External components

Abstract

It suppresses the decrease in creatine content over time. [Solution] The topical composition contains creatine and creatinine in a specific mass ratio.

Description

Technical Field

[0001] The present invention relates to an external composition.

Background Art

[0002] Creatine, which is one of the amino acids, is known to be present in living organisms such as muscles. Creatine is converted into creatine phosphate in the body and stored as an energy source. In addition, creatine is also used in compositions applied to the skin and hair for moisturizing and other purposes. For example, Patent Document 1 describes that a combination of creatine and other materials can impart firmness and elasticity to hair.

Prior Art Documents

Patent Documents

[0003]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0004] Since creatine is unstable in acidic or neutral solutions, it is necessary to devise a dissolution method in order to stably incorporate creatine into a composition. However, the pH range of external compositions mainly used for hair and skin is often in the acidic to neutral range from the viewpoint of safety. Therefore, a method for incorporating creatine that does not rely solely on pH adjustment has been demanded.

Means for Solving the Problems

[0005] As a result of intensive studies in view of such a situation, the present inventors have found that when creatine and creatinine are blended at a specific mass ratio, the amount of creatine in the preparation can be kept constant, and thus the present invention has been completed.

[0006] That is, the present invention includes the following inventions. Item 1. (A) Creatine (B) Creatinine A topical composition containing the following. Section 2. The topical composition according to item 1, wherein the mass ratio (A / B) of (A) creatine to (B) creatinine is 1.0 or more and 2.0 or less. Section 3. Furthermore, the topical composition according to item 2, comprising zinc gluconate. [Effects of the Invention]

[0007] The present invention makes it possible to prepare a topical composition containing creatine in a long-term stable manner by dissolving it. [Modes for carrying out the invention]

[0008] The embodiments of the present invention will be described in further detail below.

[0009] (A) Creatine Creatine is a type of organic acid found in skeletal muscle and other tissues. Including creatine in a topical composition can impart firmness and body to the hair. It is desirable that the creatine content in the topical composition be 0.1% by mass or more. It is even more desirable that the creatine content in the topical composition be 0.5% by mass or more.

[0010] (B) Creatinine Creatinine is a nitrogen-containing cyclic compound and is known to be produced by dehydration reactions of creatine. By incorporating creatine and creatinine in a certain mass ratio in topical compositions, the decrease in the creatine content of the composition can be suppressed.

[0011] The mass ratio of (A) creatine to (B) creatinine [(A) / (B)] is not particularly limited, but is preferably between 1.0 and 2.0. The mass ratio of (A) creatine to (B) creatinine [(A) / (B)] is more preferably between 1.0 and 1.5.

[0012] The pH of the topical composition of the present invention is not particularly limited, but from the viewpoint of use on skin and hair, it is preferably 3.0 to 8.0. A pH of 3.5 to 7.7 is more preferable. A pH of 4.0 to 7.0 is even more preferable.

[0013] In addition to the components described above, the topical composition of the present invention may contain other components that are normally incorporated into topical compositions, as long as they do not impair the effects of the present invention. Examples of other components include hair growth components, surfactants, fatliquoring agents, hair protectants, moisturizers, polymers, UV absorbers, solvents, pH adjusters, vitamins, antioxidants, antioxidant aids, preservatives, fragrances, cooling agents, and the like. These components may be used individually or in combination of two or more.

[0014] Examples of hair growth ingredients include peripheral vasodilators, hair follicle activators, anti-inflammatory agents, and sebum secretion inhibitors. Examples of peripheral vasodilators include carpronium chloride, nicotinic acid derivatives (e.g., benzyl nicotinate, nicotinamide, dl-α-tocopherol nicotinate, etc.), vitamin E derivatives (e.g., dl-α-tocopherol, d-α-tocopherol, dl-α-tocopherol acetate, etc.), acetylcholine, diphenhydramine hydrochloride, garlic iodide extract, spironolactone, γ-oryzanol, cepharanthine, nicorandil, minoxidil, diisopropylamine dichloroacetate, Swertia japonica extract, carrot extract, ginkgo biloba extract, cinchona extract, spruce extract, and sophora extract. Examples of hair follicle activators include mononitroguaiacol sodium, placenta extract, N-acetyl-L-methionine, adenosine, adenine, adenosine triphosphate disodium, cepharanthine, potassium aspartate, pentadecanoate glyceride, pantothenic acid, ethyl pantothenate, panthenol, yeast extract, garlic extract, royal jelly, and others.

[0015] Examples of UV absorbers include benzoic acid-based UV absorbers such as para-aminobenzoic acid, ethyl para-aminobenzoate, glyceryl para-aminobenzoate, amyl para-dimethylaminobenzoate, octyl para-dimethylaminobenzoate, and ethyl 4-[N,N-di(2-hydroxypropyl)amino]benzoate; anthranilic acid-based UV absorbers such as homomenthyl-N-acetylantranilate; salicylic acid-based UV absorbers such as ethylene glycol salicylate, phenyl salicylate, octyl salicylate, benzyl salicylate, p-tert-butylphenyl salicylate, and homomenthyl salicylate; benzyl cinnamate, 2-ethoxyethyl para-methoxycinnamate, octyl para-methoxycinnamate, glyceryl mono-2-ethylhexanoate dipara-methoxycinnamate, and isopodium para-methoxycinnamate. Examples include cinnamic acid-based UV absorbers such as ropyl-diisopropylcinnamic acid mixture, urocanic acid-based UV absorbers such as urocanic acid and ethyl urocanic acid, benzophenone-based UV absorbers such as hydroxymethoxybenzophenone, hydroxymethoxybenzophenone sulfonic acid, sodium hydroxymethoxybenzophenone sulfonate, dihydroxydimethoxybenzophenone, sodium dihydroxydimethoxybenzophenone disulfonate, dihydroxybenzophenone, and tetrahydroxybenzophenone, as well as 4-tert-butyl-4'-methoxydibenzoylmethane, 2,4,6-trianilino-p-(carbo-2'-ethylhexyl-1'-oxy)-1,3,5-triazine, and 2-(2-hydroxy-5-methylphenyl)benzotriazole.

[0016] Examples of fatliquoring agents include oils and fats, waxes, hydrocarbons, higher fatty acids, higher alcohols, and synthetic ester oils. Examples of oils and fats include avocado oil, camellia oil, almond oil, macadamia nut oil, corn oil, grapeseed oil, meadowfoam oil, olive oil, rapeseed oil, egg yolk oil, sesame oil, wheat germ oil, sasanqua oil, castor oil, safflower oil, cottonseed oil, soybean oil, peanut oil, tea seed oil, kaya oil, rice bran oil, jojoba oil, germ oil, cocoa butter, coconut oil, horse fat, hydrogenated coconut oil, palm oil, beef tallow, mutton fat, hydrogenated beef tallow, palm kernel oil, lard, Japanese wax kernel oil, and hydrogenated castor oil. Examples of waxes include beeswax, candelilla wax, cotton wax, carnauba wax, Japanese wax, bayberry wax, privet wax, whale wax, montan wax, rice bran wax, lanolin, kapok wax, lanolin acetate, liquid lanolin, sugarcane wax, reduced lanolin, jojoba wax, hard lanolin, shellac wax, and POE-lanolin alcohol ether. Examples of hydrocarbons include liquid paraffin, ozokerite, squalene, paraffin, ceresin, petrolatum, and microcrystalline wax. Examples of higher fatty acids include lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, 12-hydroxystearic acid, undecylenic acid, tallic acid, isostearic acid, linoleic acid, linolenic acid, eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA). Examples of higher alcohols include linear alcohols such as lauryl alcohol, cetyl alcohol, stearyl alcohol, behenyl alcohol, myristyl alcohol, oleyl alcohol, and cetostearyl alcohol, as well as branched-chain alcohols such as monostearyl glycerin ether (batyl alcohol), 2-decyltetradecinol, lanolin alcohol, cholesterol, phytosterols, hexyldodecanol, isostearyl alcohol, and octyldodecanol.Synthetic ester oils include isopropyl myristate, cetyl octanoate, octyldodecyl myristate, isopropyl palmitate, butyl stearate, hexyl laurate, myristyl myristate, decyl oleate, hexyldecyl dimethyloctanoate, cetyl lactate, myristyl lactate, lanolin acetate, isocetyl stearate, isocetyl isostearate, ethylene glycol di-2-ethylhexylate, dipentaerythritol fatty acid ester, N-alkyl glycol monoisostearate, neopentyl glycol dicaprate, diisostearyl malate, glycerin di-2-heptylundecanoate, trimethylolpropane tri-2-ethylhexylate, trimethylolpropane triisostearate, pentaneerythritol tetra-2-ethylhexylate, glycerin tri-2-ethylhexylate, and tri Trimethylolpropane isostearate, cetyl 2-ethylhexanoate, 2-ethylhexyl palmitate, glyceryl trimyristate, glyceride tri-2-heptyl undecanoate, methyl castor oil fatty acid ester, oleic acid oil, cetostearyl alcohol, acetoglyceride, 2-heptyl undecyl palmitate, diisobutyl adipate, 2-octyl lauroyl-L-glutamate Examples include dodecyl esters, di-2-heptylundecyl adipate, ethyl laurate, di-2-ethylhexyl sebatate, 2-hexyldecyl myristate, 2-hexyldecyl palmitate, 2-hexyldecyl adipate, diisopropyl sebatate, 2-ethylhexyl succinate, glyceryl trioctanoate, glyceryl triisopalmitate, isopropyl lanolinate, and hexyl laurate.

[0017] Examples of hair protectants include linear polysiloxanes such as dimethylpolysiloxane, methylphenylpolysiloxane, and methylhydrogenpolysiloxane; cyclic polysiloxanes such as decamethylpolysiloxane, dodecamethylpolysiloxane, and tetramethyltetrahydrogenpolysiloxane; and silicone resins.

[0018] Examples of humectants include polyethylene glycol, propylene glycol, glycerin, 1,3-butylene glycol, sorbitol, maltitol, maltotriose, mannitol, sucrose, erythritol, glucose, fructose, starch-derived sugars, maltose, xylitol, sugar alcohols such as starch-derived sugar-reduced alcohols, amino acids, chondroitin sulfate, hyaluronic acid, acetylated sodium hyaluronate, mucoitin sulfate, collagen derivatives, cholesteryl-12-hydroxystearate, sodium lactate, bile salts, seawater (including dried material), deep-sea water (including dried material), chitosan derivatives, sodium pyrrolidone carboxylate, and diglycerin-ethylene oxide-propylene oxide adducts.

[0019] Water is an example of a solvent. Furthermore, examples include lower alcohols such as methanol, propanol, isopropanol, isobutyl alcohol, and t-butyl alcohol; dihydric alcohols such as ethylene glycol, propylene glycol, trimethylene glycol, 1,2-butylene glycol, and 1,3-butylene glycol; trihydric alcohols such as glycerin, trimethylolpropane, and 1,2,6-hexanetriol; tetrahydric alcohols such as pentaerythritol; pentahydric alcohols such as xylitol; hexahydric alcohols such as sorbitol and mannitol; polyhydric alcohol polymers such as diethylene glycol, dipropylene glycol, triethylene glycol, polypropylene glycol, tetraethylene glycol, diglycerin, polyethylene glycol, triglycerin, tetraglycerin, and polyglycerin; dihydric alcohol alkyl ethers such as ethylene glycol monomethyl ether; dihydric alcohol alkyl ethers such as diethylene glycol monomethyl ether and diethylene glycol monoethyl ether; dihydric alcohol ether esters such as ethylene glycol monomethyl ether acetate; and glycerin monoalkyl ethers such as xyl alcohol, cerakyl alcohol, and batyl alcohol. The type of water used is not particularly limited; for example, distilled water, pure water, ultrapure water, purified water, tap water, etc., can be used. It can also be used in mixture with alcohol, which is used as a solvent.

[0020] Examples of pH adjusters include, for example, citric acid, lactic acid, acetic acid, hydrochloric acid, potassium hydroxide, sodium hydroxide, sodium lactate, sodium citrate, sodium lactate, etc. These can be used alone or in combination, and can be used not only for adjusting the pH value, but also for the purpose of buffering the adjusted pH value.

[0021] Examples of vitamins include, for example, vitamins A, B1, B2, B6, E, and their derivatives, pantothenic acid, and its derivatives, etc.

[0022] Examples of antioxidants include, for example, tocopherols, dibutylhydroxytoluene, butylhydroxyanisole, gallic acid esters, etc.

[0023] Examples of antioxidant aids include, for example, organic acids such as benzoic acid, sodium benzoate, undecylenic acid, salicylic acid, sorbic acid, paraoxybenzoate, and their derivatives, phenols such as isopropylmethylphenol, phenoxyethanol, 1,2 - hexanediol, 1,2 - pentanediol, etc.

[0024] Examples of preservatives include, for example, organic acids such as benzoic acid, sodium benzoate, undecylenic acid, salicylic acid, sorbic acid, paraoxybenzoate, and their derivatives, phenols such as isopropylmethylphenol, phenoxyethanol, 1,2 - hexanediol, 1,2 - pentanediol, etc.

[0025] Examples of fragrances include known fragrances used in topical compositions, which may be natural fragrances or synthetic fragrances. Also, they may be single - ingredient fragrances or compounded fragrances. Specific examples of fragrances include menthol, carvone, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronellol, α-terpineol, methyl acetate, citronellyl acetate, methyl eugenol, cineole, linalool, ethyl linalool, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, perilla oil, wintergreen oil, clove oil, eucalyptus oil, pimento oil, d-camphor, d-borneol, fennel oil, cinnamon oil, cinnamaldehyde, peppermint oil, vanillin, and others.

[0026] The application site of the topical composition is not particularly limited and can be applied to the skin or hair. It is preferable to apply the topical composition to the hair.

[0027] The application form of the topical composition is not particularly limited and can be used, for example, as a pharmaceutical, quasi-drug, or cosmetic. The dosage form of the topical composition is not particularly limited and can be, for example, liquid, emulsion, suspension, cream, ointment, aerosol, spray, etc.

[0028] When the aforementioned external composition is used on hair, known applications can be appropriately adopted, such as hair growth agents, hair tonics, lotions, cosmetics, shampoos, rinses, and conditioners. Among these, conditioners are preferred. [Examples]

[0029] The present invention will be described in more detail below with reference to test examples and formulation examples, but the present invention is not limited to these. The topical compositions of Examples 1 to 6 and Comparative Examples 1 to 6 shown in Table 1 were prepared by mixing and stirring each component according to conventional methods.

[0030] [Table 1]

[0031] (Creatine content measurement) For the topical compositions of Examples 1-6 and Comparative Examples 1-6, samples were prepared after being stored at -5°C for one month and after being stored at 40°C for one month. For each sample, the creatine content and creatinine content were measured by gradient elution using high-performance liquid chromatography (HPLC).

[0032] First, TEGO® Cosmo C 100, manufactured by Evonik, was prepared as the standard substance for creatine. Additionally, TEGO® Cosmo C 250, also manufactured by Evonik, was prepared as the standard substance for creatinine. Next, using the creatine and creatinine standards mentioned above, standard samples for the calibration curve shown in Table 2 were prepared.

[0033] [Table 2]

[0034] As shown in Table 2, 20 mg of creatine standard was precisely weighed and dissolved in ultrapure water to a total volume of 10 mL to obtain standard stock solution A (creatine, 2 mg / mL). Similarly, 20 mg of the above creatinine standard was precisely weighed and dissolved in ultrapure water to a total volume of 10 mL to obtain standard stock solution B (creatinine, 2 mg / mL). Standard stock solutions A and B were diluted with methanol to obtain calibration curve standard samples (S1-S5). Methanol was used as the blank sample. Next, for the cosmetic compositions of Examples 1-6 and Comparative Examples 1-6, samples stored at -5°C for one month and samples stored at 40°C for one month were stirred, and approximately 0.2 g of each was taken into a container. Furthermore, the samples were dissolved in methanol to make a total volume of 50 mL, and then sonicated to completely dissolve in methanol to obtain analytical samples. Next, as shown in Table 3, the creatine and creatinine content in each analytical sample was measured by gradient elution under the following analytical conditions, while varying the concentrations of mobile phase A and mobile phase B over time.

[0035] [Table 3]

[0036] (HPLC conditions) Guard column: HILICpak VG-502A (Shodex) Analytical column: HILICpak VG-502D 2.0 × 150 mm, 5 μm (Shodex) Mobile phase A: Ultrapure water Mobile phase B: Acetonitrile Flow rate: 0.3mL / min Column temperature: 40℃ Sampler temperature: 10℃ Injection volume: 5μL Detection wavelengths: 210nm (creatine), 234nm (creatinine) Analysis time: 20 minutes

[0037] (Creatine stability assessment) The creatine stability of the topical compositions in Examples 1-6 and Comparative Examples 1-6 was evaluated. The creatine stability was determined by calculating the percentage change in creatine content of a sample left at 40°C for one month compared to the percentage change in creatine content of a sample left at -5°C for one month. The evaluation criteria for creatine stability were as follows. ◎: The difference in creatine change rate relative to 100% is less than ±20%. ○: The difference in creatine change rate relative to 100% is ±20% or more and less than ±30%. ×: Difference in creatine change rate relative to 100% is ±30% or more.

Claims

1. (A) Creatine (B) Creatinine A topical composition containing the following.

2. The topical composition according to claim 1, wherein the mass ratio (A / B) of (A) creatine to (B) creatinine is 1.0 or more and 2.0 or less.

3. Furthermore, the topical composition according to claim 2 further comprises zinc gluconate.

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