyoxyethylene oleyl ether with the hair raising agent composition of this invention. (E) Polyoxyethylene oleyl ether can be used individually by 1 type or in combination of 2 or more types. The average EO addition mole number of polyoxyethylene oleyl ether becomes like this. Preferably it is 1-20, More preferably, it is 1-10, More preferably, it is 1-5.

As for the compounding quantity of (E) polyoxyethylene oleyl ether, 0.01-10 mass% is preferable in a hair raising composition, More preferably, it is 0.05-5 mass%. If the blending amount is too small, satisfactory transdermal absorption promoting effect may not be exhibited, and even if blended in excess of 10% by mass, the effect improvement beyond that is not usually exhibited, and the usability such as stickiness may be reduced. .

Ethanol can be mix | blended with the hair raising composition of this invention, and fermentation ethanol is preferable at the point of suppressing the irritating smell. 40 mass% is preferable, and, as for the minimum of the compounding quantity in the hair raising composition of ethanol, the upper limit of a compounding quantity is preferable, 90 mass% is preferable, More preferably, it is 80 mass%, More preferably, Is 70 mass%.

In addition to the essential components described above, the parenting agent composition may be blended with any component within the range not impairing the effects of the present invention depending on the purpose of use and the like. Examples of such optional components include alcohols other than ethanol, nonionic surfactants, saccharide surfactants, other surfactants, celluloses, fats and oils, polymer resins, colorants, flavoring agents, ultraviolet absorbers, and keratin solubilizers. It can be used individually by 1 type or in combination of 2 or more types.

As surfactant, as celluloses, such as polyoxyethylene hardened castor oil, polyoxyethylene hardened castor oil mono or isostearate, glycerin fatty acid ester, hydroxymethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, etc. Examples of the polymer resins such as safflower oil, moonshine colostrum oil and jojoba oil include, for example, amphoteric, cationic, anionic and nonionic polymers such as ultraviolet absorbents such as octyl oxycinnamate (neoheliopan AV; Haamann & Reimer trade name), Examples of keratin solubilizers such as oxybenzone and uronic acid include salicylic acid and resorcin.

When mix | blending a fragrance with the raising agent composition of this invention, the fragrance used is based on the fragrance and fragrance composition of Unexamined-Japanese-Patent No. 2003-95895, and when mix | blending a fragrance composition, with respect to the whole raising agent composition whole quantity, It is preferable to mix | blend so that a fragrance composition may be 0.00001-50 mass%, More preferably, it is 0.0001-30 mass%.

The parenting agent composition of this invention can be prepared according to a conventional method, and can be prepared in the form of a uniform solution, lotion, a gel, etc. Moreover, the hair raising composition of this invention can take the form of an aerosol, and in that case, in addition to the said component, lower alcohols, such as n-propyl alcohol and isopropyl alcohol, butane, propane, isobutane, liquefied petroleum gas Compressed gases, such as flammable gases, such as dimethyl ether, nitrogen gas, oxygen gas, carbon dioxide gas, and nitrous oxide gas, can be mix | blended, and the mixture of these can also be used. In that case, dimethyl ether and nitrogen gas are mixed at a mass ratio (dimethyl ether / nitrogen gas) = 99.99 / 0.01 to 50/50, and liquefied petroleum gas and dimethyl ether are mass ratio (liquefied petroleum gas / dimethyl ether) = 99/1 to 1 It is preferable to mix | blend / 99 and liquefied petroleum gas and nitrogen in mass ratio (liquefied petroleum gas / nitrogen) = 99.99 / 0.01-50 / 50.

Since the parenting agent composition of the present invention has a percutaneous absorption promoting effect on the scalp of the parenting active ingredient, it exhibits excellent parenting effect, and has high practicality in which the parenting active ingredient is stable for a long time, and the above (A) and ( It is useful as a percutaneous absorption accelerator of the hair raising active ingredient which consists of a mixture which mix | blends (B), (C), Preferably (E) component with the mixture containing D) component. Moreover, since it contains 5-50 mass% of water, it is suitable also for sensitive skin and can reduce an ethanol odor.

(Example)

Hereinafter, although an Example and a comparative example are shown and this invention is demonstrated concretely, this invention is not limited to the following Example. In addition, in the following example, when there is no specification in particular, "%" of a composition shows the mass%.

Examples 1 to 11 and Comparative Examples 1 to 5

The parenting agent composition of the composition shown to Tables 1-3 was prepared, and the skin transmittance of the parenting active ingredient in the parenting agent composition, and the low temperature stability of the parenting agent composition were evaluated. The results are written together in Tables 1-3.

<Skin Permeability of Parenting Active Ingredients>

Skin permeability was measured using the glass Franz type diffusion cell shown in FIG. The skin transmittance measuring method of the active ingredient using Franz type diffusion cell is demonstrated using FIGS.

The exfoliated skin 5 (5 cm x 5 cm) of a mortar (HARTLEY type, female) previously shaved off is placed in the Franz-type diffusion cell 1 (diffusion effective film area approximately 4 cm ² ), and the stratum corneum layer is on the donor (2). It was inserted and fixed so that the dermal side was on the receptor (3). After the receptor 3 side was filled with physiological saline, it was kept at 32 ° C. in the constant temperature layer while stirring with a stirrer 4. 50 µL of the test sample was added to the donor 2 (stratum corneum side), and physiological saline in the receptor 3 was sampled 24 hours after the addition. The active parenting ingredient in physiological saline was quantified, and the said effective amount (skin permeation amount) in the receptor 3 phase was measured.

The relative value (%) of the permeation amount of each composition when the permeation amount of the 2% ethanol solution (control) of each active ingredient was made into 100% of the transmittance | permeability was computed.

About the quantification method of the hair raising active ingredient, it shows below.

(1) tocopherol acetate

It measured based on the Japanese Pharmacopoeia Commentary, Tocopherol Acetate Assay.

(2) Nicotinic acid amide Quantification was carried out using high performance liquid chromatography (HPLC).

Detector: ultraviolet absorbance photometer (wavelength: 210-270 nm)

Column: Inertsil ODS-2 (φ4.6 × 150mm, manufactured by GLS Sciences)

Mobile phase: methanol / water mixture

<Low Temperature Stability Evaluation>

After filling 50 mL of the test sample in the transparent glass bottle with a cap, the presence or absence of precipitation and precipitation at the time of storing at -5 degreeC was evaluated externally. The external appearance was observed and low temperature stability was evaluated on the following references | standards.

standard

Number of days before precipitation or sediment was confirmed

<1 week: ×

1 to 2 weeks: △

Precipitation and sedimentation have not been confirmed after 2 weeks: ○

While all of the parenting agent compositions (Examples 1 to 11) of the present invention exhibited excellent properties in skin penetration, all of the parenting agent compositions (Comparative Examples 1 to 5) outside the scope of the present invention did not exhibit excellent characteristics. .

Hereinafter, the Example of the hair raising agent composition is shown. In addition, the hair raising composition of each following example was prepared according to the conventional method of each formulation according to each composition.

Example 12

(Hair growth lotion)

Furtherance %

D-pantothenyl alcohol 2.0

Nicotinic Acid Amide 1.0

6-benzylaminopurine 1.0

β-glyciletic acid 0.5

Isopropylmethylphenol 0.5

Pyroctonolamine 0.1

Frequent X 0.1

Propylene Glycol 5.0

PEG 300 1.0

Propylene Glycol Oleate 0.5

Monooctanoic Acid Propylene Glycol 0.5

POE (2) Oleyl Ether 0.5

POE (30) tetraoleic acid sorbet 0.05

1-menthol (synthetic) 0.1

Hinokithiol 0.3

Methylparaben 0.1

Citric Acid 0.05

Spices * 0.3

Purified water 20.0

99% ethanol balance

Total 100.0

* The composition of Table 2B of Japanese Patent Laid-Open No. 2003-113019 was used.

Example 13

(Hair growth hair spray)

Furtherance %

(Stock)

Pantothenylethyl Ether 1.0

Salicylic Acid 0.5

Pyroctonolamine 0.1

Nicotinic Acid Amide 0.05

β-glycitinic acid 0.05

6-benzylaminopurine 1.0

PEG 300 3.0

Propylene Glycol Oleate 0.5

POE (2) Oleyl Ether 0.1

POE (40) Cured Castor Oil 0.5

Yeonmyeongcho Extract 1.0

Citric Acid 0.1

1-menthol (synthetic) 0.5

Fragrance *

Purified water 30.0

99% ethanol balance

Total 100.0

(Diluent)

The stock solution 75

Dimethyl ether 25

Nitrogen

Total 100.0

Product pressure: 0.6 MPa (25 ℃)

* Table 2D composition of Unexamined-Japanese-Patent No. 2003-113019 was used.

Example 14

(Hair growth tonic)

Furtherance %

Tocopherol Acetate 0.1

β-glycitinic acid 0.1

Nicotinic Acid Amide 0.1

6-benzylaminopurine 1.0

Isopropylmethylphenol 0.1

PEG 300 1.0

POE (2) Oleyl Ether 0.1

Oleic Acid Propylene Glycol 1.0

Coleus Paul's Coli Root Extract 0.5

Succinic Acid 0.1

Fragrance * 0.5

Purified water 35.0

95% ethanol balance

Total 100.0

* A composition of Table 2 of Japanese Patent Laid-Open No. 2003-113019 is used.

The skin permeability of the hair raising component was evaluated in the same manner as in the above example with respect to the hair raising composition of the various formulations of Examples 12 to 14, and all showed high skin permeability of the hair raising component.

The raw material used by the said example is shown.

Raw material name product name Raw Material Maker Tocopherol Acetate Acetic acid DL-α-tocopherol DSM Nutrition Japan Co., Ltd. D-pantothenyl alcohol Pantonol Daiichi Fine Chemical Co., Ltd. Nicotinic acid amide Nicotinic acid amide DSM Nutrition Japan Co., Ltd. Pantothenylethyl ether Pantothenylethyl ether Daiichi Fine Chemical Co., Ltd. β-glycitinic acid β-glycitinic acid Maruzen Seyaku Co., Ltd. Isofurophyllmethylphenol Isofurophyllmethylphenol Osaka Kasei Co., Ltd. Pyrrophytonolamine Octopyrox Clariant Japan Salicylic acid Salicylic acid Yoshitomi Fine Chemical Co., Ltd. 6-benzylaminopurine 6-benzylaminopurine Sansho Seyaku Co., Ltd. Polyethylene Glycol 300 PEG 300  Lion Chemical Co., Ltd. Propylene glycol oleate Sansoft 250DV Taiyo Kagaku Corporation Propylene glycol oleate NOFABLE PO-991 Nippon Yushi Corporation Ethyl oleate Purified Ethyl Oleate Nippon Yushi Corporation Glyceryl Oleate NIKKOLMGO Nikko Chemicals Oleic acid sorbitan Emema SPO-100 Nihon Emulsion Co., Ltd. Monooctanoic Acid Propylene Glycol NIKKOL SEFSOL218 Nikko Chemicals Propylene glycol laurate Emarex PGML Nihon Emulsion Co., Ltd.

Coleus phospholipid extract Coleus X Toyota Makori Corporation Frequent X Barberry Extract Liquid Maruzen Seyaku Co., Ltd. Hinoki Thiol Hinoki Thiol Takasagokoryo Co., Ltd. Methylparaphene Methyl Paraoxybenzoate Yoshitomi Seyaku Co., Ltd. POE (2) oleyl ether Nonion E-202S Nippon Yushi Corporation POE (30) tetraoleic acid sorbet GO-430V Nikko Chemicals Propylene glycol Propylene glycol Asahi Tenka Corporation 1,3-butylene glycol 1,3-butylene glycol Daiselka Gaku High School POE (40) Cured Castor Oil HC-40 Nihon Emulsion Co., Ltd. 1-menthol (synthetic) 1-menthol Takasago Koryo High School Citric acid Citric acid Fusoka Gaku High School Succinic acid Succinic acid Fusoka Gaku High School 99% ethanol 99% Primary Fermentation Alcohol Shinwa Alcohol Sankyo Co., Ltd. 95% ethanol 95% primary fermentation alcohol Shinwa Alcohol Sankyo Co., Ltd. Dimethyl ether Dimethyl ether Sumitomo Seka

The parenting agent composition of this invention is effective in raising hair growth by mix | blending (B) polyhydric alcohol and (C) fatty acid propylene glycol ester with the parenting agent composition containing (A) the raising parent active ingredient and (D) 5-50 mass% of water. The percutaneous absorption of the components can be promoted, and the excellent hair growth effect can be exhibited, and the storage stability can be improved.

Claims (4)

(A) Raising hair active ingredient, (B) polyhydric alcohol, (C) fatty acid propylene glycol ester, and (D) 5-50 mass% of water, The nurturing agent composition characterized by the above-mentioned. The parenting agent composition of Claim 1 which further contains (E) polyoxyethylene oleyl ether. The method according to claim 1 or 2, wherein (A) the rearing hair effective ingredient is tocopherol acetate, nicotinic acid amide, pantothenyl alcohol, acetylpantotenylethyl ether, hinokithiol, barberry extract, β-glyciletin acid, 1-menthol, A parenting composition comprising one or two or more selected from pyrophytonolamine and isopropylmethylphenol. 3. The parenting hair according to claim 1 or 2, wherein (B) the polyhydric alcohol is one or two or more selected from polyethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, and isoprene glycol. Agent composition.

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