Cosmetic topical preparations and cosmetics

Abstract

To provide novel administration means of a valuable material having fat-dissolving action.SOLUTION: A tape agent, a patch agent or a cataplasm which contains any one or more kinds of a fat-decomposing agent, a fat-dissolving agent or a fat metabolism promoter, is aimed at fat reduction or / and partial slimming or / and tightening of skin.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to an external preparation and a cosmetic for the purpose of subcutaneous fat decomposition and dissolution. Specifically, it relates to the technical field of external preparations and cosmetics containing a fat-dissolving agent or the like as a main component as a valuable component.

Background Art

[0002] Subcutaneous fat accumulation is related to the dysfunction of adipocytes, and the accumulated triglycerides are enzymatically decomposed and further decomposed into fatty acids, glycerol, and / or glycerol esters. For various reasons, the accumulation of triglycerides occurs in adipocytes, resulting in subcutaneous fat accumulation. As a result, it causes overweight and problems in treatment and beauty.

[0003] For obesity presenting an excessive fat layer among this subcutaneous fat accumulation and obesity, a method of directly injecting a composition for removing subcutaneous fat accumulation subcutaneously is taken. For this, phosphatidylcholine preparations typified by Lipostabil of Sanofi-Aventis are used (Patent Documents 1, 2). On the other hand, subcutaneous injection of deoxycholic acid is also known. However, it is regarded as a problem from the viewpoint of safety such as pain and skin swelling during the procedure, and it can be said that it is a high-risk method. Also, in the case of injection, the injection needle must be shaken subcutaneously for a certain area and injected. Furthermore, due to the unevenness of the injected liquid, the convenience of fat dissolution changes and unevenness of the skin occurs. Patent Document 3 proposes a dosage form such as a wax using phosphatidylcholine, and Patent Document 4 proposes a liquid preparation composed of a carnitine derivative. However, no development has been made for skin external preparations such as patch agents, patchy agents, and tape agents.

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Patent Document 2

[0005] The object of the present invention is to provide a novel means of administering a valuable substance having a fat-dissolving effect. Specifically, the invention relates to a patch, tape, or pup-type topical preparation and cosmetic containing a valuable substance having a fat-degrading or fat-dissolving effect. [Means for solving the problem]

[0006] Until now, there have been no transdermal formulations intended for fat dissolution. Therefore, when developing the above-mentioned valuable substances into transdermal formulations, there was no knowledge whatsoever regarding the concentration of the valuable substances, the frequency of skin application, etc. As a result, ensuring the combination of valuable substances, the stability of the formulation, and skin penetration became important challenges. The inventors of this invention have solved these problems and succeeded in manufacturing topical preparations and cosmetics containing valuable substances with fat-dissolving properties, thereby completing the present invention.

[0007] The inventors of the present invention have discovered that by incorporating a fat-dissolving agent or the like as an active ingredient into a sheet-type adhesive patch, poultices, or tapes, the valuable ingredient can be absorbed transdermally, making it possible to use it as a topical preparation or cosmetic that is effective in reducing fat and / or localized fat loss and / or skin tightening, and have thus completed the present invention. The present invention is as follows: [1] A topical preparation or cosmetic containing one or more of the following: a fat-decomposing agent, a fat-dissolving agent, or a fat-metabolism-promoting agent, for the purpose of reducing fat and / or localized fat loss and / or skin tightening. [2] A topical preparation or cosmetic intended for fat reduction and / or localized fat reduction and / or skin tightening, containing 0.1% by mass or more of one or more fat-reducing ingredients selected from the group consisting of fat-decomposing agents, fat-dissolving agents and fat-metabolism promoters. [3] The topical preparation or cosmetic described in [1] or [2], wherein the fat-degrading agent is lipase. [4] The topical preparation or cosmetic described in [3], which contains lipase, Mg salt and Ca salt. [5] The topical preparation or cosmetic according to [1] or [2], wherein the fat-dissolving agent is one or more selected from the group consisting of phosphatidylcholine, adenosine triphosphate and its sodium salt, and deoxycholic acid and its salt. [6] The topical preparation or cosmetic according to [1] or [2], wherein the fat metabolism promoter is one or more selected from the group consisting of amino acids, L-carnitine, inositol, capsaicin, and caffeine. [7] The topical preparation or cosmetic according to [6], wherein the amino acid is one or more selected from the group consisting of tyrosine, serine, threonine, phenylalanine, tryptophan, isoleucine, lysine, arginine, betaine, histidine, glutamine, glycine, and cysteine. [8] An external preparation or cosmetic according to any of [1] to [7], wherein the external preparation or cosmetic is an adhesive sheet. [9] The topical preparation or cosmetic described in [8], which is based on an acrylic, rubber, or silicone adhesive.

[10] A topical preparation or cosmetic according to [8], which is based on a water-soluble resin.

[11] A topical preparation or cosmetic containing phosphatidylcholine and one or more selected from the group consisting of astaxanthin, tocopherol acetate, tocopherol, ascorbyl palmitate, and diethanolamine.

[12] A topical preparation or cosmetic containing sodium deoxycholate and an acidic substance.

[13] An external preparation or cosmetic according to any one of [1] to [9], comprising an ointment and a support sheet, wherein the ointment contains one or more of a lipolytic agent, a lipolytic agent, or a lipolytic agent in an acrylic, rubber, or silicone adhesive, the support sheet is a nonwoven fabric, woven fabric, knitted fabric, or polyurethane film, and the thickness of the ointment is 5 to 200 μm.

[14] The external preparation or cosmetic according to

[13] , wherein the support sheet is a polyurethane film with a thickness of 3 to 50 μm, the ointment is a roll-shaped viscous sheet, and the thickness of the ointment is 5 to 100 μm. A method for producing an external preparation or cosmetic as described in any of

[15] , [8], to

[10] , comprising the following steps (a), (b), or (c): (a) When the base is a solution-type adhesive, A step of uniformly mixing an adhesive solution and at least one valuable substance selected from the group consisting of a lipolytic agent, a lipolytic agent, and a lipolytic agent. The process involves applying the obtained adhesive solution onto a release sheet and drying the solvent, and A process of laminating the dried adhesive layer onto a support sheet as needed; (b) If the base is a hot melt adhesive, A process of uniformly kneading an adhesive composition and at least one valuable substance selected from the group consisting of lipolytic agents, lipolytic agents and lipolytic agents at high temperature, and A step of applying the obtained adhesive mixture to a release sheet or support sheet; (c) When the base is a poultice base, A process of uniformly mixing water with at least one valuable substance selected from the group consisting of water-soluble resins, lipolytic agents, lipolytic agents and lipolytic agents, and A step of applying the obtained water-soluble resin composition to a release sheet or support sheet. [Effects of the Invention]

[0008] According to the present invention, subcutaneous fat in the application area can be easily and uniformly dissolved. One aspect of the external preparation of the present invention, such as a tape-type transdermal preparation, a patch-type transdermal preparation, a pap-type transdermal preparation, etc., is expected to have the effect of easily diffusing a fat-dissolving agent into subcutaneous tissue, decomposing, burning or dissolving the subcutaneous fat in the obese area, causing partial weight loss, reducing eye bags and creating a small face line. In addition, a tightening effect can be expected by dissolving the subcutaneous fat in the sagging part.

Brief Description of the Drawings

[0009] [Figure 1] Bottom view of the sheet-like preparation of Example 8 as seen from the support side [Figure 2] Graph showing changes in subcutaneous fat thickness of the abdomen [Figure 3] Graph showing changes in subcutaneous fat thickness of the upper arm

Modes for Carrying Out the Invention

[0010] The external preparation and cosmetic of the present invention are compositions in which a valuable substance having a fat-dissolving action is dissolved and dispersed in a base, and it is more preferable that this composition is laminated on one surface of a support sheet. The external preparation or cosmetic of the present invention is preferably used for the purpose of fat reduction or / and partial weight loss or / and skin tightening.

[0011] The above support sheet is not particularly limited, and a sheet generally used as a support sheet for conventional tape-type transdermal preparations, patch-type transdermal preparations, pap-type transdermal preparations, etc. is preferable. For example, sheets such as cellulose acetate, ethyl cellulose, polyethylene resin, polypropylene resin, ethylene-propylene copolymer, ethylene-vinyl acetate copolymer, vinyl chloride-based resin, vinylidene chloride resin, vinyl acetate-vinyl chloride copolymer, polyamide-based resin, polyester resin, ABS resin, SIS resin, SEBS resin, PIB-based resin, urethane resin, silicone resin, aluminum, etc. can be mentioned. Also, these sheets may be woven or non-woven fabrics of fibers of the above materials, or laminated sheets of these sheets, woven fabrics and non-woven fabrics.

[0012] The above-mentioned base is not particularly limited, and bases that have been conventionally used as bases for transdermal formulations can be used. In the case of tape-type transdermal formulations and patch-type transdermal formulations, the base is an adhesive, and in the case of tape-type transdermal formulations, it is necessary to have excellent adhesion to the skin and be able to be removed without leaving any residue, so acrylic adhesives and rubber adhesives are preferably used. In the case of pap-type formulations, a base consisting of a water-soluble resin and water is generally used.

[0013] As the acrylic adhesive described above, (co)polymers of alkyl (meth)acrylates, which are esters of aliphatic alcohols having 4 to 18 carbon atoms and (meth)acrylic acid, and (co)polymers of alkyl (meth)acrylates and functional monomers are preferably used.

[0014] Examples of the alkyl (meth)acrylate esters mentioned above include butyl (meth)acrylate, isobutyl (meth)acrylate, hexyl (meth)acrylate, octyl (meth)acrylate, 2-ethylhexyl (meth)acrylate, isooctyl (meth)acrylate, decyl (meth)acrylate, isodecyl (meth)acrylate, lauryl (meth)acrylate, and stearyl (meth)acrylate.

[0015] Examples of the above-mentioned functional monomers include 2-hydroxyethyl (meth)acrylate, hydroxypropyl (meth)acrylate, (meth)acrylic acid, maleic acid, maleic anhydride, fumaric acid, crotonic acid, butyl maleate, acrylamide, dimethylacrylamide, diethylacrylamide, butoxymethylacrylamide, ethoxymethylacrylamide, methylol(meth)acrylamide, dimethylaminoacrylate, and N-vinyl-2-pyrrolidone.

[0016] Furthermore, polymerizable monomers copolymerizable with alkyl (meth)acrylate may be copolymerized. Examples of polymerizable monomers include vinyl acetate, styrene, α-methylstyrene, vinyl chloride, acrylonitrile, ethylene, propylene, and butadiene. Preferably, the alkyl (meth)acrylate component of the (co)polymer is 50% by mass or more. Specifically, these are copolymers of alkyl acrylates, and copolymers of alkyl acrylates with acrylic acid, acrylamide, vinyl acetate, etc. Plasticizers such as isopropyl myristate or isopropyl palmitate may be added to these adhesives to improve skin adhesion.

[0017] The thickness of the adhesive layer (plaster) is preferably 5 μm to 200 μm, and more preferably 10 μm to 200 μm. A thickness of 5 μm to 100 μm is also desirable. Specifically, HiPAS® adhesive (acrylic ester, manufactured by Cosmedi Pharmaceutical Co., Ltd.) and MASCOS10 (product name) adhesive (acrylic ester, manufactured by Cosmedi Pharmaceutical Co., Ltd.) can be suitably used.

[0018] Furthermore, it is preferable that the acrylic copolymer is post-crosslinked with a metal chelate compound. To obtain appropriate cohesive force and tackiness, it is preferable to add 0.05 to 2.0 parts by mass of the metal chelate compound per 100 parts by mass of the acrylic copolymer.

[0019] Examples of the above-mentioned metal chelate compounds include aluminum acetylacetonate, aluminum glycinate, and aluminum hydroxide gel, which may be used alone or in combination.

[0020] As the above-mentioned rubber-based adhesive, conventionally known rubber-based adhesives mainly composed of rubber such as natural rubber, polyisoprene, polyisobutylene, polybutadiene, styrene-butadiene copolymer, styrene-butadiene-styrene copolymer, styrene-isoprene copolymer, styrene-isoprene-styrene copolymer, and urethane rubber can be used.

[0021] The above-mentioned rubber-based adhesive may optionally contain tackifiers such as rosin resins, polyterpene resins, coumarone-indene resins, petroleum resins, terpene-phenol resins, and alicyclic hydrocarbons. The content of the tackifier is not particularly limited, but is generally 20 to 80% by mass of the total amount of the rubber-based adhesive and the tackifier. The above-mentioned rubber-based adhesive may further contain plasticizers, fillers, and antioxidants such as liquid paraffin, liquid polybutene, liquid polyisoprene, mineral oil lanolin, liquid polyacrylate, squalane, and olive oil.

[0022] Examples of the water-soluble resins mentioned above include natural polymers such as gum arabic, tragacan gum, locust bean gum, guar gum, choco gum, karaya gum, agar, starch, carrageenan, alginic acid, alginate, propylene glycol alginate, dextran, dextrin, amylose, gelatin, collagen, pullulan, pectin, amylopectin, sodium amylopectin semiglycolate, chitin, albumin, casein, polyglutamic acid, methylcellulose, ethylcellulose, propylcellulose, ethylmethylcellulose, hydroxycellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, hydroxypropyl starch, carboxymethylcellulose starch, alkali metal carboxymethylcellulose, alkali metal cellulose sulfate, and cellulose acetate. Examples of synthetic polymers include semi-synthetic polymers such as talates, starch-acrylic acid graft copolymers, cross-linked gelatin, phthalic acid-modified gelatin, and succinic acid-modified gelatin; and synthetic polymers such as polyvinyl alcohol, polyvinylpyrrolidone, polyvinyl methyl ether, methyl vinyl ester, polyacrylate (e.g., sodium polyacrylate), carboxyvinyl polymer, vinylpyrrolidone-ethyl acrylate copolymer, vinylpyrrolidone-styrene copolymer, vinylpyrrolidone-vinyl acetate copolymer, vinyl acetate-(meth)acrylic acid copolymer, vinyl acetate-crotonic acid copolymer, polyvinyl sulfonic acid, polyitaconic acid, polyhydroxyethyl acrylate, polyacrylamide, styrene-maleic acid anhydride copolymer, ethylene-maleic acid anhydride copolymer, and acrylamide-acrylic acid copolymer.

[0023] The amount of water contained in a patch-type formulation is generally 1 to 90% by mass, preferably 5 to 85% by mass. If the water content is too low, drug absorption slows down, and the cooling effect due to water evaporation when the patch is applied to the skin tends to decrease. Conversely, if the water content is too high, the fluidity of the water-soluble polymer increases, making it difficult to maintain the shape of the formulation.

[0024] The above-mentioned pap-type formulation may contain, as needed, resins such as acrylic resins, rubber, and silicone resins; humectants such as polyhydric alcohols (e.g., glycerin, polypropylene glycol); inorganic fillers such as kaolin, bentonite, zinc oxide, and titanium dioxide; viscosity modifiers; antioxidants; and so on.

[0025] Transdermal absorption enhancers may be added to the above base. Examples of transdermal absorption enhancers include alcohols such as menthol, camphor, and cetyl alcohol; fatty acid esters such as isopropyl palmitate and isopropyl myristate; glycerin esters such as glycerin monolaurate, glycerin monooleate, and glycerin monocaprate; acid amides such as diethanolamide laurate; and neutral surfactants such as polyethylene glycol dilauryl ether and sodium dodecyl sulfate. The amount of transdermal absorption enhancer added should be kept to a minimum; too little will not improve the transdermal absorption effect, while too much will reduce the viscosity. Therefore, 3 to 40 parts by mass per 100 parts by mass of the base is preferable.

[0026] The topical preparation or cosmetic composition of the present invention contains one or more of the following as a valuable substance: a lipolytic agent, a lipolytic agent, or a lipolytic agent. The valuable substance is an ingredient that works to reduce fat and is present in the preparation at a concentration of 0.1% by mass or more. For the breakdown, dissolution, or promotion of metabolism of subcutaneous fat, the content of the valuable substance is preferably 0.1 to 50% by mass, and more preferably 0.2 to 30% by mass. Furthermore, the amount of the valuable ingredient per square centimeter is preferably 1 μg to 100 mg. In addition to valuable substances having fat-decomposing / dissolving and fat-metabolizing effects, the topical preparation or cosmetic of the present invention can enhance its fat-decomposing and dissolving effect by using in combination ingredients that promote fat burning, ingredients that promote fat breakdown and excretion from fat cells, and skin-tightening ingredients.

[0027] Fat-degrading agents include lipase-like lipolytic enzymes, and hormones such as glucagon, adrenaline, noradrenaline, ghrelin, growth hormone, testosterone, and cortisol. Depending on the area and purpose of treatment, it is also effective to use in combination with proteases as protein-degrading enzymes, collagenase as collagen-degrading enzymes, hyaluronidase as hyaluronic acid-degrading enzymes, and enzyme-fermented plant extracts extracted from vegetables, fruits, and seaweed. Lipase is preferred as the fat-degrading agent. When using lipase, a lipase stabilizer may be included. For example, glycerol, glycine, mercaptoethanol, Triton X-100, Triton N-101, deoxycholic acid or its salt, Mg 2+ Ions, Ca 2+ Examples include ions, BSA, and salts. Mg 2+ Ions and Ca 2+ Ions can coexist as salts.

[0028] Examples of fat-dissolving agents include phosphatidylcholine, Fucus vesiculosus extract, tyrosine, adenosine triphosphate and its sodium salt, horse chestnut, Persian walnut, methylpropanediol, methylsilanol mannuronate, pasqueflower, Corydalis, deoxycholic acid or its salts, chenodeoxycholic acid, etc. Furthermore, examples include xanthine derivatives (caffeine, theophylline, theobromine, xanthine, aminophylline, choline theophylline, diprophylline, proxyphylline, and oxtrifyline, etc.), Cocculus trilobus extract, thistle extract, Stephania tetrandra extract, Curcuma zedoaria extract, Corydalis extract, Platycodon grandiflorus extract, Hedera helix extract, Pepper extract, Ipomoea purpurea root extract, Centella asiatica extract, Gardenia fruit extract, Hummaria oxycinnasa extract, Strawberry leaf extract, and others. The fat-dissolving agent is preferably one or more selected from the group consisting of phosphatidylcholine, adenosine triphosphate and its sodium salt, and deoxycholic acid or its salt. Furthermore, astaxanthin, tocopherol acetate, tocopherol, ascorbyl palmitate, and diethanolamine are preferred as stabilizers for phosphatidylcholine. When adding a salt of deoxycholic acid, it is desirable to include an acidic substance, such as citric acid, lactic acid, oleic acid, or tartaric acid, to promote penetration into the skin.

[0029] Examples of fat metabolism promoters include amino acids such as tyrosine, serine, threonine, phenylalanine, tryptophan, isoleucine, lysine, arginine, betaine, histidine, glutamine, glycine, and cysteine, while components that promote fat burning include L-carnitine, inositol, capsaicin, caffeine, coenzyme Q10, and catechin. The fat metabolism promoter is preferably one or more selected from the group consisting of amino acids, L-carnitine, inositol, capsaicin, and caffeine, and it is also preferable to use one or more amino acids from the above group.

[0030] While the above-mentioned beneficial substances and base are essential components in this invention, the addition of other beneficial substances for skin is not limited. Examples include pigment inhibitors, moisturizers, metabolic activators, antioxidants, reactive oxygen species scavengers, and radical scavengers.

[0031] Pigmentation inhibitors The present invention may include the addition of pigmentation inhibitors. Specific examples of pigmentation inhibitors include p-aminobenzoic acid derivatives, salicylic acid derivatives, benzenesulfonamide derivatives, imidazole derivatives, naphthalene derivatives, hydroxyanthranilic acid or its salts and their derivatives, anthranilic acid derivatives, coumarin derivatives, allantoin derivatives, nicotinic acid derivatives, ascorbic acid or its salts and their derivatives, tocopherol or its salts and their derivatives, tocotrienol or its salts and their derivatives, kojic acid or its derivatives, oxybenzone, benzophenone, guaiazulene, shikonin, baicalin or its salts and their derivatives, baicalein or its salts and their derivatives Examples include berberine or its salts and derivatives thereof, apigenin or its salts and derivatives thereof, luteolin or its salts and derivatives thereof, kaempferol or its salts and derivatives thereof, quercetin or its salts and derivatives thereof, quercitrin or its salts and derivatives thereof, isoquercitrin or its salts and derivatives thereof, rutin or its salts and derivatives thereof, myricetin or its salts and derivatives thereof, naringenin or its salts and derivatives thereof, hesperidin or its salts and derivatives thereof, glutathione or its salts and derivatives thereof, ellagic acid or its salts and derivatives thereof, and so on.

[0032] Moisturizer The present invention may contain added humectants. Specific examples of humectants include quince seed, agar or its derivatives, casein, glucose, galactose, mannose, xylose, fructose, maltose, isomaltose, cellobiose, genthiobiose, trehalose, pyralose, 1,3-butylene glycol, glycerin, propylene glycol, polyethylene glycol, dipropylene glycol, 1,2-pentanediol, 1,5-pentanediol, 1,2-hexanediol, 1,6-hexanediol, mannitol and sorbitol, 1,2-propanediol, 1,3-propanediol, polypropylene glycol, and 1,2-butanediol. , 1,3-butanediol, 1,4-butanediol, pentylene glycol, hexylene glycol, 1,3-pentanediol, 1,4-pentanediol, erythritol, pentaerythritol, dipentaerythritol, xylitol, maltitol, inositol, panthenol or its derivatives, dextrin, gelatin, pectin, starch, carrageenan, carboxymethyl chitin or chitosan, chitosan salt, sulfated chitin or chitosan, phosphorylated chitin or chitosan, alginic acid or its salt, hyaluronic acid or its salt, chondroitin sulfate or its salt, β-1,3-glucan, β-1,4-glucan, β-1,Examples include 6-glucan, glucosamine, heparin, ethylcellulose, methylcellulose, carboxymethylcellulose, carboxyethylcellulose, sodium carboxyethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, nitrocellulose, crystalline cellulose, hydroxypropyl methylcellulose, polyvinyl alcohol, polyvinyl methyl ether, polyvinylpyrrolidone, polyacrylates, carboxyvinyl polymers, water-soluble polymers such as dermatan sulfate and keratan sulfate, pyrrolidone carboxylic acid or its salts, polyglutamic acid or its salts, pyrrolidone carboxylic acid contained in natural moisturizing factors, urea, urocanic acid, betaine, sodium lactate, aspartic acid, glutamic acid, isoleucine, histidine, phenylalanine, threonine, serine, valine, proline, glycine, alanine, lysine, arginine, ceramides such as ceramide 1, ceramide 2, ceramide 3, ceramide 4, ceramide 5, ceramide 6II, and ceramide 9.

[0033] Metabolic activators Metabolic activators may be added to the present invention. Specific examples of metabolic activators include: Vitamin A group: retinol or its salts and derivatives thereof, retinal or its salts and derivatives thereof, dehydroretinal or its salts and derivatives thereof, retinoic acid or its salts and derivatives thereof, carotene or its salts and derivatives thereof, lycopene or its salts and derivatives thereof, Vitamin B group: Thiamine or its salts and derivatives thereof, riboflavin or its salts and derivatives thereof, pyridoxine or its salts and derivatives thereof, pyridoxal or its salts and derivatives thereof, cyanocobalamin or its salts and derivatives thereof, folic acid or its salts and derivatives thereof, nicotinic acid or its salts and derivatives thereof, pantothenic acid or its salts and derivatives thereof, biotin or its salts and derivatives thereof, choline or its salts and derivatives thereof, inositol or its salts and derivatives thereof, Vitamin C group: Ascorbic acid or its salts and their derivatives, Vitamin D group: Ergocalciferol or its salts and derivatives thereof, cholecalciferol and its salts and derivatives thereof, Vitamin E group, etc.: Tocopherol or its salts and derivatives thereof, tocotrienol or its salts and derivatives thereof, ubiquinone or its salts and derivatives thereof, linoleic acid or its salts and derivatives thereof, linolenic acid or its salts and derivatives thereof, arachidonic acid or its salts and derivatives thereof, etc., carnitine or its salts and derivatives thereof, ferulic acid or its salts and derivatives thereof, γ-oryzanol or its salts and derivatives thereof, Vitamin P group: Rutin or its salts and derivatives thereof, hesperidin or its salts and derivatives thereof, amino acids and others: Valine, leucine, isoleucine, threonine, methionine, phenylalanine, tryptophan, lysine, glycine, alanine, asparagine, glutamine, serine, cysteine, cystine, tyrosine, proline, hydroxyproline, aspartic acid, glutamic acid, hydroxylysine, arginine, ornithine, histidine or derivatives thereof, etc., as well as their sulfates, phosphates, nitrates, citrates, or amino acid derivatives such as pyrrolidone carboxylic acid, etc., α-hydroxy acids such as glycolic acid, citric acid, malic acid, tartaric acid, lactic acid, succinic acid, etc., 2-hydroxycarboxylic acids, polyhydroxycarboxylic acids or hydroxypolycarboxylic acids, lactobionic acid, photosensitizer 301, hinokitiol, pantothenic acid or derivatives thereof, allantoin, trimethylglycine, proteoglycans, etc.

[0034] Antioxidants Antioxidants may be added to the present invention. Specific examples of antioxidants include ascorbic acid or its salts and derivatives thereof, tocopherol or its salts and derivatives thereof, tocotrienol or its salts and derivatives thereof, butylhydroxytoluene (BHT), butylhydroxyanisole (BHA), coenzyme Qn (n=7~10), pyrroloquinoline quinone, propyl gallate, sesamol, and carotenoids. Since phosphatidylcholine is easily oxidized, it is desirable to include antioxidants such as astaxanthin, tocopherol acetate, tocopherol, and ascorbyl palmitate. The amount added is preferably 0.001 parts by mass or more per 1 part by mass of phosphatidylcholine. Furthermore, the presence of diethanolamine, ammonium chloride, ammonia, etc., further improves stability. The amount added is preferably 0.001 parts by mass or more.

[0035] Reactive oxygen species scavenger / Radical scavenger The present invention may include the addition of reactive oxygen species scavengers and radical scavengers. Specific examples of reactive oxygen species scavengers and radical scavengers include superoxide dismutase, catalase, glutathione peroxidase, bilirubin, quercetin, quercitrin, catechin, catechin derivatives, rutin or its derivatives, gallic acid or its salts and their derivatives, curcumin or its salts and their derivatives, transferrin, ceruloplasmin, coenzyme Qn (n=7~10), uric acid, bilirubin, metallothionein, and the like.

[0036] In addition to the above-mentioned components, the present invention may also include components commonly used in topical skin preparations such as cosmetics and pharmaceuticals. It consists of one or more components, such as aqueous components, oily components, plant extracts, animal extracts, powders, surfactants, oils, alcohols, pH adjusters, preservatives, thickeners, pigments, and fragrances, which are part of the base and may also function as valuable substances due to their effects on the skin (for example, skin tightening effect).

[0037] The external preparation or cosmetic composition of the present invention may also be in the form of a patch sheet. When topical preparations and cosmetics are applied as adhesive sheets, the size of the patch is typically between 0.5 and 300 square centimeters. Patches smaller than 0.5 square centimeters have limited effectiveness and are difficult to achieve. Patches larger than 300 square centimeters tend to have adhesion problems when covering the body surface. To cover a large body surface, multiple patches of 300 square centimeters or less can be used. Tapes and poultices are similar in size to patches. Alternatively, the adhesive sheet may be provided in a roll and cut to the appropriate size for use in different areas. In this case, the sheet width should be between 1 cm and 30 cm, and it should be portable.

[0038] For topical preparations and cosmetics in the form of adhesive sheets to be stably applied to and retained on the skin, it is not essential, but more preferable, to have a support sheet on the back of the adhesive base. Suitable support sheets, considering flexibility, include nonwoven fabrics, knitted fabrics, woven fabrics, polyurethane films, polyurethane foams, polyethylene films, PP (polypropylene), and EVA (ethylene vinyl acetate). For films, a thickness of 3 to 70 μm is appropriate. Polyurethane films with a thickness of 3 to 50 μm are particularly preferred. Polyurethane films with a thickness of 5 to 15 μm, which can be applied for long periods without skin irritation, are even more preferred as support sheets.

[0039] The manufacturing method for the topical preparations and cosmetics of the present invention differs depending on the adhesive base. When a solution-type adhesive is used as the base (adhesive composition A in the examples), the adhesive composition, various valuable substances, and other additives are uniformly mixed, the resulting adhesive solution is applied to a release sheet, the solvent is dried, and if necessary, the dried adhesive layer is laminated onto a support sheet and cut to an appropriate size to obtain the product. When a hot-melt type adhesive is used as the base (adhesive composition B in the examples), the adhesive composition, various valuable substances, and other additives are uniformly kneaded at a high temperature, and then the resulting adhesive mixture is applied to a release sheet or support sheet. When the base is a puff base (adhesive composition C in the examples), the adhesive composition, various valuable substances, and other additives are uniformly kneaded, and then the resulting water-soluble resin composition is applied to a release sheet or support sheet.

[0040] The topical preparation and cosmetic of the present invention are applied to the skin of the area where fat is to be removed. The application area is the entire skin and is not particularly limited. The number of applications of the topical preparation and cosmetic is determined according to the area where fat is to be removed. The application time for one application is approximately 0.5 to 48 hours, and for multiple applications, it is effective to apply them at intervals of 0 to 7 days.

[0041] This invention makes it possible to slim down specific areas of the body. It is particularly effective when applied to the face. For example, when applied to the area under the eyelids, it can reduce the puffiness (eye bags) under the eyelids. [Examples]

[0042] The present invention will be described in more detail below with reference to the following examples. These examples are merely illustrative examples of the present invention, and the scope of the present invention is not limited to these examples.

[0043] Examples 1-7 As shown in Table 1, 100 parts by mass of three adhesive compositions, including HiPAS® adhesive (acrylic ester, manufactured by Cosmedi Pharmaceutical Co., Ltd.), were mixed with phosphatidylcholine (Wako Pure Chemical Industries) and deoxycholic acid (Wako Pure Chemical Industries) dissolved in ethanol, as well as other components, to form a homogeneous solution. This solution was then applied to a 26 μm thick PET sheet and dried to obtain a tape-type formulation with a 50 μm thick adhesive layer.

[0044] [Table 1]

[0045] Adhesive composition A: A composition containing 10 parts by mass of isopropyl myristate (IPM) in 100 parts by mass of HiPAS® adhesive. Adhesive composition B: A composition obtained by mixing SIS, liquid paraffin, and Alcon P100 (tackifier) ​​in a ratio of 30:40:30 parts by mass while heating at 150°C. Adhesive composition C: A composition obtained by mixing sodium polyacrylate, concentrated glycerin, water, citric acid, and aluminum glycinate in a ratio of 8:30:50:1:0.1 parts by mass. Stabilizers: 1. Astaxanthin, 2. Tocopherol acetate, 3. Diethanolamine

[0046] Example 8: Manufacture of patch Various components were dissolved in ethanol and added to the adhesive solution so that the mass percentage after drying was as shown in Table 2, creating a homogeneous solution. This solution was then applied to a 40 μm thick release PET sheet and dried. After drying, it was transferred to a 10 μm thick urethane film, and a sheet-like formulation with a 50 μm thick adhesive layer was obtained. The obtained sheet was punched out into tape as shown in Figure 1 to obtain a 70 × 95 mm fat-burning patch.

[0047] [Table 2]

[0048] Evaluation of subcutaneous fat thickness <Number of subjects> 9 people <Measurement Period> First 2 weeks + Last 2 weeks *Subcutaneous fat thickness was measured before use, at 2 weeks of use, and at 4 weeks of use. <Application Method> Upper Arm: Apply to the outer side of the upper arm, starting 8 cm from the elbow. Abdomen: The patches were attached vertically on either side of the navel. <Duration of application> From the time immediately after bathing until before bathing the following day. Changed daily. <Measurement method> abdomen: Measurement of subcutaneous fat thickness: Measured using a Tanita subcutaneous fat thickness meter SR803. The measurement was taken approximately 5 cm horizontally from the navel, vertically to the right from the person's perspective. Upper arm: Measurement of subcutaneous fat thickness: Measured using a Tanita subcutaneous fat thickness meter SR803. The measurement was taken on the outer side of the upper arm, 10 cm from the elbow. <result> The pre-use measurement data was set to 100%, and the post-use values ​​were calculated. The results are shown in Tables 3 and 4 and Figures 2 and 3.

[0049] [Table 3]

[0050] [Table 4]

[0051] A clear reduction in subcutaneous fat was observed after 4 weeks of applying the patch agent of the present invention to the abdomen and upper arms.

Claims

1. A patch containing 0.2 to 30% by mass of a fat-dissolving agent for the purpose of fat reduction and / or localized fat reduction and / or skin tightening, The fat-dissolving agent is phosphatidylcholine and deoxycholic acid or a salt thereof. The adhesive sheet is an adhesive sheet with an acrylic or rubber-based adhesive as its base.

2. A method for manufacturing an adhesive sheet according to claim 1, comprising the following steps (a) or (b): (a) When the base is an acrylic adhesive, A step of uniformly mixing an adhesive solution, phosphatidylcholine, and deoxycholic acid or a salt thereof. The process involves applying the obtained adhesive solution onto a release sheet and drying the solvent, and A process of laminating the dried adhesive layer onto a support sheet as needed; (b) When the base is a rubber-based adhesive, A sticky composition, and a process of uniformly kneading phosphatidylcholine and deoxycholic acid or a salt thereof at high temperature, A step of applying the obtained adhesive mixture to a release sheet or support sheet.

Images