JP2022020578A - Cosmetic external preparation and cosmetic - Google Patents

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

The present invention relates to an external preparation and a cosmetic for the purpose of subcutaneous lipolysis / dissolution. More specifically, the present invention relates to the technical fields of external preparations and cosmetics containing a fat dissolving agent or the like as a main component as a valuable component.

Subcutaneous accumulation of fat is associated with adipocyte dysfunction, where the accumulated triglycerides are enzymatically degraded and redistributed into fatty acids, glycerol and / or glycerol esters. For various reasons, triglyceride accumulation occurs in adipocytes, resulting in subcutaneous fat accumulation. As a result, there are problems in overweight, treatment and beauty.

For obesity showing an excessive fat layer among the subcutaneous fat accumulation and obesity, a method of directly injecting a composition for removing the subcutaneous fat accumulation is adopted. For this, a phosphatidylcholine preparation represented by Lipostabil of Sanofi-Aventis is used (Patent Documents 1 and 2). On the other hand, subcutaneous injection of deoxycholic acid is also known. However, it can be said that it is a high-risk method because it is in a situation where it is regarded as a problem from the viewpoint of safety such as pain and swelling of the skin during the treatment. In addition, in the case of injection, the injection needle must be shaken subcutaneously for a certain area to inject. Furthermore, the convenience of fat dissolution changes depending on the unevenness of the injected liquid, and unevenness of the skin occurs.
Patent Document 3 proposes a wax-like dosage form using phosphatidylcholine, and Patent Document 4 proposes a liquid preparation composed of a carnitine derivative. However, no development has been made on external skin preparations such as patches, paps, and tapes.

Japanese Patent Publication No. 2007-509085 Special Table 2007-515439A Re-table 2009-12308 No. Japanese Unexamined Patent Publication No. 2006-16383

An object of the present invention is to provide a new means for administering a valuable substance having a fat dissolving action. Specifically, it is a patch-like, tape-like, or pap-like external preparation and cosmetic containing valuable resources having lipolytic and lipolytic effects.

Since there has been no transdermal preparation for the purpose of fat dissolution until now, there is no knowledge about the concentration of valuables, frequency of skin application, etc. when converting the above valuables into transdermal preparations, which is valuable. How to ensure the combination of substances, the stability of the pharmaceutical product and the transferability to the skin became important issues. The present inventors have solved such a problem and succeeded in producing an external preparation and a cosmetic containing a valuable resource having a fat-dissolving action, and have completed the present invention.

When the present inventors include a fat dissolving agent or the like as an active ingredient in a sheet-type patch type such as a patch, a poultice, or a tape, the valuable component is percutaneously absorbed to reduce fat or / and partially lose weight or /. And discovered that it can be used as an external preparation or cosmetic having an effect on skin tightening, and completed the present invention.
The present invention is as shown below.
[1] An external preparation or cosmetic containing one or more of a lipolytic agent, a fat dissolving agent or a fat metabolism promoting agent, for the purpose of reducing fat and / and partially thinning or / and tightening the skin.
[2] Fat reduction or / and partial thinning or / and skin containing 0.1% by mass or more of one or more components acting on fat reduction selected from the group consisting of lipolytic agents, fat dissolving agents and fat metabolism promoting agents. External agents or cosmetics for the purpose of tightening.
[3] The external preparation or cosmetic according to [1] or [2], wherein the lipolytic agent is lipase.
[4] The external preparation or cosmetic according to [3], which contains lipase, Mg salt and Ca salt.
[5] The external preparation or cosmetic according to [1] or [2], wherein the fat-dissolving agent is at least one selected from the group consisting of phosphatidylcholine, adenosine triphosphate and sodium salts thereof, and deoxycholic acid and salts thereof. Fee.
[6] The external preparation or cosmetic according to [1] or [2], wherein the fat metabolism promoter is at least one selected from the group consisting of amino acids, L-carnitine, inositol, capsaicin and caffeine.
[7] The external preparation according to [6], wherein the amino acid is at least one selected from the group consisting of tyrosine, serine, threonine, phenylalanine, tryptophan, isoleucine, lysine, arginine, betaine, histidine, glutamine, glycine and cysteine. Or cosmetics.
[8] The external preparation or cosmetic according to any one of [1] to [7], wherein the external preparation or cosmetic is a sticking sheet.
[9] The external preparation or cosmetic according to [8], which is based on an acrylic, rubber-based or silicone-based adhesive.
[10] The external preparation or cosmetic according to [8], which is based on a water-soluble resin.
[11] An external preparation or cosmetic in which phosphatidylcholine and one or more selected from the group consisting of astaxanthin, tocopherol acetate, tocopherol, ascorbyl palmitate and diethanolamine coexist.
[12] An external preparation or cosmetic in which sodium deoxycholate and an acidic substance coexist.
[13] The plaster is composed of a plaster and a support sheet, and the plaster contains one or more of a lipolytic agent, a lipolytic agent or a fat metabolism promoter in an acrylic, rubber or silicone adhesive. The external preparation or cosmetic according to any one of [1] to [9], wherein the support sheet is a non-woven fabric, a woven cloth, a knitted cloth or a polyurethane film, and the plaster thickness is 5 to 200 μm.
[14] The external preparation or cosmetic according to [13], wherein the support sheet is a polyurethane film having a thickness of 3 to 50 μm, the plaster is a roll-shaped viscous sheet, and the plaster has a thickness of 5 to 100 μm.
[15] The method for producing an external preparation or cosmetic according to any one of [8] to [10], which comprises the following steps (a), (b), or (c):
(A) When the base is a solution type adhesive
A step of uniformly mixing a pressure-sensitive adhesive solution and at least one valuable resource selected from the group consisting of a lipolytic agent, a lipolytic agent and a fat metabolism promoter.
A step of applying the obtained pressure-sensitive adhesive solution on a release sheet and drying the solvent, and a step of laminating the dried pressure-sensitive adhesive layer on the support sheet as needed;
(B) When the base is a hot melt type adhesive
A step of uniformly kneading the tacky composition and at least one valuable material selected from the group consisting of a lipolytic agent, a lipolytic agent and a fat metabolism promoter at a high temperature, and a release of the obtained pressure-sensitive adhesive mixture. The process of applying to a sheet or support sheet;
(C) If the base is a pap base,
Release at least one valuable resource selected from the group consisting of a water-soluble resin, a lipolytic agent, a lipolytic agent and a fat metabolism promoter, a step of uniformly kneading water, and the obtained water-soluble resin composition. The process of applying to a mold sheet or support sheet.

According to the present invention, the subcutaneous fat at the application site can be easily and uniformly dissolved.
The tape-type transdermal absorption preparation, patch-type transdermal absorption preparation, pap-type transdermal absorption preparation, etc., which are one aspect of the external preparation of the present invention, can be expected to have the effect of easily diffusing the adipose tissue into the subcutaneous tissue. , Decomposes, burns or dissolves subcutaneous fat in obese areas, partially thins, reduces eye bags and creates small face lines. In addition, a tightening effect can be expected by dissolving the subcutaneous fat in the slack portion.

Bottom view of the sheet-shaped pharmaceutical product of Example 8 as viewed from the support side. Graph showing changes in subcutaneous fat thickness in the abdomen Graph showing changes in subcutaneous fat thickness of the upper arm

The external preparation and cosmetics of the present invention are compositions in which valuable resources having a fat-dissolving action are dissolved and dispersed in a base, and it is more preferable that the composition is laminated on one surface of a support sheet. The external preparation or cosmetic of the present invention is suitably used for the purpose of reducing fat and / and partially thinning and / and tightening the skin.

The support sheet is not particularly limited, and a sheet generally used as a support sheet for a tape-type transdermal absorption preparation, a patch-type percutaneous absorption preparation, a pap-type percutaneous absorption preparation, or the like is preferable, for example. , Cellulose acetate, ethyl cellulose, polyethylene resin, polypropylene resin, ethylene-propylene copolymer, ethylene-vinyl acetate copolymer, vinyl chloride resin, vinylidene chloride resin, vinyl acetate-vinyl chloride copolymer, polyamide resin, polyester Examples thereof include sheets of resin, ABS resin, SIS resin, SEBS resin, PIB resin, urethane resin, silicone resin, aluminum and the like. Further, these sheets may be woven fabrics or non-woven fabrics of the fibers of the above materials, or may be laminated sheets of these sheets, woven fabrics and non-woven fabrics.

The above-mentioned base is not particularly limited, and a base conventionally used as a base of a transdermal absorption preparation can be used, and in the case of a tape-type transdermal absorption preparation or a patch-type percutaneous absorption preparation, an adhesive. Therefore, in the case of a tape-type transcutaneous absorption preparation, it is necessary that it has excellent adhesiveness to the skin and can be peeled off without adhesive residue. Therefore, an acrylic pressure-sensitive adhesive and a rubber-based pressure-sensitive adhesive are preferably used. Further, in the case of a pap-type preparation, a base composed of a water-soluble resin and water is generally used.

The acrylic pressure-sensitive adhesive is functional with a (co) polymer of an aliphatic alcohol having 4 to 18 carbon atoms and a (meth) acrylic acid alkyl ester, which is an ester of (meth) acrylic acid, and a (meth) acrylic acid alkyl ester. A (co) polymer with a sex monomer is preferably used.

Examples of the (meth) acrylic acid alkyl ester include butyl (meth) acrylic acid, isobutyl (meth) acrylic acid, hexyl (meth) acrylic acid, octyl (meth) acrylic acid, 2-ethylhexyl (meth) acrylic acid, and ( Examples thereof include isooctyl acrylate (meth), decyl (meth) acrylate, isodecyl (meth) acrylate, lauryl (meth) acrylate, and stearyl (meth) acrylate.

Examples of the functional monomer include 2-hydroxyethyl (meth) acrylate, hydroxypropyl (meth) acrylate, (meth) acrylic acid, maleic acid, maleic anhydride, fumaric acid, crotonic acid, and butyl maleate. Examples thereof include acrylamide, dimethylacrylamide, diethylacrylamide, butoxymethylacrylamide, ethoxymethylacrylamide, methylol (meth) acrylamide, dimethylaminoacrylate, N-vinyl-2-pyrrolidone and the like.

Further, a polymerizable monomer copolymerizable with the (meth) acrylic acid alkyl ester may be copolymerized, and examples of the polymerizable monomer include vinyl acetate, styrene, α-methylstyrene, vinyl chloride, acrylonitrile, and ethylene. Examples thereof include propylene and butadiene. The (meth) acrylic acid alkyl ester component of the (co) polymer is preferably 50% by mass or more.
Specifically, it is a copolymer of acrylic acid alkyl ester, and a copolymer of acrylic acid, acrylamide, vinyl acetate, etc. mainly containing acrylic acid alkyl ester. A plasticizer such as isopropyl myristate or isopropyl palmitate may be added to these adhesives to improve skin adhesion.

The thickness of the adhesive layer (plaster) is preferably 5 μm to 200 μm, more preferably 10 μm to 200 μm. It is also desirable that the thickness of the adhesive layer (plaster) is 5 μm to 100 μm. Specifically, HiPAS (registered trademark) adhesive (acrylic ester, manufactured by Cosmed Pharmaceutical Co., Ltd.) and MASCOS10 (trade name) adhesive (acrylic ester, manufactured by Cosmed Pharmaceutical Co., Ltd.) can be preferably used. ..

Further, the acrylic copolymer is preferably post-crosslinked with a metal chelate compound. In order to obtain appropriate cohesive force and adhesiveness, it is preferable to add 0.05 to 2.0 parts by mass of the metal chelate compound with respect to 100 parts by mass of the acrylic copolymer.

Examples of the metal chelate compound include aluminum acetylacetonate, aluminum glycinate, and aluminum hydroxide gel, which may be used alone or in combination.

Examples of the rubber-based pressure-sensitive adhesive include natural rubber, polyisiprene, polyisobutylene, polybutadiene, styrene-butadiene copolymer, styrene-butadiene-styrene copolymer, styrene-isoprene copolymer, and styrene-isoprene-styrene copolymer. Conventionally known rubber-based adhesives mainly composed of rubber such as urethane rubber can be used.

The rubber-based pressure-sensitive adhesive contains a tackifier such as a rosin-based resin, a polyterpene-based resin, a kumaron-inden-based resin, a petroleum-based resin, a terpene-phenol-based resin, and an alicyclic hydrocarbon, if necessary. You may. 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 pressure-sensitive adhesive and the tackifier.
Further, a plasticizer such as liquid paraffin, liquid polybutene, liquid polyisoprene, mineral oil lanolin, liquid polyacrylate, squalane, olive oil, a filler, an antiaging agent and the like may be added to the rubber-based pressure-sensitive adhesive.

Examples of the water-soluble resin include Arabic gum, tragan gum, locust bean gum, guar gum, echo gum, karaya gum, agar, starch, carrageenan, alginic acid, alginate, propylene glycol alginate, dextran, dextrin, amylose, gelatin, collagen, and purulan. , Pectin, amyropectin, amyropectin sodium semiglycolate, chitin, albumin, casein, polyglutamic acid and other natural polymers, methylcellulose, ethylcellulose, propylcellulose, ethylmethylcellulose, hydroxycellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, hydroxypropylstarch, carbokimethyl Semi-synthetic polymers such as sisterch, alkali metal carboxymethyl cellulose, alkali metal cellulose sulfate, cellulose acetate phthalate, starch-acrylic acid graft copolymer, cross-linked gelatin, phthalic acid-modified gelatin anhydride, succinic acid-modified gelatin, polyvinyl alcohol, polyvinyl Pyrrolidone, polyvinyl methyl ether, methyl vinyl ester, polyacrylate (eg, sodium polyacrylic acid), carboxyvinyl polymer, vinyl pyrrolidone-ethyl acrylate copolymer, vinyl pyrrolidone-styrene copolymer, vinyl pyrrolidone-vinyl acetate Polymers, vinyl acetate- (meth) acrylic acid copolymers, vinyl acetate-crotonic acid copolymers, polyvinyl sulfonic acid, polyitaconic acid, polyhydroxyethyl acrylates, polyacrylamides, styrene-maleic acid anhydride copolymers, Examples thereof include synthetic polymers such as an ethylene-maleic acid anhydride copolymer and an acrylamide-acrylic acid copolymer.

As for the amount of water contained in the pap-type preparation, if the water content is low, the absorption of the drug is delayed, and when the pap-type preparation is applied to the skin, the cooling effect due to the evaporation of water tends to decrease, and vice versa. When the amount is too large, the fluidity of the water-soluble polymer tends to increase, and it tends to be difficult to maintain the shape of the pharmaceutical product. Therefore, it is generally 1 to 90% by mass, preferably 5 to 85% by mass.

The above-mentioned pap-type preparations include, if necessary, resins such as acrylic resins, rubbers and silicone resins, moisturizers such as polyhydric alcohols (eg, glycerin and polypropylene glycol), kaolin, bentonite, zinc flower and titanium dioxide. Inorganic fillers such as, viscosity modifiers, antiaging agents and the like may be added.

A transdermal absorption promoter may be added to the base. Examples of the transdermal absorption promoter 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 lauric acid diethanolamide; neutral surfactants such as polyethylene glycol dilauryl ether and sodium dodecyl sulfate can be mentioned.
If the amount of the percutaneous absorption accelerator added is too small, the percutaneous absorption effect is not improved, and if it is too large, the adhesiveness is lowered. Therefore, 3 to 40 parts by mass is preferable with respect to 100 parts by mass of the base.

The external preparation or cosmetic of the present invention contains at least one of a lipolytic agent, a fat dissolving agent and a fat metabolism promoting agent as a valuable resource. Valuables are components that act to reduce fat and are contained in the pharmaceutical product in an amount of 0.1% by mass or more. The content of valuables is preferably 0.1 to 50% by mass, more preferably 0.2 to 30% by mass, for the purpose of decomposing, dissolving or promoting metabolism of subcutaneous fat. Further, the amount of the valuable component per square cm is preferably 1 μg to 100 mg.
In addition to valuable resources having lipolysis / dissolution and lipolysis promoting effects, the external preparation or cosmetic of the present invention is used in combination with a component that promotes fat burning, a component that promotes lipolysis and excretion from adipocytes, a skin tightening component, and the like. By doing so, the lipolysis / dissolving effect can be enhanced.

Lipolytic agents include lipolytic enzymes such as lipase, hormones such as glucagon, adrenaline, noradrenaline, ghrelin, growth hormone, testosterone, cortisol, and the like. It is also effective to use protease as a proteolytic enzyme, collagenase as a collagen degrading enzyme, hyaluronidase as a hyaluronidase degrading enzyme, and an enzyme fermented plant extract fermented and extracted from vegetables, fruits and seaweed according to the care site and purpose. be.
Lipase is the preferred lipolytic agent. When lipase is used, a lipase stabilizer may coexist. For example, glycerol, glycine, mercaptoethanol, triton X-100, triton N-101, deoxycholic acid or a salt thereof, Mg ²⁺ ion, Ca ²⁺ ion, BSA, salts and the like can be mentioned. Mg ²⁺ ions and Ca ²⁺ ions may coexist as salts.

Examples of the fat dissolving agent include phosphatidylcholine, hibamata extract, tyrosine, adenosine triphosphate and its sodium salt, horse chestnut, persian glumi, methylpropanediol, methylsilanol mannuronate, okinagusa, fumitory man, deoxycholic acid or its salt, and chenodeoxycholic acid. Acid, etc. can be mentioned. Furthermore, xanthin derivatives (caffeine, theophylline, theobromine, xanthin, aminophyllin, cholineteophylline, diprophylline, proxiphyllin, oxtriphyllin, etc.), Aotsuzurafuji (Kibomi) extract, Azami extract, Otsuzurafuji (self-defense) extract, Gajutsu (莪朮) ) Extract, Karakusakeman extract, Kyoko (kikyo, Kikyo root) extract, Kizuta extract, pepper (kosho) extract, Sarashinayouma root extract, Tupokusa extract, Guchinashi fruit extract, Fumaria okinus extract, strawberry leaf extract, and the like.
The fat-dissolving agent is preferably one or more selected from the group consisting of phosphatidylcholine, adenosine triphosphate and sodium salts thereof, and deoxycholic acid or salts thereof.
Further, as the stabilizer of phosphatidylcholine, astaxanthin, tocopherol acetate, tocopherol, ascorbyl palmitate, diethanolamine and the like are preferable. When a salt of deoxycholic acid is added, it is desirable to coexist with an acidic substance such as citric acid, lactic acid, oleic acid, tartaric acid, etc. in order to promote penetration into the skin.

Amino acids such as tyrosine, serine, threonine, phenylalanine, tryptophan, isoleucine, lysine, arginine, betaine, histidine, glutamine, glycine, and cysteine as fat metabolism promoters, and L-carnitine, inositol, and capsaicin as fat burning promoters. , Caffeine, coenzyme Q10, catechin, etc.
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 preferable to use one or more amino acids from the above.

The above valuables and bases are essential ingredients in the present invention, but the addition of other skin valuables is not limited. For example, a pigmentation inhibitor, a moisturizer, a metabolism activator, an antioxidant, an active oxygen scavenger / radical scavenger, and the like can be mentioned.

Pigmentation inhibitor A pigmentation inhibitor can be added to the present invention. Specific examples of the pigmentation inhibitor include p-aminobenzoic acid derivative, sulcylic acid derivative, benzenesulfonamide derivative, imidazole derivative, naphthalene derivative, hydroxyanthranic acid or a salt thereof, and their derivatives, anthranic acid derivative, coumarin derivative, and allantin. Derivatives, nicotinic acid derivatives, ascorbic acid or salts thereof and derivatives thereof, tocopherols or salts thereof and derivatives thereof, tocotrienol or salts thereof and derivatives thereof, kodiic acid or derivatives thereof, oxybenzone, benzophenone, guaiazulene, ciconin, bicarin or Its salts and their derivatives, baicalene or its salts and their derivatives, velverin or its salts and their derivatives, apigenin or its salts and their derivatives, luteolin or its salts and their derivatives, kenferol or its salts and theirs. Derivatives of quercetin or salts thereof and derivatives thereof, quercitrin or salts thereof and derivatives thereof, isoquercitrin or salts thereof and derivatives thereof, rutin or salts thereof and derivatives thereof, mylicetin or salts thereof and derivatives thereof. , Naringenin or salts thereof and derivatives thereof, hesperidin or salts thereof and derivatives thereof, glutathione or salts thereof and derivatives thereof, ellagic acid or salts thereof and derivatives thereof, and the like.

Moisturizer A moisturizer can be added to the present invention. Specific examples of moisturizers include quince seeds, agar or derivatives thereof, casein, glucose, galactose, mannose, xylose, fructose, maltose, isomartose, cellobiose, gentiobiose, 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, 1,2-Butanediol, 1,3-Butanediol, 1,4-Butanediol, Pentylene Glycol, Hexylene Glycol, 1,3-Pentanediol, 1,4-Pentanediol , Erythritol, pentaerythritol, dipentaerythritol, xylitol, martitol, inositol, pantenol or derivatives thereof, dextrin, gelatin, pectin, starch, carrageenan, carboxymethyl chitin or chitosan, chitosan salt, sulfated chitin or chitosan, phosphorylation. 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-1,6-glucan, glucosamine, heparin, ethylcellulose , Methyl cellulose, carboxymethyl cellulose, carboxyethyl cellulose, sodium carboxyethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, nitrocellulose, crystalline cellulose, hydroxypropylmethylcellulose, polyvinyl alcohol, polyvinylmethyl ether, polyvinylpyrrolidone, polyacrylic acid salt, carboxyvinyl polymer, dermatane Water-soluble polymers such as sulfuric acid and keratane sulfate, pyrrolidone carboxylic acid or a salt thereof, polyglutamic acid or a salt thereof, pyrrolidone carboxylic acid contained in a natural moisturizing factor, urea, urocanic acid, betaine, sodium lactate, aspartic acid, glutamate. , Isoleucine, histidine, phenylalanine, threonine, serine, valine, proline, glycine, alanine, lysine, arginine, ceramide 1, ceramide 2, ceramide 3, ceramide 4, ceramide 5, ceramide 6II, ceramides such as ceramide 9, etc. Can be mentioned.

Metabolite Activator A metabolism activator can be added to the present invention. Specific examples of the metabolic activator include vitamin A group: retinol or a salt thereof and a derivative thereof, retinal or a salt thereof and a derivative thereof, dehydroretinal or a salt thereof and a derivative thereof, retinoic acid or a salt thereof and a derivative thereof. , Carotene or its salts and their derivatives, lycopene or its salts and their derivatives,
B vitamins: thiamine or a salt thereof and a derivative thereof, riboflavin or a salt thereof and a derivative thereof, pyridoxine or a salt thereof and a derivative thereof, pyridoxal or a salt thereof and a derivative thereof, cyanocobalamine or a salt thereof and a derivative thereof, folic acid. Or salts thereof and derivatives thereof, nicotinic acid or salts thereof and derivatives thereof, pantothenic acid or salts thereof and derivatives thereof, biotin or salts thereof and derivatives thereof, choline or salts thereof and derivatives thereof, inositol or salts thereof. And their derivatives,
Vitamin C group: ascorbic acid or its salts and their derivatives,
Vitamin D group: ergocalciferol or its salt and its derivatives, choleciferol and its salts and their derivatives,
Vitamin E group, etc .: tocopherol or a salt thereof and a derivative thereof, tocotrienol or a salt thereof and a derivative thereof, ubiquinone or a salt thereof and a derivative thereof, linoleic acid or a salt thereof and a derivative thereof, linolenic acid or a salt thereof and their salts. Derivatives, arachidonic acid or salts thereof and derivatives thereof, carnitine or salts thereof and derivatives thereof, ferulic acid or salts thereof and derivatives thereof, γ-orizanol or salts thereof and derivatives thereof,
Vitamin P group: rutin or its salt and its derivatives, hesperidin or its salts and their derivatives, amino acids, etc .: valine, leucine, isoleucine, treonine, 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, and their sulfates, phosphates, nitrates, citrates, or pyrrolidone carboxylics. Amino acids such as amino acid derivatives such as acids, α-hydroxy acids such as glycolic acid, citric acid, malic acid, tartaric acid, lactic acid and succinic acid, 2-hydroxycarboxylic acids, polyhydroxycarboxylic acids or hydroxypolycarboxylic acids, lactobionic acid. , Photosensitizer No. 301, hinokithiol, pantothenic acid or a derivative thereof, allantin, trimethylglycine, proteoglycan, and the like.

Antioxidants Antioxidants can be added to the present invention. Specific examples of antioxidants include ascorbic acid or a salt thereof and a derivative thereof, tocopherol or a salt thereof and a derivative thereof, tocotrienol or a salt thereof and a derivative thereof, butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), and the like. Examples thereof include coenzyme Qn (n = 7 to 10), pyroquinolinquinone, propyl ascorbic acid, sesamol, carotenoids and the like. Since phosphatidylcholine is easily oxidized, it is desirable to coexist with an antioxidant such as astaxanthin, tocopherol acetate, tocopherol, and ascorbyl palmitate. The amount added is preferably 0.001 part by mass or more with respect to 1 part by mass of phosphatidylcholine. Further, when diethanolamine, ammonium chloride, ammonia and the like coexist, the stability is further improved. The addition amount is preferably 0.001 part by mass or more.

Active oxygen scavenger / radical scavenger An active oxygen scavenger / radical scavenger can be added to the present invention. Specific examples of active oxygen scavengers / radical scavengers include superoxide dismutase, catalase, glutathione peroxidase, birylbin, quercetin, quercitrin, catechin, catechin derivatives, rutin or derivatives thereof, gallic acid or salts thereof, and derivatives thereof, curcumin. Alternatively, salts thereof and derivatives thereof, transferase, celluloplasmin, coenzyme Qn (n = 7 to 10), uric acid, gallic acid, metallothioneine, and the like can be mentioned.

In addition to the above-mentioned constituent components, components usually used for external skin preparations such as cosmetics and pharmaceuticals may be added to the present invention. It consists of one or more components consisting of aqueous components, oily components, plant extracts, animal extracts, powders, surfactants, oils, alcohols, pH regulators, preservatives, thickeners, pigments, fragrances, etc. It may also act as a valuable resource due to its effect on the skin (eg, skin tightening action) as a part of the base.

The external preparation or cosmetic of the present invention may be a sticking sheet.
When the external preparation and the cosmetic used as the patch sheet are patch agents, the size of the patch is 0.5 to 300 square cm. If it is less than 0.5 square cm, the effect is limited and the effectiveness is difficult to be exhibited. If it exceeds 300 square cm, there is a tendency for problems in adhesion to cover the body surface. To cover a wide body surface, a plurality of patches of 300 square cm or less may be used. The tape agent and the poultice agent have the same size as the patch agent.
Separately, the pasted sheet may be made into a roll-shaped sheet, cut according to the part to be used, and used in an appropriate size. In that case, the seat width may be 1 cm or more and 30 cm or less and a portable size.

In order to stably apply the external preparation and cosmetics, which are adhesive sheets, to the skin and hold them on the skin, it is not essential, but more preferable, to have a support sheet on the back surface of the adhesive base.
As the support sheet, non-woven fabric, knitted cloth, woven cloth, polyurethane film, polyurethane foam, polyethylene film, PP (polypropylene), EVA (ethylene vinyl acetate) and the like are suitable in consideration of flexibility. For films, a thickness of 3 to 70 μm is suitable. In particular, a polyurethane film having a thickness of 3 to 50 μm is preferable. A polyurethane film having a thickness of 5 to 15 μm that can be applied for a long time without stuffiness on the skin is more preferable as the support sheet.

In order to produce the external preparation / cosmetic of the present invention, the production method differs depending on the adhesive base. When a solution-type adhesive is used as a base (adhesive composition A in Examples), the adhesive composition, various valuable resources, and other additives are uniformly mixed, and the obtained adhesive solution is used as a release sheet. It is applied on top and the solvent is dried, and if necessary, a dried pressure-sensitive adhesive layer is laminated on a support sheet and cut into an appropriate size to obtain a product. When the hot melt type adhesive is used as a base (adhesive composition B in Examples), the adhesive composition, various valuable resources, and other additives are uniformly kneaded at a high temperature, and then the obtained adhesive mixture is obtained. Is applied to the release sheet or the support sheet. When the base is a pap base (tacky composition C in Examples), the sticky composition, various valuable resources, and other additives are uniformly kneaded, and then the obtained water-soluble resin composition is released from the mold. Apply to sheet or support sheet.

The external preparation and cosmetics of the present invention are applied to the skin of the site where fat is desired to be removed. The application site is the entire skin and is not particularly limited. Set the number of external agents and cosmetics to be applied according to the area where you want to remove fat. The application time for one time is about 0.5 hours to 48 hours, and in the case of multiple applications, it is effective to apply at intervals of 0 to 7 days.

According to the present invention, it is possible to partially thin a desired part of the body. In particular, application to the face is likely to be effective. For example, when applied under the eyelids, the effect of reducing the bulge (eyelids) under the eyelids can be obtained.

Hereinafter, the present invention will be described in more detail with reference to the following examples. These examples are merely examples for specifically explaining the present invention, and the scope of the present invention is not limited to these examples.

Examples 1-7
As shown in Table 1, phosphatidylcholine (Wako Pure Chemical Industries, Ltd.) dissolved in ethanol in 100 parts by mass of three kinds of pressure-sensitive adhesive compositions such as HiPAS (registered trademark) pressure-sensitive adhesive (acrylic ester, manufactured by Cosmed Pharmaceutical Industries, Ltd.) ), Deoxycholic acid (Wako Pure Chemical Industries, Ltd.), and other ingredients to make a uniform solution, which is applied to a PET sheet with a thickness of 26 μm, dried, and a tape-type preparation in which a pressure-sensitive adhesive layer with a thickness of 50 μm is laminated. Got

Adhesive composition A: Composition containing 10 parts by mass of isopropyl myristate (IPM) in 100 parts by mass of HiPAS (registered trademark) Adhesive composition B: SIS, liquid paraffin, 30 parts of Archon P100 (adhesive imparting agent) : 40: 30 parts by mass of composition mixed while heating at 150 ° C. Adhesive composition C: Sodium polyacrylate, concentrated glycerin, water, citric acid, aluminum glycinate 8:30:50: 1 : Composition stabilizer mixed at a ratio of 0.1 parts by mass: 1. Astaxanthin, 2. Tocopherol acetate, 3. Diethanolamine

Example 8 Production of patch agent Various components are dissolved in ethanol and added to the adhesive solution so that the parts by mass after drying are shown in Table 2, and the solution is made uniform and applied to a release PET sheet having a thickness of 40 μm. After drying, the product was transferred to a urethane film (thickness 10 μm) to obtain a sheet-like preparation having an adhesive layer having a thickness of 50 μm laminated. The obtained sheet was punched into a tape as shown in FIG. 1 to obtain a fat burning patch having a size of 70 × 95 mm.

Evaluation of subcutaneous fat thickness <Number of subjects> 9 subjects <Measurement period> First half 2 weeks + Second half 2 weeks * Subcutaneous fat thickness was measured before use, 2 weeks after use, and 4 weeks after use.
<Application method> Upper arm: Attached from 8 cm from the elbow on the outside of the upper arm.
Abdomen: Attached vertically to the left and right with the navel in between.
<Attachment time> From the longest bathing period to the next day before bathing. I replaced it every day.
<Measuring method>
Abdomen: Subcutaneous fat thickness measurement: Measured using Tanita Subcutaneous Fat Thickness Gauge SR803.
The measurement was performed about 5 cm from the navel and vertically to the right of the person.
Upper arm: Subcutaneous fat thickness measurement: Measured using Tanita Subcutaneous Fat Thickness Gauge SR803.
A measurement was made 10 cm from the elbow on the outside of the upper arm.
<result>
The measurement data before use was set to 100%, and the numerical value after use was calculated. The results are shown in Tables 3 and 4 and FIGS. 2 and 3.

A clear decrease in subcutaneous fat was observed in 4 weeks by the patch of the present invention applied to the abdomen and upper arm.

Claims (15)

An external preparation or cosmetic containing one or more of a lipolytic agent, a fat dissolving agent or a fat metabolism promoting agent, for the purpose of reducing fat and / and partially thinning or / and tightening the skin. For the purpose of fat reduction and / and partial thinning or / and skin tightening containing 0.1% by mass or more of one or more components acting on fat reduction selected from the group consisting of lipolytic agents, fat dissolving agents and fat metabolism promoters. External preparations or cosmetics. The external preparation or cosmetic according to claim 1 or 2, wherein the lipolytic agent is lipase. The external preparation or cosmetic according to claim 3, which contains a lipase, an Mg salt and a Ca salt. The external preparation or cosmetic according to claim 1 or 2, wherein the fat-dissolving agent is at least one selected from the group consisting of phosphatidylcholine, adenosine triphosphate and sodium salts thereof, and deoxycholic acid and salts thereof. The external preparation or cosmetic according to claim 1 or 2, wherein the fat metabolism promoter is at least one selected from the group consisting of amino acids, L-carnitine, inositol, capsaicin and caffeine. The external preparation or cosmetic according to claim 6, wherein the amino acid is at least one selected from the group consisting of tyrosine, serine, threonine, phenylalanine, tryptophan, isoleucine, lysine, arginine, betaine, histidine, glutamine, glycine and cysteine. .. The external preparation or cosmetic according to any one of claims 1 to 7, wherein the external preparation or cosmetic is a sticking sheet. The external preparation or cosmetic according to claim 8, which is based on an acrylic, rubber-based or silicone-based adhesive. The external preparation or cosmetic according to claim 8, which is based on a water-soluble resin. An external preparation or cosmetic in which phosphatidylcholine coexists with at least one selected from the group consisting of astaxanthin, tocopherol acetate, tocopherol, ascorbyl palmitate and diethanolamine. An external preparation or cosmetic in which sodium deoxycholate and an acidic substance coexist. It is composed of a plaster body and a support sheet, and the plaster body contains one or more of a lipolytic agent, a lipolytic agent or a fat metabolism promoter in an acrylic, rubber or silicone adhesive, and the said. The external preparation or cosmetic according to any one of claims 1 to 9, wherein the support sheet is a non-woven fabric, a woven cloth, a knitted cloth or a polyurethane film, and the thickness of the plaster is 5 to 200 μm. The external preparation or cosmetic according to claim 13, wherein the support sheet is a polyurethane film having a thickness of 3 to 50 μm, the plaster is a roll-shaped sheet, and the plaster has a thickness of 5 to 100 μm. The method for producing an external preparation or cosmetic according to any one of claims 8 to 10, which comprises the following steps (a), (b), or (c):
(A) When the base is a solution type adhesive
A step of uniformly mixing a pressure-sensitive adhesive solution and at least one valuable resource selected from the group consisting of a lipolytic agent, a lipolytic agent and a fat metabolism promoter.
A step of applying the obtained pressure-sensitive adhesive solution on a release sheet and drying the solvent, and a step of laminating the dried pressure-sensitive adhesive layer on the support sheet as needed;
(B) When the base is a hot melt type adhesive
A step of uniformly kneading the tacky composition and at least one valuable material selected from the group consisting of a lipolytic agent, a lipolytic agent and a fat metabolism promoter at a high temperature, and a release of the obtained pressure-sensitive adhesive mixture. The process of applying to a sheet or support sheet;
(C) If the base is a pap base,
Release at least one valuable resource selected from the group consisting of a water-soluble resin, a lipolytic agent, a lipolytic agent and a fat metabolism promoter, a step of uniformly kneading water, and the obtained water-soluble resin composition. The process of applying to a mold sheet or support sheet.

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