JP3513871B2 - Skin whitening external preparation - Google Patents

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin, more specifically, a cosmetic having an excellent whitening effect on the skin such as suppression of inflammation such as hot flashes and erythema of the skin after sunburn and prevention of pigmentation. , Skin external preparations such as external medicines.

[0002]

2. Description of the Related Art Conventionally, an external skin preparation such as an emulsion, a cream, a lotion, a pack, a dispersion, a detergent, an ointment, a cream or a liquid for external use has an object to impart a predetermined medicinal effect to them. As a medicinal ingredient is added. For example, in order to prevent skin darkening caused by sunburn etc., spots caused by pigmentation, freckles etc., such as calamine, ascorbic acid, glutathione, colloidal sulfur, hydroquinone, cinnamic aldehyde, placenta extract, etc. A whitening agent has been added. Furthermore, anti-inflammatory agents such as glycyrrhizic acid, indomethacin, aloe extract and chamomile extract are added for the purpose of suppressing inflammation such as hot flashes and erythema of the skin after sunburn and suppressing the occurrence of pigmentation. ing.

[0003]

However, in the external preparations for skin such as cosmetics and external medicines containing these whitening agents and / or anti-inflammatory agents, the performance of the whitening agents and / or anti-inflammatory agents is sufficiently exhibited. In many cases, the desired medicinal effect cannot be obtained due to the absence or deterioration in the formulation, and improvement thereof has been desired. The present invention has been made in view of the above circumstances, and for a skin external preparation containing a whitening agent and / or an anti-inflammatory agent, the performance of the whitening agent and / or the anti-inflammatory agent is sufficiently exhibited, and its stability is An object is to provide an improved external preparation for skin.

[0004]

[Means for Solving the Problems] The present inventors have conducted extensive studies to improve the effect of the medicinal component of a skin external preparation containing a whitening agent and / or an anti-inflammatory agent, and as a result, have combined it with an acerola extract. It was found that the action of the original whitening agent and / or anti-inflammatory agent is sufficiently exerted by the treatment, and the present invention has been completed.

That is, the present invention relates to a whitening skin external preparation containing the following components (A) and (B); (A) acerola extract (B) whitening agent and / or anti-inflammatory agent. Whitening agent
L-ascorbic acid sodium sulfate, L-as
Corbic acid phosphate magnesium, L-ascor
Sodium biphosphate phosphate, Licorice extract, Sodium
Select from Uhakuhi extract, Toki extract and placenta extract
At least one of the
Dipotassium tyrrhizinate, stearyl glycyrrhetinate
And an external preparation for whitening skin, which is at least one selected from chamomile extracts .

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION The acerola extract, which is the component (A) of the external whitening agent for whitening of the present invention, is of the genus Malpigia (Ma).
Acerola, scientific name Malpi
ghia emarginata DC; the scientific name of acerola is its time, region,
Also, the description in the paper differs depending on the researcher. Previously Malpighia punicifolia L. and Malpighia glabra L.
Has been confused as the scientific name of acerola, but currently Malpighia emarginata DC described in "TROPICAL AND SUBTROPICAL FRUITS" edited by Steven Nagy et al. In 1980 is the most suitable. Extraction is carried out from the fruit of 1) using an extraction solvent. The extraction process is
Although not particularly limited, it is extracted at a low temperature or room temperature or under heating with a suitable solvent.

Examples of the above-mentioned extraction solvent include one or more of water; lower monohydric alcohols such as methyl alcohol and ethyl alcohol; liquid polyhydric alcohols such as glycerin, propylene glycol and 1,3-butylene glycol. Can be used. As an example of a preferred extraction method, purified water is used for extraction at a low temperature, followed by filtration, and 1,3-butylene glycol is further mixed to a concentration of 20 to 70% (W / W). , And a method of performing filtration again.

The compounding amount (content) of the acerola extract in the whitening skin external preparation of the present invention is preferably 0.00005 to 5% by weight (hereinafter referred to as "% by weight") as a dry solid content.
Is simply represented by "%"), and more preferably 0.00
It is 05 to 1%. If the compounding amount (content) of this acerola extract is less than 0.00005%, a sufficient effect may not be obtained, and even if it exceeds 5%, the effect is further increased. Absent.

The component (B) of the whitening skin external preparation of the present invention is selected from whitening agents and / or anti-inflammatory agents. These can be used alone or in combination of two or more. Specific examples of the drug efficacy of the component (B) include the following. As a whitening agent,
L-ascorbic acid sodium sulfate, L-as
Corbic acid phosphate magnesium, L-ascor
Sodium biphosphate phosphate, Licorice extract, Sodium
Select from Uhakuhi extract, Toki extract and placenta extract
At least one of As an anti-inflammatory agent,
Dipotassium glycyrrhizinate, glycyrrhetinic acid steer
At least one selected from lily and chamomile extract
Can be mentioned.

The content of the above-mentioned component (B), a whitening agent and / or an anti-inflammatory agent, in the external preparation for skin of the present invention varies depending on the kind of the agent, but it is preferable that the content is within the following range. That is, the blending amount (content) of the whitening agent is preferably 0.00001 to 10%, more preferably 0.
It is 0001 to 5%, and the compounding amount (content) of the anti-inflammatory agent is preferably 0.00001 to 20%, more preferably 0.0001 to 10%. When a plant extract or the like is used as it is as an extract, the amount is a dry solid content. When the content of the whitening agent and / or the anti-inflammatory agent is within the above range, by combining with the acerola extract, the stability of the external preparation for skin can be improved with time without affecting the acerola extract in the external preparation for skin. It can improve and exhibit high whitening and anti-inflammatory effects.

The external preparation for skin of the present invention is prepared by blending the essential components (A) and (B) with various forms of bases known as ordinary external compositions according to a conventional method. be able to. The form of the external preparation for skin is not particularly limited, and examples thereof include emulsion, cream, lotion, pack,
It can be used as a skin care cosmetic such as a cleansing agent, a cosmetic such as lipstick or makeup cosmetic, or a drug such as an ointment, a dispersion, a cream or a liquid for external use, and the dosage form thereof is not particularly limited. Molds, pastes, mousses, gels, powders, solution systems, solubilization systems, emulsification systems, powder dispersion systems, and multilayers can be used.

In addition to the above-mentioned components (A) and (B), the external preparation for skin of the present invention generally contains cosmetics, quasi-drugs, external medicines, etc. within a range not impairing the effects of the present invention. Ingredients used in the formulation, namely water (purified water, hot spring water,
Deep water etc.), oil agent, surfactant, metal soap, gelling agent, powder, alcohols, water-soluble polymer, film forming agent,
Resins, UV protectors, inclusion compounds, antibacterial agents, fragrances, deodorants, salts, pH regulators, cooling agents, animal / microorganism derived extracts, plant extracts, blood circulation promoters, astringents, antiseborrheic agents , Active oxygen scavenger, cell activator, moisturizer, keratolytic agent, enzyme,
One kind or two or more kinds of hormones, vitamins and the like can be appropriately added.

The oil agent may be a natural oil, a synthetic oil, a solid, a semi-solid, or a liquid as long as it is used in ordinary cosmetics. ,
Any oil agent such as hydrocarbons, waxes, fatty acids, higher alcohols, ester oils, silicone oils, and fluorine-based oils can be used. For example, squalane, squalene, ceresin, paraffin, paraffin wax, liquid paraffin, pristane, polyisobutylene,
Hydrocarbons such as microcrystalline wax and vaseline; waxes such as beeswax, carnauba wax, candelilla wax, whale wax; beef tallow, beef leg fat, beef bone fat, hardened beef tallow, hardened oil, turtle oil, pork fat, horse fat , Animal oils such as mink oil, liver oil, egg yolk oil; lanolin, liquid lanolin, reduced lanolin, lanolin alcohol, hard lanolin, lanolin acetate, lanolin fatty acid isopropyl, POE lanolin alcohol ether, POE lanolin alcohol acetate, lanolin fatty acid polyethylene glycol, POE hydrogen Lanolin derivatives such as added lanolin alcohol ether; lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, undecylenic acid, oleic acid, arachidonic acid, docosahexaenoic acid (DHA), isostearic acid, 12-hydroxy Fatty acids such as stearic acid.

As an oil agent, lauryl alcohol,
Myristyl alcohol, palmityl alcohol, stearyl alcohol, behenyl alcohol, hexadecyl alcohol, oleyl alcohol, isostearyl alcohol, hexyldodecanol, octyldodecanol,
Cetostearyl alcohol, 2-decyltetradecinol, cholesterol, phytosterol, sitosterol, lanosterol, POE cholesterol ether,
Higher alcohols such as monostearyl glycerin ether (batyl alcohol); diisobutyl adipate, 2-hexyldecyl adipate, adipic acid-di-2-
Heptyl undecyl, mono-isostearate-N-alkyl glycol, isocetyl isostearate, trimethylolpropane triisostearate, ethylene glycol di-2-ethylhexanoate, cetyl 2-ethylhexanoate, trimethylol tri-2-ethylhexanoate. Propane, tetra-2-ethylhexanoate pentaerythritol, cetyl octanoate, octyldodecyl gum ester, oleyl oleate, octyldodecyl oleate, decyl oleate, neopentyl glycol dicaprate, triethyl citrate, 2-ethylhexyl succinate. , Amyl acetate, ethyl acetate, butyl acetate, isocetyl stearate, butyl stearate, diisopropyl sebacate, di-2-ethylhexyl sebacate,
Cetyl lactate, myristyl lactate, isopropyl palmitate, 2-ethylhexyl palmitate, 2-hexyldecyl palmitate, 2-heptylundecyl palmitate, cholesteryl 12-hydroxystearate, dipentaerythritol fatty acid ester, isopropyl myristate, myristin Octyldodecyl acid, 2-hexyldecyl myristate, myristyl myristate,
Examples include ester oils such as hexyldecyl dimethyloctanoate, ethyl laurate, hexyl laurate, N-lauroyl-L-glutamic acid-2-octyldodecyl ester, and diisostearyl malate.

Further, as an oil agent, acetoglyceride,
Triisooctanoic acid glyceride, triisostearic acid glyceride, triisopalmitic acid glyceride,
Glyceride oils such as tri-2-ethylhexanoic acid glyceride, monostearic acid glyceride, di-2-heptylundecanoic acid glyceride, trimyristate glyceride; dimethylpolysiloxane, methylphenylpolysiloxane, methylhydrogenpolysiloxane,
Higher alkoxy-modified silicone such as octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, dodecamethylcyclohexasiloxane, tetramethyltetrahydrogencyclotetrasiloxane, stearoxysilicone; higher fatty acid-modified silicone, silicone resin, silicone rubber, silicone oil Silicone-based oil agents such as; Fluorine-based oil agents such as perfluoropolyether, perfluorodecalin, and perfluorooctane.

As the surfactant, anionic, cationic, nonionic and amphoteric surfactants are used. As the anionic surfactant, sodium stearate,
Fatty acid soaps such as triethanolamine palmitate, alkyl ether carboxylic acids and salts thereof, carboxylates such as condensates of amino acids and fatty acids, alkyl sulfonic acids, alkene sulfonates, sulfonates of fatty acid esters, sulfones of fatty acid amides Acid salts, sulfonic acid salts of alkyl sulfonates and their formalin condensates, alkyl sulfuric acid ester salts, secondary higher alcohol sulfuric acid ester salts, alkyl and allyl ether sulfuric acid ester salts, sulfuric acid ester salts of fatty acid esters, fatty acid alkylolamides Sulfate ester salts, sulfate oil salts such as funnel oil,
Examples thereof include alkyl phosphates, ether phosphates, alkyl allyl ether phosphates, amide phosphates, N-acyl amino acid activators and the like.

Examples of the cationic surfactant include alkylamine salts, amine salts such as polyamine and aminoalcohol fatty acid derivatives, alkyl quaternary ammonium salts, aromatic quaternary ammonium salts, pyridinium salts and imidazolium salts. As the nonionic surfactant, sorbitan fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, propylene glycol fatty acid ester, polyethylene glycol fatty acid ester, sucrose fatty acid ester, polyoxyethylene alkyl ether, polyoxypropylene alkyl ether,
Polyoxyethylene alkyl phenyl ether, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene sorbitol fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyoxyethylene propylene glycol fatty acid ester, polyoxyethylene castor oil, polyoxy Ethylene hydrogenated castor oil, polyoxyethylene phytostanol ether, polyoxyethylene phytosterol ether, polyoxyethylene cholestanol ether, polyoxyethylene cholesteryl ether, polyoxyalkylene-modified organopolysiloxane, polyoxyalkylene / alkyl co-modified organopolysiloxane, Examples include alkanolamides, sugar ethers, sugar amides and the like. Examples of the amphoteric surfactant include betaine, aminocarboxylic acid salt, and imidazoline derivative.

As the metal soap, aluminum 12-hydroxystearate, zinc stearate, aluminum stearate, calcium stearate, magnesium stearate, zinc myristate, magnesium myristate, zinc cetyl phosphate, calcium cetyl phosphate, sodium zinc cetyl phosphate, Zinc laurate,
Examples include zinc undecylenate and the like.

As the gelling agent, N-lauroyl-L-
Glutamic acid, amino acid derivatives such as α, γ-di-n-butylamine, dextrin palmitate, dextrin stearate, dextrin 2-ethylhexanoate palmitate and other dextrin fatty acid esters, sucrose palmitate, sucrose stearin Examples thereof include sucrose fatty acid esters such as acid esters, benzylidene derivatives of sorbitol such as monobenzylidene sorbitol, dibenzylidene sorbitol, and organically modified clay minerals such as dimethylbenzyl dodecyl ammonium montmorillonite clay and dimethyl dioctadecyl ammonium montmorillonite clay.

As the powder, as long as it is used in ordinary cosmetics, its shape (spherical shape, needle shape, plate shape, etc.), particle diameter (fume shape, fine particles, pigment grade, etc.), particle structure ( Porous,
Inorganic powder, organic powder, pigment, etc. can be used regardless of whether they are non-porous or the like. For example, as the inorganic powder, magnesium oxide, barium sulfate, calcium sulfate, magnesium sulfate, calcium carbonate, magnesium carbonate, talc, synthetic mica, mica, kaolin, sericite, muscovite, synthetic mica, phlogopite, phlogopite, Biotite,
Lithia mica, silicic acid, anhydrous silicic acid, aluminum silicate, magnesium silicate, magnesium aluminum silicate, sulfur-containing aluminum silicate, calcium silicate, barium silicate, strontium silicate, metal tungstate, hydroxyapatite, vermiculite , Heidilite, montmorillonite, zeolite, ceramics powder, dicalcium phosphate, alumina, aluminum hydroxide, boron nitride, boron nitride and the like.

As the organic powder, polyamide powder,
Polyester powder, polyethylene powder, polypropylene powder, polystyrene powder, polyurethane, benzoguanamine powder, polymethylbenzoguanamine powder, tetrafluoroethylene powder, polymethylmethacrylate powder, silk powder, nylon powder, 12 nylon, 6 nylon, styrene / acrylic acid copolymer Coalesce, divinylbenzene / styrene copolymer, vinyl resin, urea resin, phenol resin, fluororesin, silicon resin, acrylic resin, melamine resin, epoxy resin, polycarbonate resin, microcrystalline fiber powder,
Examples thereof include lauroyl lysine.

The colored pigments include inorganic red pigments such as iron oxide, iron hydroxide and iron titanate, inorganic brown pigments such as γ-iron oxide, inorganic yellow pigments such as yellow iron oxide and ocher, and black iron oxide. Inorganic black pigments such as carbon black, inorganic purple pigments such as manganese violet and cobalt violet, inorganic green pigments such as chromium hydroxide, chromium oxide, cobalt oxide and cobalt titanate, inorganic blue pigments such as navy blue and ultramarine blue, tar pigments Examples include pigments obtained by making a dye into a lake, pigments obtained by making a natural dye into a lake, and composite powders obtained by combining these powders. Examples of the pearl pigment include titanium oxide-coated mica, titanium oxide-coated mica, bismuth oxychloride, titanium oxide-coated bismuth oxychloride, titanium oxide-coated talc, fish scale foil, titanium oxide-coated colored mica and the like. Examples of metal powder pigments include aluminum powder, copper powder, and stainless powder.

As tar dyes, Red No. 3 and Red 10
No. 4, Red 106, Red 201, Red 202, Red 204, Red 205, Red 220, Red 226
No., Red 227, Red 228, Red 230, Red 401, Red 505, Yellow 4, Yellow 5, Yellow 2
02, yellow 203, yellow 204, yellow 401,
Blue No. 1, Blue No. 2, Blue No. 201, Blue No. 404, Green No. 3, Green No. 201, Green No. 204, Green No. 205,
Orange 201, Orange 203, Orange 204, Orange 20
No. 6, orange No. 207, and the like. Examples of natural pigments include carminic acid, laccaic acid, calsamine, bradylin and crocin. Powders such as the above-mentioned inorganic powders, organic powders, pigments and tar dyes may be compounded or surface-treated with an oil agent, silicone, or a fluorine compound.

As the ultraviolet ray protective agent, 2-ethylhexyl paramethoxycinnamate, isopropyl paramethoxycinnamate, paramethoxyhydrocinnamate diethanolamine salt, diparamethoxycinnamate-glyceryl mono-2-ethylhexanoate. , Octyl methoxycinnamate, methyl isopropyl cinnamate, and other cinnamic acid UV absorbers; 2-hydroxy-4-methoxybenzophenone, 2
-Hydroxy-4-methoxybenzophenone-5-sulfuric acid, 2-hydroxy-4-methoxybenzophenone-5
-Sodium sulfate, 2,4-dihydroxybenzophenone, 2,2'-dihydroxy-4,4'-dimethoxybenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone, 2,2 ', 4,4'-tetrahydroxy Benzophenone-based UV absorbers such as benzophenone and 2-hydroxy-4-n-octoxybenzophenone;
Para-aminobenzoic acid, ethyl para-aminobenzoate, butyl para-aminobenzoate, para-dimethylaminobenzoic acid-
2-ethylhexyl, glyceryl paraaminobenzoate,
Examples thereof include benzoic acid type ultraviolet absorbers such as amyl paraaminobenzoate.

As a UV protection agent, salicylic acid-2
-Ethylhexyl, triethanolamine salicylate,
Salicylic acid UV absorbers such as homomenthyl salicylate, dipropylene glycol salicylate, methyl salicylate, ethylene glycol salicylate, phenyl salicylate, amyl salicylate, benzyl salicylate, isopropylbenzyl salicylate, potassium salicylate; 4-t
A dibenzoylmethane-based ultraviolet absorber such as -butyl-4'-methoxydibenzoylmethane, 4-isopropyldibenzoylmethane, 4-methoxydibenzoylmethane, 4-t-butyl-4'-hydroxydibenzoylmethane;
Menthyl-O-aminobenzoate, 2-phenyl-benzimidazole-5-sulfate, 2-phenyl-5-methylbenzoxazole, 3- (4-methylbenzylidene)
Camphor, 2-ethylhexyl-2-cyano-3,3-
Diphenyl acrylate, 2-ethyl-2-cyano-
Anthranilic acid type UV absorbers such as 3,3′-diphenyl acrylate, 2- (2′-hydroxy-5-methylphenyl) benzotriazole and menthyl anthranilate; Urocanic acid type UV absorbers such as ethyl urocanate; Titanium oxide , Zirconium oxide, cerium oxide and the like.

Examples of alcohols include lower alcohols such as ethanol and isopropanol, and glycerin, diglycerin, ethylene glycol, diethylene glycol, triethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, polyethylene glycol and the like. Examples thereof include polyhydric alcohol.

As the water-soluble polymer, gum arabic, tragacanth, galactan, carob gum, guar gum,
Plant-based macromolecules such as karaya gum, carrageenan, pectin, agar, algae colloid, trant gum, locust bean gum and galactomannan; microbial macromolecules such as xanthan gum, dextran, succinoglucan and pullulan; animals such as casein, albumin and gelatin -Based polymers; starch-based polymers such as starch, carboxymethyl starch, and methyl hydroxypropyl starch; methyl cellulose, ethyl cellulose, methyl hydroxypropyl cellulose, carboxymethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, nitrocellulose, sodium cellulose sulfate, sodium carboxymethyl cellulose , Crystalline cellulose, cellulosic polymer of cellulose powder; sodium alginate, alginate Alginic acid-based polymers such as pyrene glycol ester; Vinyl-based polymers such as polyvinyl methyl ether, carboxyvinyl polymer, and alkyl-modified carboxyvinyl polymers; Polyoxyethylene-based polymers; Polyoxyethylene-polyoxypropylene copolymer-based polymers; Poly Acrylic polymers such as sodium acrylate, polyethyl acrylate and polyacrylamide; inorganic water-soluble polymers such as polyethyleneimine, cationic polymer, bentonite, laponite and hectorite. In addition, a film forming agent such as polyvinyl alcohol or polyvinylpyrrolidone is also included in this.

As the antibacterial agent, benzoic acid, sodium benzoate, carboxylic acid, sorbic acid, potassium sorbate, paraoxybenzoic acid ester, parachlorometacresol, hexachlorophene, benzalkonium chloride, chlorhexidine chloride, trichlorocarbanilide, Photosensitizer,
Examples include bis (2-pyridylthio-1-oxide) zinc, phenoxyethanol and thiantol, and isopropylmethylphenol. Examples of the pH adjuster include potassium carbonate, sodium hydrogen carbonate, ammonium hydrogen carbonate and the like. Examples of the cooling agent include L-menthol and camphor.

Examples of the cell activating agent include deoxyribonucleic acid and salts thereof, adenylic acid derivatives such as adenosine triphosphate and adenosine monophosphate and salts thereof, ribonucleic acid and salts thereof, cyclic AMP, cyclic GMP, flavin adenine. Nucleotide, guanine, adenine, cytosine, thymine, xanthine and their derivatives, such as caffeine, theoferin and their salts, nucleic acid-related substances, calf blood extract, serum deproteinized extract, spleen extract, bird etc. Egg component, chicken cob extract, shell extract, shellfish extract, royal jelly, silk protein and its degradation products or their derivatives, hemoglobin or its degradation products,
Lactoferrin or its degradation product, mollusc extract such as squid, fish meat extract, mammals, birds, shellfish, insects,
Examples include animal-derived extracts such as fish, molluscs and crustaceans, yeast extracts, lactic acid bacterium extracts, and fermented metabolite-derived extracts such as bifidobacteria extracts.

Further, as cell activating agents, retinol and its derivatives (retinol palmitate, retinol acetate, etc.), retinal and its derivatives, dehydroretinal, carotenoids and other vitamins A, thiamines (thiamine hydrochloride, thiamine sulfate). Salt), riboflavins (riboflavin, riboflavin acetate, etc.), pyridoxines (pyridoxine hydrochloride, pyridoxine dioctanoate, etc.), flavin adenine nucleotides, cyanocobalamin, folic acid, nicotinic acids (nicotinamide,
Benzyl nicotinate etc.), vitamin Bs such as choline,
Apricot extract, Ginkgo biloba extract, Panax ginseng extract, Barley extract, Orange extract, Cucumber extract, Kiwi extract, Shiitake extract, Horse mackerel extract, Assemblage extract, Taiso extract, Capsicum extract, Garlic extract Substance, carrot extract, bouncy extract, peach extract, lettuce extract, lemon extract, Reishi extract,
Rosemary extract, plant-derived extracts such as hinokitiol and cepharanthin, α- and γ-linolenic acid, eicosapentaenoic acid and their derivatives, estradiol and its derivatives and their salts, glycolic acid, succinic acid, lactic acid, salicylic acid Examples thereof include organic acids and their derivatives, salts thereof, and the like. One or two or more of the above-mentioned cell activating agents can be appropriately selected and mixed.

Examples of active oxygen scavengers include superoxide dismutase, mannitol, bilirubin, cholesterol, tryptophan, histidine, quercetin, quercitrin, catechin, catechin derivatives, rutin, rutin derivatives, taurine, thiotaurine, eggshell membrane extracts, gallic acid. , Gallic acid derivative, yeast extract, ganoderma lucidum extract, yashajitsu extract, ginkgo biloba extract, peony extract, melissa extract, parsley extract and dicoppi extract, retinol and its derivatives (retinol palmitate, retinol acetate etc.) ), Retinal and its derivatives, vitamins A such as dehydroretinal; thiamines (thiamine hydrochloride, thiamine sulfate, etc.), riboflavins (riboflavin, riboflavin acetate, etc.), pyridoxines (pyrihydrochloride). Xin, pyridoxine dioctanoate, etc.), flavin adenine nucleotide, cyanocobalamin, folic acid, nicotinic acids (nicotinamide, benzyl nicotinate, etc.), choline and other vitamin Bs; ergocalciferol, cholecalciferol, dihydroxysta Vitamin Ds such as nal; tocopherol and its derivatives (dl-α (β, γ) -tocopherol,
Acetic acid dl-α-tocopherol, nicotinic acid-dl-α
-Tocopherol, linoleic acid-dl-α-tocopherol, succinic acid dl-α-tocopherol, etc.), vitamin Es such as ubiquinones; and dibutylhydroxytoluene and butylhydroxyanisole.

Examples of moisturizers include mucopolysaccharides such as alkaline hot spring water, deep water, hyaluronic acid, chondroitin sulfate, dermatan sulfate, heparan sulfate, heparin and keratan sulfate or salts thereof, proteins such as collagen, elastin and keratin. Or their derivatives and their salts, soybean and egg-derived phospholipids, glycolipids,
Ceramide, mucin, honey, erythritol, maltose, maltitol, xylitol, xylose, pentaerythritol, fructose, dextrin and its derivatives, mannitol, sorbitol, inositol, trehalose, sugars such as glucose, urea, asparagine, aspartic acid, alanine, arginine. , Isoleucine, ortinin, glutamine, glycine, glutamic acid and its derivatives and salts thereof, cysteine, cystine, citrulline, threonine, serine, tyrosine,
Examples thereof include tryptophan, theanine, valine, histidine, hydroxylysine, hydroxyproline, pyrrolidonecarboxylic acid and salts thereof, amino acids such as proline, phenylalanine, methionine and lysine, and derivatives or salts thereof.

Further, as a moisturizing agent, D-panthenol, avocado extract, almond oil, carob extract, rice extract, strawberry extract, fennel extract, mung bean extract, Coptis chinensis extract, olive oil, Astragalus vulgaris extract, Cocoa butter, oats extract, kizuta extract, kumasaza extract, gardenia extract, grapefruit extract, ginger extract, gentiana extract,
Burdock extract, Kobotsudori extract, sesame extract, cactus extract, Sophoraceae extract, ginger extract, dio extract, shea butter, sycamore extract, senkyu extract, mallow extract, pearl extract, camellia extract Substance, corn extract, euglena extract, tormentilla extract, dokudami extract, bakumondou extract, haute bean extract, hamamelis extract, mint extract, green mint extract, mint extract, parsley extract, rose extract , Sunflower extract, cypress extract, luffa extract, prune extract, butchers bloom extract, borage oil, botanical extract, jojoba oil, bodaiju extract, hops extract, pine extract, horse chestnut extract, macadamia nut oil , Quince extract,
Examples include purple extract, meadow home oil, melissa extract, cornflower extract, lily extract, yuzu extract, lime extract, lavender extract, gentian extract, oleander extract and apple extract. The moisturizers listed above can be blended by appropriately selecting one kind or two or more kinds.

As vitamins, vitamin Ks such as phytonadione, menaquinone, menadione and menadiol,
Examples thereof include vitamin Ps such as eriocitrin and hesperidin, biotin, cartinin, and ferulic acid. As blood circulation promoters, nonyl acid warenylamide, capsaicin, zingerone, cantharisin tincture, ictamol, α
—Bornole, inositol hexanicotinate, cyclanderate, cinnarizine, tolazoline, acetylcholine, verapamil, γ-oryzanol and the like. Skin astringents include tannic acid, antiseborrheic agents such as thianthol, and enzymes include lipase, papain and the like.

[0039]

The present invention will be described in more detail with reference to Reference Examples, Test Examples and Examples, but the present invention is not limited thereto.

Reference Example 1. Production of acerola extract Acerola (scientific name: Malpighia emarginata DC)
Purified water was added to the fruit of the above, extraction was performed at low temperature for 1 day, and then filtration was performed to obtain an acerola extract (dry solid content 1.7).
%).

Reference Example 2. Production of plant extract 100 ml of 70% (v / v) ethyl alcohol was added to each 10 g of licorice (JP), touki (JP) and sohakuhi (JP), and extracted for 3 days with occasional stirring at room temperature. , Each plant extract was obtained by filtration (dry solid content was 2.0%, 1.0%, 1.1%, 1.0%,
0.8%).

Reference Example 3. Manufacture of chamomile extract 20 g of dried chamomile flowers was finely chopped, 100 ml of 1,3-butylene glycol was added, and the mixture was extracted at room temperature for 5 days with occasional stirring, and filtered to obtain a chamomile extract (dry solid content. 0.9%).

Reference Example 4. Production of bovine placenta extract 1 kg of bovine placenta from 3 to 4 months of gestation is frozen and thawed, impurities are washed away after removal, 5 liters of purified water is added, and the mixture is extracted under reduced pressure and low temperature for 3 days and filtered to obtain a placenta extract. Was obtained (dry solid content 3.5%).

Test Example 1. Tyrosinase activity inhibition test With respect to the acerola extract obtained in Reference Example 1 and the plant extract obtained in Reference Example 2, the tyrosinase activity inhibition rate of the sample alone or in combination thereof was examined by the following method.
That is, an enzyme solution (manufactured by Sigma, 28,000) was added to each sample.
0.1 unit of 10 mg of tyrosinase dissolved in 20 ml of 0.1 M phosphate buffer (pH 6.8)] was added to 0.1 ml of 0.1 M phosphate buffer (pH 6.8) to make 4.0 ml, This was incubated at 25 ° C for 10 minutes.

Next, a substrate solution [L-DOPA (manufactured by Tokyo Kasei) 198.0 mg, which had been previously kept at 25 ° C., was added thereto.
Was dissolved in 100 ml of 0.1 M phosphate buffer (pH 6.8)] 1.0 ml was added and reacted for 10 minutes. After the reaction, the absorbance (ODS) at 475 nm was measured. Similarly, the absorbance (ODHE) at the time of reacting with the enzyme deactivated by heating and the absorbance (ODB) when the sample was not added were measured, and the activity inhibition rate of tyrosinase activity was calculated by the following formula. The results are shown in Table 1.

[0046]

[Equation 1]

[0047]

[Table 1]

As is clear from Table 1, when the acerola extract and the whitening agent are combined, the tyrosinase activity inhibitory action is higher than when the acerola extract or the whitening agent is used alone, and a synergistic whitening effect is exhibited. It was

Test Example 2. Melanin production inhibition test by cell culture By the following method, regarding the acerola extract and bovine placenta extract obtained in Reference Example 1 and the plant extract obtained in Reference Example 2,
The melanin production inhibitory effect of the samples alone or in combination thereof was examined. Using mouse-derived B16 melanoma cultured cells as culture cells, an appropriate amount of medium was placed in two 6-well petri dishes, and B16 melanoma cells were seeded at 37 ° C.
Let stand in a carbon dioxide concentration of 5%. On the next day, each sample is mixed with the sample preparation solution so that the final concentration becomes 0 (control), 1, 10, 100 μg / ml. On the 5th day of culture, the medium is exchanged and the sample preparation solution is added again. On the next day, the medium was removed, and one dish was washed with phosphate buffer and then collected, and the whiteness of the B16 melanoma cultured cells was evaluated according to the following criteria.

(Judgment criteria) ++: Very white with respect to the control. +: Clearly white with respect to the control. ±: slightly whiter than the control. -: The same black color as the control.

With respect to the remaining one dish, the cells were fixed with formalin and then added to 1% crystal violet solution for staining. The number of viable cells (A) and the number of control cells (B) for each sample concentration were measured with a monoserator (manufactured by Olympus), and the cell viability was calculated by the following formula. The results are shown in Table 2. Cell viability (%) = (A / B) × 100

[0052]

[Table 2]

As is clear from Table 2, when the acerola extract and the whitening agent are combined, the melanin production inhibitory action is higher than when the acerola extract or the whitening agent is used alone, and a synergistic whitening effect is exhibited. , And low toxicity to B16 melanoma cultured cells.

Test Example 3. Erythema Suppression Test The backs of colored guinea pigs (15 in each group) were shaved and irradiated with ultraviolet rays under anesthesia. UV irradiation is FL2 made by Toshiba Corporation
Three 0S / BLB lamps and three FL20S / E30 lamps are irradiated at the same time, and the amount of ultraviolet rays is 4.8 × 10 6 erg /
cm2. 0.2 ml each of the sample prepared by the composition shown in Table 3 and the following production method was applied to four places on the back of the guinea pig 24 hours before, immediately after and 12 hours after and 24 hours after the ultraviolet irradiation. However, the application site was thoroughly washed with warm water before irradiation. 24 hours after irradiation,
After 7 days, the degree of pigmentation was observed and evaluated according to the following criteria. The results are also shown in Table 3.

[0055]

[Table 3]

(Production Method) A. Ingredients (1)-(6), (10) and (11) are mixed and heated to 70 ° C. B. Mix components (7)-(9) and (12) and heat to 70
Keep at ℃. C. B was added to A, mixed, and then cooled to obtain a cream.

[0057] (Evaluation criteria for erythema suppressing effect) <Evaluation> <Contents> Efficient erythema is not observed at all. Effective Erythema is very slight. Slightly effective erythema is observed, but the boundary with the non-irradiated area is unclear. Ineffective erythema was observed, and the boundary with the non-irradiated area was clear.

[0058] (Evaluation criteria for pigmentation suppression effect) <Evaluation> <Contents> No significant pigmentation is observed. Effectively slight pigmentation is observed. Somewhat effective pigmentation is observed, but the boundary with the non-irradiated site is unclear. Ineffective pigmentation was observed and the boundary with the non-irradiated area was clear.

As shown in the results of Table 3, the composition of the present invention product 1 in which the acerola extract and stearyl glycyrrhetinate were combined and blended, and the composition of the invention product 2 in which the acerola extract and chamomile extract were combined and blended It was revealed that by applying these to the skin, erythema and pigmentation due to ultraviolet rays were effectively suppressed.

Example 1. Cream Preparation Example A cream was prepared according to the composition shown in Table 4 and the following production method, and the skin beautifying effect when the acerola extract and a whitening agent and / or an anti-inflammatory agent were combined was examined. The results are shown in Table 4.

[0061]

[Table 4]

(Production Method) A. Ingredients (1)-(6) and (10) are mixed and heated to 70 ° C.
Keep on. B. Ingredients (8)-(9) and (12) are mixed and heated to 70
Keep at ℃. C. After adding B to A and mixing (7) and (11), the mixture was cooled to obtain a cream.

(Test Method) For each test cream product, 15 women aged 27 to 54 were used as a panel, and an appropriate amount of the test cream was applied to the face after washing the face twice a day every morning and night for 12 weeks. The whitening effect by application was evaluated according to the following criteria.

(Evaluation criteria) <Evaluation> <Contents> Effective The dullness of the skin is no longer noticeable. Somewhat effective The dullness of the skin became less noticeable. Ineffective No change from before use.

As shown in the results of Table 4, the composition of the present invention product 1 in which the acerola extract and magnesium L-ascorbyl phosphate were combined and blended, and the composition of the present invention product 2 in which the acerola extract and dipotassium glycyrrhizinate were combined were prepared. Composition,
The composition of the product 3 of the present invention in which the acerola extract is combined with magnesium L-ascorbyl phosphate and dipotassium glycyrrhizinate is to prevent the occurrence of "dullness" and improve the skin by applying these to the skin. It was revealed that it was possible to obtain beautiful skin.

[0091]

INDUSTRIAL APPLICABILITY According to the present invention, by combining an acerola extract with a whitening agent and / or an anti-inflammatory agent and blending it with a skin external preparation, the inherent properties of the whitening agent and / or anti-inflammatory agent can be sufficiently achieved. Since it can be exerted, the external preparation for skin has a stable and excellent whitening action and anti-inflammatory action, and therefore exhibits a high inhibitory effect on hot flashes due to sunburn and erythema due to ultraviolet irradiation, or on pigmentation. Effective in preventing and improving skin darkening due to sunburn, spots and freckles. As described above, the external preparation for skin of the present invention can sufficiently exhibit the inherent properties of a whitening agent and / or an anti-inflammatory agent, and thus is extremely useful in beauty and medicine.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI A61K 7/00 A61K 7/00 J KU 7/48 7/48 35/78 35/78 C A61P 17/00 A61P 17/00 (72) Inventor Shizuka Uehara 48-18 Sakaemachi, Kita-ku, Tokyo Kose Research Headquarters (72) Inventor Ichiro Sasaki 48-18 Sakaemachi, Kita-ku, Tokyo Kose Research Headquarters (72) Invention Kenichi Nagamine 2-5-1-203 Misumi Town, Higashimurayama City, Tokyo (72) Inventor Takashi Kito 1-21-25-103 Namiki, Kawaguchi City, Saitama Prefecture (56) Reference JP-A-7-61915 (JP, A) JP 10-95704 (JP, A) JP 7-277939 (JP, A) JP 10-114670 (JP, A) JP 9-291011 (JP, A) JP 9 -183718 (JP, A) JP-A-2-200610 (JP, A) (58) Fields investigated (Int .Cl. ⁷ , DB name) A61K ^7/ 00-7/50

Claims (3)

(57) [Claims] 1. A skin whitening external preparation containing the following components (A) and (B); (A) acerola extract (B) whitening agent and / or anti-inflammatory agent, wherein the whitening agent is
L-ascorbic acid sodium sulfate, L-as
Corbic acid phosphate magnesium, L-ascor
Sodium biphosphate phosphate, Licorice extract, Sodium
Select from Uhakuhi extract, Toki extract and placenta extract
At least one of the
Dipotassium tyrrhizinate, stearyl glycyrrhetinate
And an external preparation for whitening skin, which is at least one selected from chamomile extracts . 2. The skin whitening external use according to claim 1, wherein the blended amount of the acerola extract is 0.00005 to 5% by weight as a dry solid content, and the blended amount of the whitening agent is 0.00001 to 10% by weight. Agent. 3. The whitening skin according to claim 1, wherein the blended amount of the acerola extract is 0.00005 to 5% by weight as a dry solid content, and the blended amount of the anti-inflammatory agent is 0.00001 to 20% by weight. Topical agent.