JP3519269B2 - External preparation for skin - Google Patents

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin. More specifically, it relates to a skin external preparation which is excellent in the effect of promoting lipid decomposition and the effect of improving rough skin.

[0002]

2. Description of the Related Art Conventionally, in order to reduce excess fat and maintain a lean body, in addition to various exercises and dietary restrictions, use of skin cosmetics such as gels and creams that promote metabolism in the body. It has been known.

To such a cosmetic, a xanthine derivative is incorporated for the purpose of slimming effect in order to promote the lipolysis of adipocytes constituting fat.

On the other hand, a skin cosmetic for the purpose of improving rough skin generally contains a polysaccharide.

[0005]

However, in the conventional skin cosmetics for slimming effect, the effect of promoting lipolysis of adipocytes is not always sufficient.

In view of the above-mentioned viewpoints, the present inventor diligently studied the lipolytic effect of the xanthine derivative, and as a result, when the xanthine derivative, the polysaccharide and a certain specific compound were added to the skin external preparation, it was surprising. The inventors have found that the effect of promoting lipolysis of adipocytes and the effect of improving rough skin are synergistically increased, and the present invention has been completed.

An object of the present invention is to provide a skin external preparation which is extremely excellent in promoting lipolysis of adipocytes and improving rough skin.

[0008]

Means for Solving the Problems That is, the present invention provides a xanthine derivative, one or more polysaccharides selected from the group consisting of erythritol, hyaluronic acid, and salts thereof , and (1) below. It is intended to provide an external preparation for skin, which comprises at least one of the specific compounds shown. (1) Glycine, valine, leucine, isileucine, phenylalanine, serine, alanine, tyrosine, threonine, proline, hydroxyproline, tryptophan, methionine, cystine, aspartic acid, arginine, glutamic acid, glutamine, lysine, arginine,
Histidine, trimethylglycine, glutathione.

The present invention also provides that the xanthine derivative is one or more selected from the group consisting of caffeine, theophylline, theobromine, xanthine, aminophylline, choline theophylline, diprophylline, proxyphylline and oxtriphylline. The above-mentioned external preparation for skin is provided.

Further, in the present invention, the external preparation for skin is a fat
The above-mentioned skin external preparation is provided as a skin external preparation for accelerating decomposition .

[0011]

BEST MODE FOR CARRYING OUT THE INVENTION The constitution of the present invention will be described in detail below.

Examples of the xanthine derivative used in the present invention include caffeine, theophylline, theobromine, xanthine, aminophylline, choline theophylline, diprophylline, proxyphylline, oxtriphylline and the like, and particularly, caffeine, aminophylline and theophylline. Is preferred. These can be used alone or in combination of two or more. As these derivatives, those obtained from plants such as synthetic or tea leaves can be used, and commercially available products can be used.

The content of the xanthine derivative in the external preparation for skin is 0.0001% by weight or more, preferably 0.005 to 10.0% by weight, based on the total amount of the external preparation for skin.

The polysaccharide used in the present invention is preferably erythritol, sialic acid, trehalose, glucosamine, glucuronic acid, dextran, mucoitin sulfate, hyaluronic acid and the like. These can be used alone or in combination of two or more.

The content of the polysaccharide in the external preparation for skin is 0.0001% by weight or more, preferably 0.001 to 10.0% by weight, based on the total amount of the external preparation for skin.

In the present invention, the specific compound to be blended with the above-mentioned essential components is at least one of the specific compounds shown in the following (1), and it is possible to use one kind alone or two or more kinds in combination. it can. (1) Glycine, valine, leucine, isileucine, phenylalanine, serine, alanine, tyrosine, threonine, proline, hydroxyproline, tryptophan, methionine, cystine, aspartic acid, arginine, glutamic acid, glutamine, lysine, arginine,
Histidine, trimethylglycine, glutathione.

The amount of the above specified compound incorporated into the external preparation for skin is 0.001% by weight or more, preferably 0.001% by weight or more.
It is 5 to 10% by weight.

In addition to the above-mentioned essential constituents, the external preparation for skin of the present invention contains other components usually used in external preparations for skin such as cosmetics and pharmaceuticals, for example, powder components, liquid oils and fats, solid oils and fats, waxes and hydrocarbons. , Higher fatty acids, higher alcohols, esters, silicones, anionic surfactants, cationic surfactants, amphoteric surfactants, nonionic surfactants, humectants, water-soluble polymer compounds, thickeners, film agents, ultraviolet rays Absorbents, sequestering agents, lower alcohols, polyhydric alcohols, sugars, amino acids, organic amines, synthetic resin emulsions, pH adjusting agents, skin nutrients, vitamins, antioxidants, antioxidant aids, fragrances, Water and the like can be appropriately added as needed, and the compound can be produced by a conventional method depending on the intended dosage form. The specific ingredients that can be mixed are listed below.
The external preparation for skin of the present invention can be prepared by blending the above essential ingredients and one or more of the following ingredients.

The powder components include talc, kaolin, mica, sericite, muscovite, phlogopite, synthetic mica, phlogopite, biotite, lithia mica, permiculite,
Magnesium carbonate, calcium carbonate, aluminum silicate, barium silicate, calcium silicate, magnesium silicate, strontium silicate, tungstate metal salt, magnesium, silica, zeolite, barium sulfate, calcined calcium sulfate, (calculated gypsum), calcium phosphate , Fluorapatite, Hydroxyapatite, Ceramic powder, Metal soap (Zinc myristate, Calcium palmitate, Aluminum stearate), Inorganic powder such as boron nitride, Polyamide resin powder (Nylon powder), Polyethylene powder, Polymethylmethacrylate powder, Polystyrene powder, styrene-acrylic acid copolymer resin powder, benzoguanamine resin powder, polytetrafluoroethylene powder, organic powder such as cellulose powder, titanium dioxide, inorganic white such as zinc oxide Pigments, iron oxide (red iron oxide),
Inorganic red pigments such as iron titanate, inorganic brown pigments such as γ-iron oxide, yellow iron oxide, inorganic yellow pigments such as ocher black iron oxide, carbon black, inorganic black pigments such as low order titanium oxide, Inorganic purple pigments such as mango violet and cobalt violet, inorganic green pigments such as chromium oxide, chromium hydroxide and cobalt titanate, inorganic blue pigments such as ultramarine blue and navy blue, titanium oxide coated mica, titanium oxide coated bismuth oxychloride. , Titanium oxide coated talc, colored titanium oxide coated mica, bismuth oxychloride, pearl pigments such as fish scale foil, aluminum powder,
Metal powder pigments such as copper powder, Red No. 201, Red No. 202, Red No. 204, Red No. 205, Red 220
No., Red 226, Red 228, Red 405, Orange 203, Orange 204, Yellow 205, Yellow 401
And organic pigments such as Blue No. 404, Red No. 3, Red No. 104, Red No. 106, Red No. 227, Red No. 230
No., Red No. 401, Red No. 505, Orange No. 205, Yellow No. 4, Yellow No. 5, Yellow No. 202, Yellow No. 203, Green No. 3
And organic pigments such as barium or aluminum lakes such as No. 1 and Blue No. 1 and natural pigments such as chlorophyll and β-carotene. However, the powder is not limited to the above components as long as it is a powder applicable to general cosmetics.

The liquid oils and fats include avocado oil, camellia oil, turtle oil, macadamia nut oil, corn oil, mink oil, olive oil, rapeseed oil, egg yolk oil, sesame oil, persic oil, wheat germ oil, southern oil, castor oil, linseed oil. Oil, safflower oil, cottonseed oil, eno oil, soybean oil, peanut oil, teaseed oil, kaya oil, rice bran oil, cinnamon oil, Japanese kiri oil, jojoba oil, germ oil, triglycerin,
Examples thereof include glycerin trioctanoate and glycerin triisopalmitate.

Examples of solid fats and oils include cacao butter, coconut oil, horse fat, hardened coconut oil, palm oil, beef tallow, sheep fat, hardened beef tallow, palm kernel oil, pork fat, beef bone fat, sorghum kernel oil, hardened oil, Examples include beef tallow, mokuro, hydrogenated castor oil, and the like.

Examples of waxes include beeswax, candelilla wax, cotton wax, carnauba wax, bayberry wax, ivowa wax, whale wax, montan wax, nuka wax, lanolin, capock wax, lanolin acetate, liquid lanolin, sugar cane wax, lanolin fatty acid isopropyl, hexyl laurate, and reduction. Lanolin, jojoba wax, hard lanolin, shellac wax, POE lanolin alcohol ether, POE lanolin alcohol acetate, POE cholesterol ether, lanolin fatty acid polyethylene glycol, POE hydrogenated lanolin alcohol ether and the like can be mentioned.

Examples of the hydrocarbon oil include liquid paraffin, ozokerite, squalene, pristane, paraffin, ceresin, squalene, petrolatum and microcrystalline wax.

Examples of the higher fatty acid include lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, 12-hydroxystearic acid, undecylenic acid, tall acid, isostearic acid, linoleic acid and linolein. Acid, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and the like.

The higher alcohols include, for example, straight chain alcohols such as lauryl alcohol, cetyl alcohol, stearyl alcohol, behenyl alcohol, myristyl alcohol, oleyl alcohol and cetostearyl alcohol, monostearyl glycerin ether (batyl alcohol), 2-decyltetradecyl alcohol. Examples thereof include branched chain alcohols such as knoll, lanolin alcohol, cholesterol, phytosterol, hexyldodecanol, isostearyl alcohol, and octyldodecanol.

The 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, 1
Cholesteryl 2-hydroxystearate, 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, trimethylolpropane triisostearate, cetyl 2-ethylhexanoate, 2-ethylhexyl palmitate, glycerin trimyristate, glyceride tri-2-heptylundecanoate, castor oil fatty acid methyl ester, oleic acid oil, cetostearyl alcohol , Acetoglyceride, 2-heptylundecyl palmitate, diisobutyl adipate, N-lauroyl-L-glutamic acid-2-octyldodecyl ester, di-2-heptylundecyl adipate, ethyl laurate, di-2 sebacate -Ethylhexyl, 2-hexyldecyl myristate, palmitic acid
Examples thereof include 2-hexyldecyl, 2-hexyldecyl adipate, diisopropyl sebacate, 2-ethylhexyl succinate, ethyl acetate, butyl acetate, amyl acetate, triethyl citrate and the like.

Examples of the silicone include chain polysiloxanes such as dimethylpolysiloxane, methylphenylpolysiloxane, and methylhydrogenpolysiloxane, cyclic chains such as decamethylpolysiloxane, dodecamethylpolysiloxane, and tetramethyltetrahydrogenpolysiloxane. Examples thereof include polysiloxane, a silicone resin having a three-dimensional network structure, silicone rubber, and a trimethylsiloxysilicic acid-octamethylcyclotetrasiloxane solution (50%).

Examples of the anionic surfactant include a soap base, a fatty acid soap such as sodium laurate and sodium palmitate, a higher alkyl sulfate ester salt such as sodium lauryl sulfate and potassium lauryl sulfate, and POE-triethanolamine lauryl sulfate. , POE-alkyl ether sulfate salts such as sodium lauryl sulfate, N-acyl sarcosinic acid such as sodium lauroyl sarcosine, N-myristoyl-N-methyl taurine sodium, coconut oil fatty acid methyl tauride sodium, sodium lauryl methyl tauride etc. Higher fatty acid amide sulfonate, POE-sodium oleyl ether phosphate, POE-phosphate ester salts such as stearyl ether phosphate, sodium di-2-ethylhexyl sulfosuccinate,
Monolauroyl monoethanolamide sodium polyoxyethylene sulfosuccinate, sulfosuccinates such as sodium lauryl polypropylene glycol sulfosuccinate, sodium linear dodecylbenzene sulfonate,
Alkylbenzene sulfonates such as linear dodecylbenzene sulfonic acid triethanolamine, linear dodecyl benzene sulfonic acid, monosodium N-lauroyl glutamate, disodium N-stearoyl glutamate,
N-myristoyl-L-monosodium glutamate and other N-
Acyl glutamate, higher fatty acid ester sulfate ester salt such as hydrogenated coconut oil fatty acid glycerin sodium sulfate,
Sulfated oil such as funnel oil, POE-alkyl ether carboxylic acid, POE-alkyl allyl ether carboxylate, α-olefin sulfonate, higher fatty acid ester sulfonate, secondary alcohol sulfate ester salt, higher fatty acid alkylolamide Examples thereof include sulfate ester salts, sodium lauroyl monoethanolamide succinate, ditriethanolamine N-palmitoyl aspartate, and sodium caseinate.

Examples of the cationic surfactant include alkyltrimethylammonium salts such as stearyltrimethylammonium chloride and lauryltrimethylammonium chloride, distearyldimethylammonium dialkyldimethylammonium chloride and poly (N, N'-dimethyl chloride).
-3,5-methylenepiperidinium), an alkylpyridinium salt such as cetylpyridinium chloride, an alkyl quaternary ammonium salt, an alkyldimethylbenzylammonium salt, an alkylisoquinolinium salt, a dialkylmorphonium salt, a POE-alkylamine, Examples thereof include alkylamine salts, polyamine fatty acid derivatives, amyl alcohol fatty acid derivatives, benzalkonium chloride and benzethonium chloride.

Examples of the amphoteric surfactant include 2-undecyl-N, N, N- (hydroxyethylcarboxymethyl) -2-
Imidazoline amphoteric surfactants such as sodium imidazoline, 2-cocoyl-2-imidazolinium hydroxide-1-carboxyethyloxy disodium salt, 2-heptadecyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine And betaine-based surfactants such as lauryl dimethylamino acetic acid betaine, alkyl betaine, amidobetaine and sulfobetaine.

Examples of lipophilic nonionic surfactants include sorbitan monooleate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan sesquioleate, sorbitan trioleate, Penta-2-ethylhexyl diglycerol sorbitan,
Tetra-2-ethylhexylate diglycerol sorbitan and other sorbitan fatty acid esters, monocotton oil fatty acid glycerin, glyceryl monoerucate, glyceryl sesquioleate, glyceryl monostearate, α, α'-glyceryl pyroglutamate oleate, glyceryl monostearate Examples thereof include glycerin polyglycerin fatty acid such as malic acid, propylene glycol fatty acid ester such as propylene glycol monostearate, hydrogenated castor oil derivative, and glycerin alkyl ether.

Examples of the hydrophilic nonionic surfactant include POE-sorbitan monooleate, POE-sorbitan monostearate, POE-sorbitan monooleate, POE-sorbitan tetraoleate, and other POE-sorbitan fatty acid esters, POE-sorbit monolaurate, POE-sorbit monooleate, POE-sorbit pentaoleate, POE-sorbit monostearate, and other POE sorbit fatty acid esters, POE-glycerin monostearate, POE-glycerin monoisostearate, POE-glycerin triisostearate and other POE-glycerin fatty acid esters, POE-monooleate, POE-distearate,
POE-monodioleate, POE-fatty acid esters such as ethylene glycol distearate, POE-lauryl ether, POE-oleyl ether, POE-stearyl ether,
POE-behenyl ether, POE-2-octyldodecyl ether, POE-cholestanol ether and other POE-alkyl ethers, POE-octylphenyl ether, POE-nonylphenyl ether, POE-dinonylphenyl ether and other PO
E-alkyl phenyl ethers, Pluronic types such as Bourronic, POE ・ POP-cetyl ether, POE ・ POP-
2-decyl tetradecyl ether, POE ・ POP-monobutyl ether, POE ・ POP-hydrogenated lanolin, POE ・ POP-glycerin ether and other POE ・ POP-alkyl ethers, Tetronic etc., tetra-POE ・ tetraPOP-ethylenediamine condensation Substances, POE-castor oil, POE-hardened castor oil, POE-hardened castor oil monoisostearate, POE-hardened castor oil triisostearate, POE-hardened castor oil monopyroglutamic acid monoisostearate diester, POE-hardened Castor oil Maleic acid and other POE-Castor oil Hardened castor oil derivative, POE-
POE- beeswax lanolin derivatives such as sorbit beeswax, coconut oil fatty acid diethanolamide, lauric acid monoethanolamide, alkanolamides such as fatty acid isopropanolamide, POE-propylene glycol fatty acid ester, POE-alkylamine, POE-fatty acid amide, sucrose Examples thereof include fatty acid ester, POE-nonylphenylformaldehyde condensate, alkylethoxydimethylamine oxide, trioleylphosphoric acid and the like.

Examples of moisturizers include polyethylene glycol, propylene glycol, glycerin, 1,3-butylene glycol, xylitol, sorbitol, maltitol, chondroitin sulfate, hyaluronic acid, mucoitin sulfate, caronic acid, atelocollagen, cholesteryl-12-. Examples thereof include hydroxy stearate, sodium lactate, bile salts, dl-pyrrolidone carboxylate, short-chain soluble collagen, diglycerin (EO) PO adduct, Isaioba rose extract, Yarrow millet extract and Merrilot extract.

Examples of natural water-soluble polymers include, for example, araavia gum, tragacanth gum, galactan, guar gum, carob gum, karaya gum, carrageenan, pectin, agar, quince seed (quince), arge colloid (cassius extract), starch (rice, corn, Potato, wheat), plant-based polymers such as glycyrrhizinate, microbial-based polymers such as xanthan gum, dextran, succinoglucan, and vullan, collagen,
Animal-based polymers such as casein, albumin and gelatin can be mentioned.

As the semi-synthetic water-soluble polymer, for example,
Starch-based polymers such as carboxymethyl starch, methyl hydroxypropyl starch, methyl cellulose, nitrocellulose, ethyl cellulose, methyl hydroxypropyl cellulose, hydroxyethyl cellulose, sodium cellulose sulfate, hydroxypropyl cellulose, carboxymethyl cellulose, sodium carboxymethyl cellulose, crystalline cellulose, cellulose Examples thereof include cellulosic polymers such as powder, and alginic acid polymers such as sodium alginate and propylene glycol alginate.

Examples of the synthetic water-soluble polymer include polyvinyl alcohol, polyvinyl methyl ether, polyvinylpyrrolidone, vinyl polymers such as carboxyvinyl polymer (Carbopol), and polyethylene glycol.
Polyoxyethylene-based polymers such as 20,000, 40,000 and 60,000, polyoxyethylene-polyoxypropylene copolymer copolymer-based polymers, sodium-acrylate, polyethyl acrylate, acrylic polymers such as polyacrylamide, polyethyleneimine, Examples include cationic polymers.

Examples of the inorganic water-soluble polymer include bentonite, silicic acid A1Mg (veegum), laponite, hectorite, silicic acid anhydride and the like.

Examples of the thickener include gum arabic,
Carrageenan, karaya gum, tragacanth gum, carob gum, quince seed (quince), casein, dextrin, gelatin, sodium pectate, sodium alginate, methyl cellulose, ethyl cellulose,
CMC, hydroxyethyl cellulose, hydroxypropyl cellulose, PVA, PVM, PVP, sodium polyacrylate, carboxyvinyl polymer, locust bean gum, guar gum, tamarind gum, dialkyldimethylammonium sulfate cellulose, xanthan gum, magnesium aluminum silicate, bentonite,
Hectorite and the like can be mentioned.

Examples of the ultraviolet absorber include para-aminobenzoic acid (hereinafter abbreviated as PABA), PABA monoglycerin ester, N, N-dipropoxy PABA ethyl ester, N,
N-diethoxy PABA ethyl ester, N, N-dimethyl PABA ethyl ester, N, N-dimethyl PABA butyl ester, N, N-
Benzoic acid-based UV absorbers such as dimethyl PABA ethyl ester, anthranilate-based UV absorbers such as homomenthyl-N-acetylanthranilate, amyl salicylate, menthyl salicylate, homomenthyl salicylate, octyl salicylate, phenyl salicylate, benzyl salicylate, p -Salicylic acid type UV absorbers such as isopropanol phenyl salicylate, octyl cinnamate, ethyl-4-isopropyl cinnamate, methyl-2,5-
Diisopropylcinnamate, ethyl-2,4-diisopropylcinnamate, methyl-2,4-diisopropylcinnamate, propyl-p-methoxycinnamate, isopropyl-p-methoxycinnamate, isoamyl-p-methoxycinnamate, octyl- p-methoxycinnamate (2-ethylhexyl-p-methoxycinnamate), 2-ethoxyethyl-p-methoxycinnamate, cyclohexyl-p-methoxycinnamate, ethyl-α-cyano-β-phenylcinnamate, 2- Ethylhexyl-α-cyano-β-phenylcinnamate, glyceryl mono-2-ethylhexanoyl-
Cinnamic acid type UV absorbers such as diparamethoxycinnamate, 2,4-dihydroxybenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone, 2,2'-dihydroxy-
4,4'-dimethoxybenzophenone, 2,2 ', 4,4'-tetrahydroxybenzophenone, 2-hydroxy-4-methoxybenzophenone, 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-carboxy Benzophenone-based UV absorbers such as benzophenone, 3- (4'-methylbenzylidene) -d, l-camphor, 3-benzylidene-d, l-camphor, urocanic acid, urocanic acid ethyl ester, 2-phenyl-5-methyl Benzoxazole, 2,2'-hydroxy-5
-Methylphenylbenzotriazole, 2- (2'-hydroxy-5'-t-octylphenyl) benzotriazole, 2-
(2'-hydroxy-5'-methylphenylbenzotriazole, dibenzalazine, dianisoylmethane, 4-methoxy
-4'-t-butyldibenzoylmethane, 5- (3,3-dimethyl-2-
Norbornylidene) -3-pentan-2-one and the like.

Examples of the sequestering agent include 1-hydroxyethane-1,1-diphosphonic acid, 1-hydroxyethane-1,1-diphosphonic acid tetrasodium salt, edetate disodium, edetate trisodium, and edet. Tetrasodium acid, sodium citrate, sodium polyphosphate, sodium metaphosphate, gluconic acid, phosphoric acid, citric acid,
Examples thereof include ascorbic acid, succinic acid, edetic acid, trisodium ethylenediamine hydroxyethyl triacetate and the like.

As the lower alcohol, for example, methanol, ethanol, propanol, isopropanol,
Examples thereof include isobutyl alcohol and t-butyl alcohol.

Examples of polyhydric alcohols are ethylene glycol, propylene glycol, trimethylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, tetramethylene glycol, 2,3-butylene glycol, pentamethylene. Glycol, 2-butene-1,4-diol, dihydric alcohol such as hexylene glycol and octylene glycol, trihydric alcohol such as glycerin, trimethylolpropane and 1,2,6-hexanetriol, pentaerythritol. Etc., tetravalent alcohols such as xylitol, hexavalent alcohols such as sorbitol, mannitol, diethylene glycol, dipropylene glycol, triethylene glycol, polypropylene glycol, tetraethylene glycol, diglycerin, polyethylene glycol. Polyol, triglycerin, tetraglycerin, polyglycerin and other polyhydric alcohol polymers, ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, ethylene glycol monobutyl ether, ethylene glycol monophenyl ether, ethylene glycol monohexyl ether,
Dihydric alcohol alkyl ethers such as ethylene glycol mono 2-methylhexyl ether, ethylene glycol isoamyl ether, ethylene glycol benzyl ether, ethylene glycol isopropyl ether, ethylene glycol dimethyl ether, ethylene glycol diethyl ether, ethylene glycol dibutyl ether, diethylene glycol monomethyl ether , Diethylene glycol monoethyl ether, diethylene glycol monobutyl ether, diethylene glycol dimethyl ether, diethylene glycol diethyl ether, diethylene glycol butyl ether, diethylene glycol methyl ethyl ether, triethylene glycol monomethyl ether, triethylene glycol monoethyl ether, Dihydric alcohol alkyl ethers such as ropylene glycol monomethyl ether, propylene glycol monoethyl ether, propylene glycol monobutyl ether, propylene glycol isopropyl ether, dipropylene glycol methyl ether, dipropylene glycol ethyl ether and dipropylene glycol butyl ether, ethylene glycol monomethyl ether Acetate, ethylene glycol monoethyl ether acetate, ethylene glycol monobutyl ether acetate, ethylene glycol monophenyl ether acetate, ethylene glycol diadibate, ethylene glycol disuccinate, diethylene glycol monoethyl ether state, diethylene glycol monobutyl ether acetate , Dihydric alcohol ether esters such as propylene glycol monomethyl ether acetate, propylene glycol monoethyl ether acetate, propylene glycol monopropyl ether acetate, propylene glycol monophenyl ether acetate, etc., glycerin monoalkyl such as xyl alcohol, ceracyl alcohol, batyl alcohol, etc. Ether, sorbitol, maltitol, maltotriose, mannitol, sucrose, erythritol,
Glucose, fructose, starch-decomposing sugar, maltose, xylitol, sugar-decomposing sugar such as reducing alcohol, glycolid, tetrahydrofurfuryl alcohol, POE-tetrahydrofurfuryl alcohol, POP-butyl ether, POP / POE-butyl ether,
Tripolyoxypropylene glycerin ether, POP-glycerin ether, POP-glycerin ether phosphoric acid, PO
P • POE-pentane erythritol ether and the like can be mentioned.

Examples of monosaccharides include tricarbon sugars such as D-glyceryl aldehyde and dihydroxyacetone, tetracarbon sugars such as D-erythrose, D-erythrulose, D-threose and erythritol, L-arabinose and D-xylose. L-lyxose, D-arabinose, D-ribose, D-ribulose,
Pentose sugars such as D-xylulose and L-xylulose, D-glucose, D-talose, D-busicose, D-galactose, D-
Fructose, L-galactose, L-mannose, D-tagatose and other hexoses, aldoheptose, heptulose and other heptasaccharides, octulose and other octoses, 2-deoxy-D-ribose, 6-deoxy-L-galactose , Deoxy sugars such as 6-deoxy-L-mannose, D-glucosamine, D-galactosamine, sialic acid, aminouronic acid, amino sugars such as muramic acid, D-glucuronic acid, D-mannuronic acid, L-guluronic acid, D -Examples include uronic acids such as galacturonic acid and L-iduronic acid.

Examples of oligosaccharides include sucrose, guanthianose, umbelliferose, lactose, planteose, isoliknoses, α, α-trehalose,
Raffinose, lychnose, umbilicin, stachyose bell bass course, etc. may be mentioned.

Examples of the polysaccharides include cellulose, quince seed, chondroitin sulfate, starch, galactan, dermatan sulfate, glycogen, gum arabic, heparan sulfate, hyaluronic acid, tragacanth gum, keratan sulfate, chondroitin, xanthan gum, mucoitin sulfate, guar gum and dextran. , Keratosulfate, locust bingham, succinoglucan, caronic acid and the like.

Examples of the amino acids include neutral amino acids such as threonine and cysteine, and basic amino acids such as hydroxylysine. Examples of the amino acid derivative include sodium acyl sarcosine (sodium lauroyl sarcosine), acyl glutamate, sodium acyl β-alanine, glutathione, and pyrrolidone carboxylic acid.

Examples of the organic amine include monoethanolamine, diethanolamine, triethanolamine, morpholine, triisopropanolamine, 2-amino-2-methyl-1,3-propanediol, 2-amino-2-methyl-1. -Propanol and the like can be mentioned.

As the synthetic resin emulsion, for example,
Examples thereof include acrylic resin emulsion, polyethyl acrylate emulsion, acrylic resin solution, polyacrylic alkyl ester emulsion, and polyvinyl acetate resin emulsion.

Examples of the pH adjusting agent include buffers such as lactic acid-sodium lactate and citric acid-sodium citrate.

Examples of vitamins include vitamins A, B1, B2, B6, E and derivatives thereof, pantothenic acid and derivatives thereof, biotin and the like.

Examples of the antioxidant include tocopherols, dibutylhydroxytoluene, butylhydroxyanisole, gallic acid esters and the like.

As the antioxidant aid, for example, phosphoric acid,
Examples thereof include citric acid, ascorbic acid, maleic acid, malonic acid, succinic acid, fumaric acid, kephalin, hexametaphosphate, phytic acid and ethylenediaminetetraacetic acid.

Other components that can be blended include preservatives such as ethylparaben and butylparaben, glycyrrhizic acid derivatives, glycyrrhetinic acid derivatives, salicylic acid derivatives, and the like.
Anti-inflammatory agents such as hinokitiol, zinc oxide, allantoin,
Whitening agents such as placenta extract, Yukinoshita extract, psyllium,
Coptis, Sikon, Peony, Assemblage, Birch, Sage, Loquat, Carrot, Aloe, Mallow, Iris, Grape, Yokuinin, Loofah, Lily, Saffron, Senkyu, Ginger, Hypericum, Ononis, Garlic, Capsicum, Chimp, Toki, Seaweed Extract such as royal jelly, photosensitizer, cholesterol derivative,
Activator such as infant blood extract, nonyl acid warenylamide,
Nicotinic acid benzyl ester, nicotinic acid β-butoxyethyl ester, capsaicin, zingerone, cantharisin tincture, ictamol, tannic acid, α-borneol, nicotinic acid tocopherol, inositol hexanicotinate, cyclanderate, cinnarizine, tolazoline, acetylcholine, verapamil , Cepharanthin,
Examples include blood circulation promoters such as γ-oryzanol, antiseborrheic agents such as sulfur and thiantol, tranexamic acid, thiotaurine, and hypotaurine.

The dosage form of the external preparation for skin of the present invention is arbitrary,
For example, a solubilizing system such as lotion, an emulsifying system such as emulsion or cream, or an arbitrary dosage form such as ointment or dispersion can be employed.

[0055]

EXAMPLES Next, the present invention will be described in more detail with reference to examples. The present invention is not limited to this. The blending amount is% by weight. Prior to the examples, the effect test method and evaluation method of the present invention will be described.

(1) Lipid-degrading effect test and evaluation method Adipocytes were isolated from adipose tissue by the method of Rodbell (M.
Rodbell, J. B. C. , 239 (2), 1964). Human adipose tissue obtained by liposuction into 2-3 mm strips,
Incubation (37 ° C, 45-60) in 0.05% collagenase solution (Banks buffer, containing 4% glucose).
Minutes) Then, it was filtered to remove undigested adipose tissue and centrifuged (1000 rpm, 1 minute). Since the specific gravity of adipocytes is less than 1, they float above. The lower layer solution was removed, a culture solution (199 medium, containing 10% newborn calf serum) was added, and redispersed. The centrifugation and medium addition were repeated twice to remove collagenase. Finally, add 30 ml of the medium described in Table 1,
After dispersing the cells, the cells were cultivated for 1 day in rotation. In each sample, the xanthine derivative was 0.2% by weight and the specific compound was 0.5% by weight. The lipid content of adipocytes before and after the culture was quantified using Triglyceride-Test Wako (Wako Pure Chemical Industries, Ltd.) (color reagent for lipid quantification) to measure the amount of degraded lipid (mg / tube). The measurement results are shown in "Table 1".

[0057]

[Table 1] -------------------------------------------------- ---------------------           Sample Degraded lipid amount (mg / tube) -------------------------------------------------- ---------------------           Not added 1.20 ± 0.18 -------------------------------------------------- ---------------------        Caffeine 3.50 ± 0.56 -------------------------------------------------- ---------------------        Caffeine + erythritol + trimethylglycine 8.25 ± 0.20 -------------------------------------------------- ---------------------        Aminophylline + hyaluronic acid        + Serine 8.65 ± 0.35 -------------------------------------------------- ---------------------        Caffeine + erythritol + L-serine        + Trimethylglycine 7.45 ± 0.89 -------------------------------------------------- ---------------------

From Table 1, it can be seen that the lipolytic effect is promoted when the xanthine derivative, the polysaccharide and the specific compound are blended.

(2) Lipid metabolism promoting effect test, skin roughening improving effect test and evaluation method 100 women in their 20s to 30s were applied to the whole body in the morning and evening with the massage gel of Example 7 to be described later and continued for 2 months. Measuring device based on the principle of light reflection of external infrared wavelengths (body fat meter BFT-200) before and after continuous use.
0, manufactured by Kett Scientific Co., Ltd.). 40 out of 100 were used as a control group from which erythritol, caffeine, and trimethylglycine were removed, and the average value of each body fat percentage was calculated. The results are shown in "Table 3". In addition, the degree of rough skin of the legs was evaluated in four levels according to the evaluation criteria of "Table 2", and the results are shown in "Table 4".

[0060]

[Table 2] "Roughness of the skin" -------------------------------------------------- --------------     Score observation state -------------------------------------------------- --------------       0 No rough skin on the legs       1 The skin is slightly rough on one leg       2 There is rough skin on the legs       3 The skin is rough as if all the legs were dusted -------------------------------------------------- --------------

[0061]

[Table 3] "Changes in body fat percentage" -------------------------------------------------- --------------                             Before continuous use After continuous use -------------------------------------------------- --------------   Control 35.5 ± 7.2% 35.2 ± 4.0%   Example 7 36.2 ± 4.2% 32.6 ± 8.8% -------------------------------------------------- --------------

[0062]

[Table 4] "Rough skin improvement effect" -------------------------------------------------- --------------                             Before continuous use After continuous use -------------------------------------------------- --------------   Control 3.1 ± 1.5 3.5 ± 1.2   Example 7 3.3 ± 1.9 2.2 ± 1.6 -------------------------------------------------- --------------

As is clear from the results of "Table 3" and "Table 4," the examples of the present invention have a lower body fat percentage and a remarkable effect of improving rough skin in comparison with the control.

Examples of the external preparation for skin of the present invention will be shown below.

Example 1 Cream (1) 3.5% by weight cetostearyl alcohol (2) Squalane 40.0 (3) Beeswax 3.0 (4) Reduced lanolin 5.0 (5) Ethylparaben 0.3 (6) ) Polyoxyethylene (20) sorbitan monopalmitate 2.0 (7) Stearic acid monoglyceride 2.0 (8) Sodium N-stearoylglutamate 0.5 (9) 2-Hydroxy-4-methoxybenzophenone 1.0 ( 10) Fragrance 0.05 (11) Caffeine 1.0 (12) Trimethylglycine 0.2 (13) 1,3-Butylene glycol 0.1 (14) Erythritol 0.5 (15) Purified water Residue (Production method) (1) to (10) were melted by heating and heated to 70 ° C (1
Add to 1) to (15) while stirring. The mixture was treated with a homomixer to make the emulsified particles finer, and then rapidly cooled with stirring to obtain a cream.

Example 2 Lotion (1) Caffeine 0.5% by weight (2) Trimethylglycine 0.5 (3) Erythritol 0.1 (4) Glycerin 4.0 (5) 1,3-Butylene glyco- 4.0 (6) Tocopherol acetate 0.05 (7) Ethanol 7.0 (8) Polyoxyethylene (18) Oleyl alcohol ether 0.5 (9) Methylparaben 0.2 (10) Citric acid 0.05 ( 11) Sodium citrate 0.1 (12) Ethylenediaminetetraacetic acid trisodium 0.02 (13) Perfume 0.05 (14) Purified water Residual (manufacturing) purified water (1) to (5), (10) Dissolve ~ (12) (aqueous phase). Separately from (7) to (6), (8),
(9) and (13) were dissolved, and this was added to the aforementioned aqueous phase to solubilize it, and filtered to obtain a lotion.

Example 3 Emulsion (1) Stearic Acid 1.5% by Weight (2) Cetyl Alcohol 0.5 (3) Beeswax 2.0 (4) Polyoxyethylene (10) Monooleate 1.0 (5) ) Octyl methoxycinnamate 2.0 (6) Caffeine 0.2 (7) L-serine 0.5 (8) Sodium hyaluronate 0.01 (9) Triethanolamine 0.75 (10) Glycerin 7. 0 (11) inosit 0.5 (12) 1,3-butylene glycol 0.5 (13) DL-alanine 0.2 (14) ethylenediamine hydroxyethyl triacetate trisodium 0.01 (15) ethylparaben 0.3 (16) Fragrance 0.03 (17) Purified water Add (6) to (14) to the residue (production method) (17) and keep at 70 ° C (aqueous phase). Other ingredients are mixed, dissolved by heating and kept at 70 ° C (oil phase). The oil phase is added to the aqueous phase for preliminary emulsification, and the mixture is uniformly emulsified with a homomixer. Then, it was rapidly cooled with stirring to obtain an emulsion.

Example 4 Foam pack (1) L-arginine 0.1% by weight (2) Caffeine 1.0 (3) DL-serine 0.2 (4) Sodium metaphosphate 0.02 (5) Trehalose 2 .0 (6) Glycerin 7.0 (7) Methylparaben 0.1 (8) Potassium hydroxide 0.15 (9) Stearic acid 0.5 (10) Myristic acid 1.0 (11) Batyl alcohol 1.5 ( 12) Polyoxyethylene (60) Hydrogenated castor oil 3.0 (13) Perfume 0.05 (14) Liquefied petroleum gas 6.0 (15) Dimethyl ether 3.0 (16) Purified water Residue (production method) (16) (1) to (8) are added to and dissolved by heating at 70 ° C, and (9) to (13) heated and stirred at 75 ° C are added thereto, and the mixture is sufficiently stirred and then cooled. This was filled in a container, and finally (14) and (15) were filled as a propellant to obtain a foam pack.

Example 5 Ointment (1) Caffeine 10.0 wt% (2) Rosemary Extract 1.0 (3) Trehalose 0.2 (4) Trimethylglycine 0.2 (5) Ethylenediaminehydroxyethyl triacetic acid Trisodium 0.01 (6) Retinol palmitate 0.5 (7) Stearyl alcohol 18.0 (8) Moku 20.0 (9) Polyoxyethylene (20) monooleate 0.25 (10) Glycerin mono Stearic acid ester 0.3 (11) Vaseline 40.0 (12) Purified water Add (1) to (5) to the residue (production method) (12), dissolve and maintain at 70 ° C (aqueous phase). The remaining components (6) to (11) are mixed and dissolved at 70 ° C (oil phase). The oil phase was added to the aqueous phase, and the mixture was uniformly emulsified with a homomixer and then cooled to obtain an ointment.

Example 6 Emulsion for massage (1) Stearic acid 1.5% by weight (2) Cetyl alcohol 0.5 (3) Polyoxyethylene (10) monooleate 1.0 (4) Vaseline 3.0 (5) Squalane 10.0 (6) Liquid paraffin 5.0 (7) Glycerin 7.0 (8) Glutathione 0.2 (9) Triethanolamine 0.75 (10) L-serine 0.05 (11) Caffeine 1.0 (12) Green tea extract 3.0 (13) Trehalose 2.0 (14) Sodium metaphosphate 0.02 (15) Ethylenediaminehydroxyethyl trisodium trisodium 0.01 (16) Ethylparaben 0. 25 (17) Perfume 0.02 (18) Purified water Add (7) to (15) to the residue (production method) (18) and keep at 70 ° C (aqueous phase). Other ingredients are mixed, dissolved by heating and kept at 70 ° C (oil phase). The oil phase is added to the aqueous phase for preliminary emulsification, and the mixture is uniformly emulsified with a homomixer. Then, it was rapidly cooled with stirring to obtain a milky lotion for massage.

Example 7 Massage Gel (1) Erythritol 2.0% by Weight (2) Caffeine 5.0 (3) Oat Extract 3.0 (4) Glycerin 50.0 (5) Trimethylglycine 0.2 (6) Carboxyvinyl polymer 0.40 (7) Polyethylene glycol 400 30.0 (8) Ethylenediamine hydroxyethyl trisodium triacetate 0.1 (9) Polyoxyethylene (10) methylpolysiloxane copolymer 2.0 (10) Squalane 1.0 (11) Perfume 0.12 (12) Potassium hydroxide 0.15 (13) Purified water Dissolve (1) to (8) in the residue (production method) (13). Apart (9)
After adding a mixture of ~ (11), (12) was added to obtain a massage gel.

Example 8 Beauty Serum (1) Caffeine 5.0% by Weight (2) Tranexamic Acid 1.0 (3) Rosemary Extract 0.1 (4) L-Arginine L-Aspartate 0.1 (5) Sodium hyaluronate 0.01 (6) Glycerin 10.0 (7) Erythrilol 5.0 (8) Carboxyvinyl polymer 0.3 (9) Ethylenediamine hydroxyethyl trisodium triacetate 0.01 (10) Ethanol 7.0 (11) Polyoxyethylene (18) Oleyl alcohol ether 0.8 (12) Macadamia nut oil 0.1 (13) Evening primrose oil 0.01 (14) Tocopherol acetate 0.01 (15) Methylparaben 0.15 ( 16) Fragrance 0.1 (17) Potassium hydroxide 0.08 (18) Purified water Dissolve (1) to (9) in the residue (production method) (18) and separately into (10) (11) to ( Add the solution of 16). Then (1
7) was added to obtain a serum.

[0073]

EFFECTS OF THE INVENTION According to the present invention, an external preparation for skin having an extremely excellent lipid decomposition promoting effect and skin roughening improving effect can be provided.

─────────────────────────────────────────────────── ─── Continuation of the front page (56) References JP-A-8-26962 (JP, A) JP-A-8-12519 (JP, A) JP-A-3-279312 (JP, A) JP-A-7- 316075 (JP, A) JP 4-124118 (JP, A) JP 8-268866 (JP, A) JP 9-255552 (JP, A) JP 5-262636 (JP, A) (58) Fields investigated (Int.Cl. ⁷ , DB name) A61K 7/00

Claims (3)

(57) [Claims] 1. A xanthine derivative and erythritol,
A skin external preparation containing one or more polysaccharides selected from the group consisting of hyaluronic acid and salts thereof , and at least one of the specific compounds shown in the following (1). (1) Glycine, valine, leucine, isileucine, phenylalanine, serine, alanine, tyrosine, threonine, proline, hydroxyproline, tryptophan, methionine, cystine, aspartic acid, arginine, glutamic acid, glutamine, lysine, arginine,
Histidine, trimethylglycine, glutathione. 2. The xanthine derivative is caffeine,
It is one or more selected from the group consisting of theophylline, theobromine, xanthine, aminophylline, choline theophylline, diprophylline, proxyphylline and oxtriphylline.
The skin external preparation described. 3. The external preparation for skin according to claim 1, wherein the external preparation for skin is an external preparation for promoting lipid decomposition.