DE10054479A1 - Cosmetic plasters for skin lightening - Google Patents

Abstract

The invention relates to cosmetic plasters containing novel combinations of active ingredients for bleaching the skin.

Description

The present invention relates to cosmetic plasters with new combinations of active ingredients for skin lightening.

Melanins are brown to black pigments and are found, for example, in the skin of the Humans and in vertebrates in certain cells, the melanocytes. below differ in skin color as well as freckles, liver spots or age spots, be do not rest on an increased number of melanocytes, but on an increased one Melanin concentration in the affected areas. During normal skin pig Noticeable pigmentants make a significant contribution to protection against UV radiation For many consumers, accumulations such as freckles or age spots are cosmetic Problem.

Since the enzyme tyrosinase is involved in the formation of melanin, the inhibition of this constitutes Enzyme is an important starting point in the development of skin lightening agents. Agents with a tyrosinase inhibiting effect are known in the prior art, for example ascorbic acid and kojic acid (JP 2780803 B2), hydroquinone (JP 2540581 B2), and the derivatives of these compounds. Furthermore, the use of Plant extracts containing skin-lightening active ingredients are known. Suitable plants are z. B. mulberry tree (JP 3106811 A), licorice (JP 5186324 B2), cucumber and lime (WO 99/49878 A1). However, many of these substances have the disadvantage that they are not oxida tion and storage are stable, especially if they are incorporated into cosmetic emulsions are.

Combinations of skin-lightening substances, in particular of, are also known Ascorbic acid derivatives with other cosmetic active ingredient classes, e.g. B. with skin soothing  Substances. The published patent application WO 98/34591 A1 discloses emulsions with magne sium ascorbyl phosphate and bisabolol as skin lightening agents. For a visible effect to achieve a treatment duration of at least 3 to 6 months with daily, Recommended for up to two applications (page 37, second paragraph). This is for many consumers difficult to carry out. Lack of consumer compliance, however, sets in positive result of the cosmetic treatment in question.

The use of a skin lightening agent is often only in a smaller area of the skin necessary, but should be done more intensely than is possible with a cream treatment is. A better one for topical local administration of cosmetic active ingredients a suitable means is a plaster.

Cosmetic plasters for lightening the skin are known in the prior art. In the patent GB 2 265 086 B discloses plasters which contain skin-lightening substances. at Cosmetic skin treatment with plasters is achieved through the occlusive effect and optionally additional permeation enhancers an improved transport of the active ingredients into the upper layers of the skin. The plasters known in the prior art come however, it often causes skin irritation due to the occlusion.

The object of the present invention was to remedy the shortcomings of the prior art and to provide a cosmetic agent suitable for skin lightening, the is comfortable and safe to use and has a minimal potential for use Has skin irritation.

Surprisingly, it was found that a patch with a combination of (a) at least a substance selected from the derivatives of ascorbic acid, kojic acid, hydroquinone, Arbutin, mulberry extract and licorice extract, (b) at least one substance selects from panthenol and the derivatives of 2-furanone, and (c) bisabolol, and optionally other common cosmetic additives an effective and gentle at the same time represents cosmetic means for lightening the skin.

A first object of the present invention is a cosmetic plaster for skin application whitening, which has a top layer, an active substance reservoir, an adhesive layer and a removable Contains protective layer and is characterized by an active ingredient combination of (a) at least  a substance selected from the derivatives of ascorbic acid, kojic acid, hydro quinone, arbutin, mulberry extract and licorice extract, (b) at least one substance, selected from panthenol and the derivatives of 2-furanone, and (c) bisholol. The skin-lightening components (a) are selected from the derivatives of ascorbic acid, Kojic acid, hydroquinone, arbutin, mulberry extract and licorice extract as well as a mixture towards this. The ascorbins are preferred both as a single substance and in a mixture acid derivatives and kojic acid. Sodium ascorbyl phosphate, magne are particularly preferred sium ascorbyl phosphate, ascorbyl monopalmitate, ascorbyl dipalmitate, ascorbyl monostearate, Ascorbyl distearate, ascorbyl monoethyl hexanoate, ascorbyl diethyl hexanoate, ascorbyl mono octanoate, ascorbyl dioctanoate, ascorbyl monoisostearate and ascorbyl diisostearate. The Ascorbic acid derivatives which are extremely preferred according to the invention are sodium ascorbyl phosphate and magnesium ascorbyl phosphate.

The skin-calming components (b) are selected from panthenol and the derivatives of 2-furanone with the general structural formula (I), and mixtures thereof.

Preferred are the 2-furanone derivatives in which the substituents R ¹ to R ⁶ independently of one another are a hydrogen atom, a hydroxyl radical, a methyl, methoxy, aminomethyl or hydroxymethyl radical, a saturated or mono- or di-unsaturated, linear or branched C ₂ -C ₄ hydrocarbon residue, a saturated or mono- or di-unsaturated, branched or linear mono-, di- or trihydroxy-C ₂ -C ₄ -hydrocarbon residue or a saturated or mono- or di-unsaturated, branched or linear arene mono-, di- or triamino-C ₂ -C ₄ hydrocarbon radical. Particularly preferred derivatives are the commercially available substances dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone (pantolactone, from Merck), 4-hydroxymethyl-γ-butyrolactone (Merck), 3.3 -Dimethyl-2-hydroxy-γ-butyrolactone (Aldrich) and 2,5-dihydro-5-methoxy-2-furanone (Merck), all stereoisomers being expressly included. The 2-furanone derivative which is extremely preferred according to the invention is pantolactone (dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone).

In a particularly preferred embodiment of the invention, the active ingredients are with the Adhesive layer and optionally other conventional cosmetic additives into one Matrix mixed, which extends over the entire pavement area. This embodiment is referred to according to the invention as a matrix plaster.

In a further preferred embodiment of the invention, the active ingredients are in gel like or pasty aqueous dispersions and optionally mixed with other usual cosmetic additives. This reservoir contains no glue and occupies only one or more limited segments on the pavement surface. This According to the invention, the embodiment is referred to as a reservoir plaster.

In a particularly preferred embodiment of the invention, the active substance reservoir or the active substance matrix contains at least one polymer to increase the cosmetic effect. Particularly suitable as polymers are natural polymers which are optionally chemically and / or physically modified, such as cellulose, nonionic cellulose derivatives, especially hydroxypropyl cellulose, hydroxyethyl cellulose and methyl hydroxypropyl cellulose, as well as quaternized cellulose derivatives, especially polyquaternium-24 and the commercial products Celquat® and Polymer JR®, and preferably Celquat® H 100, Celquat® L 200 and Polymer JR®400, furthermore dextran, dextran sulfate, chondroitin, chondroitin sulfate, chitin and chitin derivatives, in particular chitosan and its derivatives (e.g. the products Hydagen® CMF, Hydagen® HCMF, Kytamer ® PC and Chitolam® NB / 101), wherein particularly suitable chitosans have a degree of deacetylation of at least 80% and a molecular weight of 5.10 ⁵ to 5.10 ⁶ g / mol, hyaluronic acid and its derivatives, polysaccharide from fucose or rhamnose units , Xanthan gum, carrageenan, tragacanth, glycane and starch and starch derivatives, the g may also be thermally modified.

According to the invention, synthetic polymers which are cationic, can be anionic, amphoteric or non-ionic. A particularly suitable one Cationic homopolymer is the optionally crosslinked poly (methacryloyloxyethyltri methylammonium chloride) with the INCI name Polyquaternium-37. The networking can with the help of polyolefinically unsaturated compounds, for example divinyl benzene, tetraallyloxyethane, methylenebisacrylamide, diallyl ether, polyallylpolyglyceryl ether,  or allyl ethers of sugars or sugar derivatives such as erythritol, pentaerythritol, arabitol, Mannitol, sorbitol, sucrose or glucose. Methylene bisacrylamide is a preferred one Crosslinking agent. The homopolymer is preferably in the form of a non-aqueous one Polymer dispersion which should not have a polymer content below 30% by weight, used. Such polymer dispersions are available under the names Salcare® SC 95 (approx. 50% polymer content in mineral oil and tridecyl polyoxypropylene polyoxyethylene ether) and Salcare® SC 96 (approx. 50% polymer content in tridecyl polyoxypropylene polyoxyethylene ether and Propylene glycol diesters of caprylic and capric acid) are commercially available.

Furthermore, copolymers are preferably used which contain methacryloyloxyethyltrimethylammonium chloride and, as nonionic monomer units, preferably acrylamide, methacrylamide, C _1-4 -alkyl acrylate and C _1-4 -alkyl methacrylate. Among these nonionic monomers, acrylamide is particularly preferred. These copolymers can also be crosslinked, as described above for the homopolymers. A preferred copolymer according to the invention is the crosslinked acrylamide-methacryloyloxyethyltrimethylammonium chloride copolymer, commercially available e.g. B. available as an approximately 50% non-aqueous polymer dispersion under the name Salcare® SC 92.

Anionic polymers, the effect of the active ingredient used according to the invention support, contain carboxylate and / or sulfonate groups and as monomers for example Acrylic acid, methacrylic acid, crotonic acid, maleic anhydride and 2-acrylamido-2-methyl propane sulfonic acid. The acid groups can be wholly or partly as sodium, Potassium, ammonium, mono- or triethanolammonium salt are present. Preferred mono mers are 2-acrylamido-2-methylpropanesulfonic acid and acrylic acid.

Very particularly preferred anionic polymers contain 2-acrylamido-2-methylpropanesulfonic acid as the sole monomer or as comonomer, it being possible for the sulfonic acid group to be wholly or partly in salt form. The homopolymer of 2-acrylamido-2-methylpropanesulfonic acid, e.g. B. the commercial product Rheothik®11-80. Within this embodiment, it may be preferred to use copolymers of at least one anionic monomer and at least one nonionic monomer. Regarding the anionic monomers, reference is made to the substances listed above. Preferred nonionic monomers are acrylamide, methacrylamide, acrylic acid ester, methacrylic acid ester, vinyl pyrrolidone, vinyl ether and vinyl ester. Preferred anionic copolymers are acrylic acid-acrylamide copolymers and in particular polyacrylamide copolymers with monomers containing sulfonic acid groups. A particularly preferred anionic copolymer is contained in the commercial product Sepigel®305 from SEPPIC. The sodium acryloyldimethyltaurate copolymers sold under the name Simulgel®600 as a compound with isohexadecane and polysorbate-80 have also proven to be particularly effective according to the invention. Also preferred anionic homopolymers are uncrosslinked and crosslinked polyacrylic acids. Allyl ethers of pentaerythritol, sucrose and propylene can be preferred crosslinking agents. Such compounds are, for example, the commercial products Carbopol®. Particularly preferred anionic polymers are uncrosslinked and crosslinked copolymers with a high proportion of (meth) acrylic acid monomers and a small proportion of acrylic esters of C _10-30 fatty alcohols, which, for. B. contained in the commercial products Pemulen® or Carbopol® 1342.

Particularly preferred nonionic polymers are polyvinyl alcohol, polyvinyl pyrrolidones and vinyl pyrrolidone / vinyl ester copolymers, e.g. B. the commercial products Luviskol® (BASF).

In a further, particularly preferred embodiment of the invention, the active substance matrix or the active substance reservoir contain permeation enhancers which improve the transport of the active substances in and through the upper skin layers. Substances suitable as permeation enhancers are dimethyl sulfoxide, dodecyl sulfoxide, monomethylacetamide, dimethylacetamide, salicylic acid, urea, ethanol, polyvalent C _2-6 alcohols, in particular ethylene glycol, propylene glycol, glycerol and sorbitol, and also also compounds and compositions which act as nonionic emulsifiers are used, such as. B. Poly ethylene glycols, polypropylene glycols, polyethylene-polypropylene block copolymers, plant approximately 2 to 50 moles of ethylene oxide and / or 0 to 5 moles of propylene oxide to linear and branched fatty alcohols with 8 to 30 carbon atoms, fatty acids with 8 to 30 C atoms and on alkylphenols with 8 to 15 C atoms in the alkyl group, C ₁₂ -C ₃₀ fatty acid monoesters and diesters of adducts of 1 to 30 moles of ethylene oxide with polyols with 3 to 6 carbon atoms, in particular on glycerol, adducts of 5 to 60 moles of ethylene oxide on castor oil and hardened castor oil, polyol fatty acid (partial) ester of saturated C _8-30 fatty acids, e.g. B. Hydagen® HSP (Cognis) or Sovermol® types (Cognis), alkoxylated triglycerides, alkoxylated fatty acid alkyl esters, amine oxides, fatty acid alkanol amides, fatty acid N-alkylglucamides and fatty amines and their adducts of ethylene oxide and polyglycerol, sorbitan fatty acid esters and additive sorbitan esters of ethylene oxide and ethylene oxide with sorbitan fatty acid and sorbitan acid products of ethylene oxide on ethylene oxide such as the polysorbates, sugar fatty acid esters and methyl glucoside fatty acid esters and their addition products of ethylene oxide and polyglycerol, alkyl polygycosides according to the general formula RO- (Z) _x where R is alkyl, Z, sugar and x the number of sugar units, and are particularly preferred are those alkyl polyglycosides in which R consists essentially of C _8-10 alkyl groups or essentially of C _12-14 alkyl groups, or essentially of C _8-16 alkyl groups or essentially of C _12-16 alkyl groups or essentially consists of C _16-18 alkyl groups, and as a sugar building block Z bel Other mono- or oligosaccharides can be used, and values of 1.1 to 2.0 are preferred for x. Other preferred permeation enhancers are sterols, e.g. B. ergosterol, stigmasterol, sitosterol and mycosterols, phospholipids, especially glucose phospholipids, e.g. B. lecithins or phosphatidylcholines, polyglycerols and polyglycerol derivatives such as polyglycerol poly-12-hydroxystearate (commercial product Dehymuls® PGPH).

Further permeation enhancers preferred according to the invention are saturated and unsaturated C _12-30 fatty acids and C _12-30 fatty alcohols, which optionally carry hydroxyl groups and alkoxy groups, and the esters of mono- and polyhydric C _2-10 alcohols with saturated and unsaturated C _{10 -30} fatty acids, acetylated lanolin, C _10-30 fatty acid monoethanolamines, C _10-30 fatty acid diethanolamines, 1-menthol, camphor, higher hydrocarbons, in particular paraffin oils, castor oil, squalene, squalane, olive oil and pyrrolidone derivatives, especially pyrrolidone carboxylic acid. Ethylene glycol, propylene glycol, glycerol and sorbitol and their optionally ethoxylated mono- and diesters with saturated and unsaturated C _10-30 fatty acids and phospholipids are particularly preferred; Especially preferred are ethylene glycol, propylene glycol, glycerol, 1,3-butylene glycol, sorbitol, glycerol monooleate, glycerol dioleate and optionally ethoxylated sorbitan mono- and difatty acid esters and phospholipids. Many of the substances used as permeation enhancers according to the invention can be assigned an HLB value (HLB: hydrophilic-lipophilic balance). Lipophilic permeation enhancers have an HLB value of 6 or less, more hydrophilic permeation enhancers have an HLB value greater than 6. The selection of the preferred permeation enhancers depends on the active ingredients which are to be applied with the plasters according to the invention.

Furthermore, it can be preferred according to the invention, the active ingredient combination in the matrix or stabilize in the reservoir by adding at least one pH regulator. The  Optimal pH value of the active substance reservoir is determined primarily by the selection of the ascorbin acid derivatives determined. For the sodium derivatives which are particularly preferred according to the invention ascorbyl phosphate and magnesium ascorbyl phosphate, the optimal pH is 7 to 8.5. Suitable pH regulators are selected from physiologically acceptable acetates, Phosphates, carbonates, citrates, lactates and tartrates as well as triethanolamine. For setting A combination of the aforementioned regulating substances can be used to develop the optimal pH be preferred.

Further cosmetic additives which are particularly preferred according to the invention are selected from organic light protection filters, in particular benzophenone derivatives, cinnamic acid deri vaten and triazines, and inorganic light protection pigments, e.g. B. Titanium dioxide. Both organic light protection filters are liquid or crystalline at room temperature present substances which are able to absorb ultraviolet rays and which absorbed energy in the form of longer-wave radiation, e.g. B. heat to release again. A distinction is made between UVA filters and UVB filters. The organic light protection filter can be oil-soluble or water-soluble. According to the invention, particularly preferred oil-soluble UVB Filters are 3-benzylidene campers or 3-benzylidene norcampers and their derivatives, e.g. B. 3- (4-methylbenzylidene) camphor, 4-aminobenzoic acid derivatives, preferably 4- (dimethyl 2-ethylhexylamino) benzoate, 2-octyl 4- (dimethylamino) benzoate and 4- (Dimethylamino) benzoic acid amyl ester, ester of cinnamic acid, preferably 4-methoxy cinnamon 2-ethylhexyl acid, propyl 4-methoxycinnamate, isoamyl 4-methoxycinnamate or 2-cyano-3-phenylcinnamic acid 2-ethylhexyl ester (octocrylene), esters of salicylic acid, preferably 2-ethylhexyl salicylic acid, 4-isopropylbenzyl salicylic acid or sali cyl acid homomethyl ester, derivatives of benzophenone, preferably 2-hydroxy-4-meth oxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone or 2,2'-dihydroxy-4- methoxybenzophenone, ester of benzalmalonic acid, preferably 4-methoxybenzmalone di-2-ethylhexyl acid, triazine derivatives, such as. B. 2,4,6-Trianilino- (p-carbo-2'-ethyl-1'- hexyloxy) -1,3,5-triazine, octyl triazone or dioctyl butamido triazone (Uvasorb® HEB), Propane-1,3-diones such as e.g. B. 1- (4-tert-Butylphenyl) -3- (4'methoxyphenyl) propane-1,3-dione and ketotricyclo (5.2.1.0) decane derivatives.

Preferred water-soluble UVB filters are 2-phenylbenzimidazole-5-sulfonic acid and their Alkali, alkaline earth, ammonium, alkylammonium, alkanolammonium and glucammo nium salts, sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid  and their salts, sulfonic acid derivatives of 3-benzylidene camphor, such as B. 4- (2-oxo-3-bornylidenemethyl) benzenesulfonic acid and 2-methyl-5- (2-oxo-3-borny liden) sulfonic acid and its salts.

Preferred UV-A filters are, in particular, derivatives of benzoylmethane, such as, for example 1- (4'-tert-Butylphenyl) -3- (4'-methoxyphenyl) propane-1,3-dione, 4-tert-butyl-4'-methoxydi benzoylmethane (Parsol® 1789) or 1-phenyl-3- (4'-isopropylphenyl) propane-1,3-dione. The UVA and UVB filters can be used both individually and in mixtures. The The use of light protection filter mixtures is preferred according to the invention. Both Inorganic light protection pigments preferred according to the invention are finely dispersed metal oxides or salts, for example titanium dioxide, zinc oxide, iron oxide, Aluminum oxide, cerium oxide, zirconium oxide, silicates (talc), barium sulfate and zinc stearate. The Particles should have an average diameter of less than 100 nm, preferably have between 5 and 50 nm and in particular between 15 and 30 nm. You can ... a have a spherical shape, but it is also possible to use particles which has an ellipsoidal shape or otherwise deviates from the spherical shape Zen. The pigments can also be surface treated, i.e. H. hydrophilized or hydrophobized available. Typical examples are coated titanium dioxide, such as. B. Titanium dioxide T 805 (Degussa) or Eusolex® T2000 (Merck). They are used as hydrophobic coating agents all silicones and especially trialkoxyoctylsilanes or simethicones. In suns Protective agents are preferably used in the form of so-called micro or nanopigments. virtue Micronized zinc oxide is used.

Further cosmetic additives which are particularly preferred according to the invention are selected from plant extracts. Plant extracts are usually extracted by extracting the whole Plant, but in individual cases also exclusively from flowers and / or leaves and / or Seeds and / or other parts of plants. According to the invention, above all Extracts from the meristem, i.e. the divisible tissue of the plants, and special plants such as witch hazel, chamomile, marigold, pansy, peony, aloe Vera, horse chestnut, sage, willow bark, cinnamon tree (cinnamon tree), chrysanthemums, Oak bark, nettle, hops, burdock root, horsetail, hawthorn, linden flowers, Almonds, spruce needles, sandalwood, juniper, coconut, kiwi, guava, lime, mango, Apricot, wheat, melon, orange, grapefruit, avocado, rosmann, birch, beech sprouts, Mallow, cuckoo flower, yarrow, quendel, thyme, lemon balm, hake, marshmallow  (Althaea), mallow (Malva sylvestris), violet, black currant leaves, hoof preferred lettuce, quintuplets, ginseng, ginger root, sweet potato and green tea.

Algae extracts can also be used to advantage. The used according to the invention Algae extracts come from green algae, brown algae, red algae or blue-green algae (cyanobacts rien). The algae used for extraction can be of natural origin as well obtained through biotechnological processes and if necessary compared to natural ones Shape changed. The change in organisms can be done genetically, through breeding or by cultivation in media enriched with selected nutrients. Preferred algae extracts come from seaweed, blue-green algae, from the green algae Codium tomentosum and from the brown algae Fucus vesiculosus. A particularly preferred algae extract comes from blue-green algae of the species Spirulina, which is enriched in a magnesium Medium were cultured; this extract is a commercial product Spirulina Extract SPHM 3002 from the Institute for Grain Processing GmbH, Germany.

The extracts from spirulina, aloe vera, meristem, witch hazel, apri are particularly preferred kose, marigold, guava, sweet potato, lime, mango, kiwi, cucumber, green tea, mallow, Marshmallow and violet. The agents according to the invention can also be mixtures of several contained in particular from two different plant extracts. As an extractant for Production of the plant extracts mentioned can. a. Water, alcohols and their Mixtures are used. Among the alcohols are lower alcohols such as etha nol and isopropanol, but especially polyhydric alcohols such as ethylene glycol, propylene glycol and butylene glycol, both as the sole extractant and in Mix with water, preferred. The steam distillation falls under the invention they prefer extraction methods. According to the invention, the plant extracts can both be used in pure as well as in diluted form.

Further cosmetic additives preferred according to the invention are selected from clays and layered silicates, e.g. B. bentonite, flavonoids, vitamins and vitamin derivatives, in particular tocopherols and the derivatives of vitamin A, proteins, protein hydrolyzates and amino acids, gallic acid derivatives, especially propyl gallate, anti-aging agents, Inhibitors of matrix metal proteinase MMP-1, dimethyl isosorbide, cyclodextrins, mono-, Di- and oligosaccharides such as glucose, galactose, fructose, fructose, Lactose and deoxy sugars such as fucose or rhamnose, plant glycosides, ceramides and  Pseudoceramides, azelaic acid, antioxidants and preservatives, perfume oils and dyes for coloring the agent. All active and used according to the invention Excipients can optionally be in encapsulated form, e.g. B. in liposomes become.

In a preferred embodiment of the reservoir patch according to the invention, the Drug reservoir segments on the skin-facing side with a permeable Membrane covered. The membrane causes the controlled release of the active ingredients. A such a design of the patch allows the use of higher concentrations of active ingredient in the reservoir and thereby enables longer treatment times without skin irritation trigger. The membrane preferably consists of polypropylene, polycarbonate, polyethylene, Ethylene-vinyl acetate copolymer or polyvinyl pyrrolidone-containing material.

The following amounts for the active compound combinations according to the invention in % By weight always refer to the weight of the matrix mixture of adhesive, invented active ingredient combination according to the invention and further cosmetic additives according to the Example part described under point 1 evaporation of the solvent (matrix plaster) or on the weight of the adhesive-free active ingredient-containing reservoir (reservoir patch). The Active ingredient combinations according to the invention are in a total amount of 0.1 to 30 % By weight, preferably in amounts of 1.0 to 15% by weight, and particularly preferably in Amounts from 2.0 to 10% by weight are included. The skin lightening components (a) are in an amount of 0.05 to 5% by weight, preferably 0.1-2% by weight. The compo nente (b) is in an amount of 1.0 to 10% by weight, preferably 2.0 to 5.0% by weight contain. The amount of bisabolol is 0.1 to 5% by weight, preferably 1.0 to 2.0% by weight.

The adhesive layer preferably contains at least one medical adhesive selected from synthetic, natural and modified natural polymers. The synthetic adhesive polymers are selected from polyacrylates, polymethacrylates, acrylate-methacrylic copolymers, which may also contain functional comonomers, polyisobutylene, chlorobutyl rubber, phthalate resins, polyvinyl ethers, polyurethanes and silicone resins and from mixtures of these substances. The natural and modified natural adhesive polymers are selected from alkylated cellulose derivatives, which can be cationized or anionized, pectin, gelatin, karaya, rubber and mixtures of these substances. Particularly preferred adhesives are alkylated cellulose derivatives, e.g. As ethyl cellulose, polyisobutylene, esters of polyacrylic acid or polymethacrylic acid with optionally branched C _4-18 alkanols such as. B. butyl acrylate, ethylhexyl acrylate and stearyl acrylate, acrylate-methacrylate copolymers, phthalate resins, polyvinyl ether and (meth) acrylate copolymers with functional comonomers and mixtures of these substances. The (meth) acrylate copolymers with functional comonomers can contain as comonomers: monomers with a hydroxyl group such as e.g. B. 2-hydroxyethyl (meth) acrylate and 2-hydroxypropyl (meth) acrylate, monomers with a carboxyl group such as. B. maleic acid monoalkyl, especially butyl maleate, further maleic acid, maleic anhydride, fumaric acid and crotonic acid, monomers with an amide group such as. B. acrylamides, alkyl (meth) acrylamides, especially dimethylacrylamide and diethylacrylamide, alkylmethylol (meth) acrylamides, alkoxyalkyl (meth) acrylamides, especially ethoxymethyl acrylamide and butoxymethylacrylamide, furthermore diacetone acrylamide and vinylpyrrolidone, monomers with an amino group such as, for. B. dimethylaminoacrylate, also vinyl acetate, styrene, alpha-methyl styrene, acrylonitrile, ethylene, propylene and butadiene. In a particularly preferred embodiment, the polymers, in particular the (meth) acrylates, are partially crosslinked.

Examples of suitable commercial products for medical adhesive dispersions are among the Brand names GELVA® (Solutia Monsanto) and DURO-TAK® (National Starch and Chemical) is available.

Another preferred embodiment of the matrix patch according to the invention is designed analogously to the patch system disclosed in the publication WO 98/36740 A2. At least two matrix compositions are produced on the basis of polyacrylate adhesives, which differ from one another in the degree of crosslinking of the polyacrylate polymer. A low degree of cross-linking guarantees good adhesion of the polyacrylate adhesive to the skin. However, interactions between the cosmetic additives and slightly cross-linked polyacrylates lead to a deterioration in the adhesive properties. In particular, the cohesion of the adhesive is negatively influenced, which leads to the so-called cold flow of the adhesive. In the embodiment according to the invention with at least a two-layer matrix, the matrix with the lower degree of crosslinking is applied to the side facing the skin. One or more matrix layers with higher crosslinked polyacrylates are applied over this skin contact layer. The coating weight of the skin contact layer is preferably 10-30 g / m ² . With such a coating weight, the cold flow of the layer is negligible, while the degree of crosslinking results in excellent adhesion to the skin. In contrast, the more highly crosslinked, cold flow-stable matrix has an approximately three to five times higher coating weight of 50-200 g / m ² , preferably 60-120 g / m ² . The matrices are then sealed with a top layer.

The removable protective layer protects the adhesive and the drug reservoir. She will removed after using the patch. At the same time, the protective layer serves during production of the patch as a carrier on which adhesive and layers of active substance are applied. In In a preferred embodiment of the invention, the removable protective layer consists of a paper or a polymer film made of polyester, which with silicone compounds or fluoroorganic compounds are coated. Also preferred protective layer material lien are polystyrene and polyterephthalate films.

The covering layer of the plasters according to the invention can be designed such that they either occlusive, that is, impermeable to water vapor and other gases, or is breathable, i.e. gas permeable. Both types of cover layers can be made of plastic, Fibers, woven or non-woven materials.

The material of the cover layer of the plasters according to the invention is selected from polyethylene terephthalate, ethylene-vinyl acetate copolymers, polyethylene, polypropylene, polytetrafluor ethylene, polyurethane, polyacrylate or polyvinyl chloride.

If desired, the cover layer material can be coated with aluminum. gas casual cover layers can be made of per se impermeable materials Have pores and perforations to allow gas exchange.

The matrix plasters according to the invention are in a particularly preferred embodiment equipped with a gas-permeable cover layer. The reservoir according to the invention plasters are in a particularly preferred embodiment with a gas impermeable Surface layer.

The following examples are intended to explain the subject matter of the invention without it to be limited to this.  

Examples 1. Production of the matrix patch

The active ingredient combination according to the invention is used together with the permeation enhancer core and optionally other cosmetic ingredients in an organic solution medium, selected from hexane, heptane, ethyl acetate, methanol, ethanol or chloroform, dis pergiert, gradually dispersing the adhesive in an organic solution medium is added. For defoaming, the matrix dispersion is left for at least rest at room temperature for one hour. After the foam has receded, the dispersion in a uniform layer thickness of 10 to 200 microns on the peelable Protective layer applied. The solvent is left in for at least one hour Evaporate at room temperature. If necessary, the paper or film is left for about 10 minutes dried at a temperature above room temperature up to a maximum of 80 ° C.

After the solvent has completely evaporated, the matrix coating obtained in this way is sealed with a cover layer by adhesion or melting. The sealed laminate is aged at 37 ° C for 12 to 24 hours and then cut into suitable sized patches. The coating weights range from 30 to 250 g / m ² , preferably from 50 to 200 g / m ² . The patch sizes range from 0.1 to 500 cm ² , preferably from 0.5 to 100 cm ² and particularly preferably from 1 to 30 cm ² .

2. Production of the reservoir patch

The medical adhesive is dispersed in a suitable solvent and then ß in a uniform layer thickness of 10 to 200 µm on the removable protection layer applied. The evaporation of the solvent takes place as in the production of the Matrix patch. After the solvent has completely evaporated, the adhesive layer by adhesion or melting, if necessary first with the permeable membrane sealed. The top layer is then applied.

The active substance combination according to the invention is used to produce the active substance reservoir together with the permeation enhancers, the thickeners and, if appropriate other cosmetic ingredients dispersed. The active ingredient dispersion is then  Filled in segments between the cover layer and the adhesive membrane layer. To the Finally, the layers around the drug segments are heat sealed.

3. Examples

3.1 Skin-lightening matrix plasters

3.2 Skin-lightening reservoir plasters

attachment

List of trademarks of the raw materials used

Claims (15)

1. Cosmetic plaster for skin lightening, which consists of a cover layer, an active substance reservoir, an adhesive layer and a removable protective layer and is characterized in that an active substance combination consists of

• a) at least one substance selected from the derivatives of ascorbic acid, kojic acid, hydroquinone, arbutin, mulberry extract and licorice extract,
• b) at least one substance selected from panthenol and the derivatives of 2-furanone, and
• c) Bisabolol

is included. 2. Cosmetic plaster according to claim 1, characterized in that the active ingredient reservoir contains other cosmetic additives. 3. Cosmetic plaster according to claim 1, characterized in that the component (a) is selected from kojic acid and the derivatives of ascorbic acid. 4. Cosmetic plaster according to claim 1, characterized in that the component (a) is selected from sodium ascorbyl phosphate, magnesium ascorbyl phosphate and Mixtures of these. 5. Cosmetic plaster according to claim 1, characterized in that the derivatives of 2-furanones are selected from dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone (Panto lactone), 4-hydroxymethyl-γ-butyrolactone, 3,3-dimethyl-2-hydroxy-γ-butyrolactone and 2,5-dihydro-5-methoxy-2-furanone. 6. Cosmetic plaster according to one of claims 1 to 5, characterized in that additionally contains at least one polymer. 7. Cosmetic plaster according to one of claims 1 to 6, characterized in that additionally at least one substance suitable as a permeation enhancer is contained.   8. Cosmetic plaster according to one of claims 1 to 7, characterized in that additionally at least one substance selected from organic light protection filters and inorganic light protection pigments is included. 9. Cosmetic plaster according to one of claims 1 to 8, characterized in that additionally at least one substance selected from plant extracts and algae extracts, is included. 10. Cosmetic plaster according to claim 1 or 2, characterized in that the effect fabric reservoir is mixed with the adhesive layer and spread over the entire paved area extends. 11. Cosmetic plaster according to claim 1 or 2, characterized in that the Active ingredient reservoir contains no adhesive adhesive and only limited segments on the Takes up paving area. 12. Cosmetic plaster according to claim 11, characterized in that the active ingredient reservoir segments on the side facing the skin with a permeable, porous Membrane are covered. 13. Cosmetic plaster according to claim 10, characterized in that the active ingredient combination (a) + (b) + (c) in a total amount of 0.1 to 30 wt .-%, based on the total weight of the active ingredient and additive-containing adhesive layer is included. 14. Cosmetic plaster according to claim 11, characterized in that the active ingredient combination (a) + (b) + (c) in a total amount of 0.1 to 30 wt .-%, based on the weight of the adhesive-free drug reservoir is included. 15. Cosmetic plaster according to claim 1, characterized in that the cover layer is gas permeable.