WO2001064167A1

WO2001064167A1 - Cosmetic and pharmaceutical preparations for treating cellulite

Info

Publication number: WO2001064167A1
Application number: PCT/EP2001/002071
Authority: WO
Inventors: Ulrich Issberner; Marcus Claas; Vera Maienschein; Silke Nieveler; Thomas Förster; Werner Köhl
Original assignee: Henkel Kommanditgesellschaft Auf Aktien
Priority date: 2000-02-28
Filing date: 2001-02-23
Publication date: 2001-09-07
Also published as: DE10009423A1; AU2001235491A1; EP1261310A1

Abstract

The invention relates to cosmetic and pharmaceutical preparations containing a substance which stimulates and/or depolarises C nerve fibres, a phosphodiesterase inhibitor and a substance with an anti-oestrogen effect. The inventive preparations are particularly suitable for treating cellulite.

Description

COSMETIC AND PHARMACEUTICAL PREPARATIONS FOR TREATING CELLULITE

The invention relates to cosmetic and pharmaceutical preparations containing a substance that stimulates and / or depolarizes C-nerve fibers, a phosphodiesterase inhibitor and a substance with an anti-estrogenic effect. The preparations are particularly suitable for treating cellulite.

Cellulite (synonyms: panniculosis, lipodystrophy, status protrusis cutis, orange peel) is a local accumulation of fat and water in body tissue. It is a predominantly aesthetic problem associated with pitting and deepening of the skin and nodulation of the subcutaneous fatty tissue, particularly on the thighs and buttocks. In advanced stages of cellulite, pain in the area of the nodules can also occur. A clear distinction from cellulite is cellulitis (panniculitis), which is an inflammation of the subcutaneous adipose tissue and thus a serious and life-threatening illness in some cases.

The causes of cellulite are not exactly known. However, it is usually considered a cosmetic problem. However, there are also voices in the specialist literature that regard cellulite as a pathological condition that requires therapy. This approach is based on the one hand on pain conditions, which have their origin especially in the area of the strongly greased subcutaneous tissue. On the other hand, the psychological stress associated with cellulite can manifest itself in psychosomatic disorders that require treatment. The conventional treatment methods for cellulite try to promote blood circulation and have a positive influence on the connective tissue structure, for example through

- massage

- lymphatic drainage

- Diet and / or exercise, although the condition may even worsen

- magnetic fields

- Liposuction (liposuction)

- Enzyme therapy, for example with hyaluronidase or

- Taking medication to promote lipolysis

The best known and most widespread of the methods of stimulating lipolysis is to inhibit the enzyme phosphodiesterase in order to prevent or at least slow down the degradation of the cyclic AMP. The phosphodiesterase destroys the cyclic AMP by converting it to 5 ^' -AMP, which is no longer able to activate lipolysis. It is therefore important to inhibit the action of the phosphodiesterase in such a way that a high concentration of cyclic AMP is achieved in the region of the adipocytes with the aim of stimulating lipolysis. Among the various phosphodiesterase inhibitors that have been recommended, for example, as slimming agents, are the xanthine bases, especially caffeine.

Plant extracts, growth factors, inositol phosphate, alpha-hydroxycarboxylic acids and vitamin C were also recommended for the treatment of cellulite.

FR 2740681 describes cosmetic compositions for the treatment of cellulite which contain caffeine and an extract from the bark or leaves of plants of the genus Viburnum. As part of this extract, amentoflavone is described, one consisting of two apigenin units Biflavonoid. According to the teaching of this document, amentoflavone is a characteristic ingredient of viburnum and serves to standardize the dosage of the viburnum extract in the compositions according to the invention. The document does not give the person skilled in the art any indication that the amentoflavone could be the cause or jointly responsible for the anti-cellulite effect of the compositions.

FR 2609395 describes xanthine-containing pharmaceutical or cosmetic compositions with a local slimming effect which is attributed to their intracellular phosphodiesterase-inhibiting action. The compositions may contain glycosides such as bioflavonoids as additional ingredients. It is not disclosed which substances or groups of substances are to be understood under the term bioflavonoids, which is known to be contradictory in the specialist world. This does not enable the person skilled in the art to prepare a composition according to the teaching of the writing containing a bioflavonoid which has a locally slimming effect. The document also gives no indication that the bioflavonoids could contribute to the slimming properties of the compositions according to the invention.

From JP 08099813 substances obtained from plant material are known which, in addition to other substances, can contain capsaicin, flavonoids and / or isoflavones. The substances described there serve to regulate plant growth in agriculture, other applications are not mentioned.

From JP 11060460 capsaicin and vanillyl nonylamide are known as constituents of skin cosmetic preparations which bring about a feeling of warmth on the skin produced by exothermic substances. However, the document gives no evidence that these preparations could be suitable for the treatment of cellulite. The substances and methods for treating cellulite known from the prior art are unsatisfactory, particularly as regards the extent and speed of the treatment effect. There has also been a lack of means to improve the treatment effect on cellulite symptoms, which occurs in particular through the breakdown of fat cells and the remodeling of connective tissue and which is relatively slow due to physiological reasons, with an independent, physiological and / or psychological effect combine so that the user already gets a subjective impression of an effect immediately during or after the application of the agent. In practice, it has been shown that the users of an anti-cellulite agent stop using the agent very soon and are disappointed with the product used if they do not at least have the subjective impression that the agent has an effect. This means that the desired effect of the agent cannot be achieved, in particular, if there is only an objective improvement in cellulite symptoms due to the active ingredients contained in the agent.

The object of the invention was to remedy the shortcomings of the prior art and to provide an improved agent for treating cellulite. Another object of the invention was to provide an agent which combines an improved action against cellulite with an effect which is immediately noticeable when the agent is used and which gives the user the impression of an onset of action.

The object of the invention is achieved by cosmetic or pharmaceutical preparations which, in a physiologically compatible carrier, contain at least one substance which stimulates and / or depolarizes C-nerve fibers, at least one phosphodiesterase inhibitor and at least one substance with an anti-estrogenic effect.

The C-nerve fibers, also called polymodal C-nerve fibers, play an important role in the human organism for the sensory functions of the Body, especially the skin. They are primarily involved in the perception of, for example, heat, cold and itching as well as the sensation of pain (e.g. heat pain, cold pain, stinging pain, burning pain). The polymodal C-nerve fibers have a special position as a sub-group of the C-nerve fibers because they can react to several different stimuli and can also intervene in the stimulus process through the release of mediators. Different receptors such as capsaicin, bradykinin and 5-hydroxytryptamine receptors are located on the surface of the C-nerve fibers, as well as ion channels such as calcium and sodium channels, via which the C-nerve fibers can be stimulated and / or depolarized. This stimulation and / or depolarization triggers a sensory stimulus which manifests itself, for example, as a burning, tingling, sensation of warmth, cold or pain. For the purposes of the present invention, it is preferred to trigger a tingling sensation, a slight burning sensation or a feeling of warmth or coldness by stimulating and / or depolarizing the C-nerve fibers of the skin, in particular by stimulating the capsaicin receptors of these nerve fibers.

In the context of the present invention, substances influencing C nerve fibers are to be understood, for example:

- capsaicin

- Red pepper or cayenne pepper extracts

- Vanillyl nonylamide (nonivamide)

- Acid amides of 4-hydroxy-3-methoxy-benzylamine with carboxylic acids R-COOH, the carboxylic acids being selected from the group consisting of straight-chain or branched alkyl carboxylic acids having 1 to 22 carbon atoms

- Ginger extracts

- In addition to the substances listed above in JP 11060460, heat-causing substances and glycosides of the aforementioned substances, insofar as they are capable of forming glycosides. In these glycosides are those mentioned above Substances, insofar as they contain one or more hydroxyl groups, are glycosidically linked to a sugar via at least one hydroxyl group. Particularly suitable sugars are D-glucose, D-galactose, D-glucuronic acid, D-galacturonic acid, D-xylose, D-apiose, L-rhamnose, L-arabinose and D-maltose. Other suitable substances are described in PD Wall and R. Melzack (Eds.), Textbook of Pain, Churchill Livingstone Verlag, Edinburgh 1994, pp. 13 to 37 and 58 to 72.

Preferred substances influencing C-nerve fibers are capsaicin, N-vanillyl nonanamide, their glycosides and mixtures thereof.

In addition to triggering a sensory stimulus which gives the user of the preparation according to the invention the sensation of an onset of action, the substances influencing the C-nerve fibers sometimes have further desired effects. They promote the blood flow to the treated tissue and thus promote the penetration of the ingredients of the preparation into the skin. Furthermore, the removal of the degradation products which arise in the course of the lipolysis which is brought about by the use of the preparation can be promoted. In addition, the cellulite pain that occurs in severe cases can be reduced. This is the case, for example, when nonivamide is used as the substance influencing the C nerve fibers.

Suitable phosphodiesterase inhibitors in the preparations according to the invention are, for example, inhibitors as described in RM Di Salvo, Controlling the Appearance of Cellulite, Cosmetics and Toilet's Magazine HO, pp. 50-59 (1995) or in L. Stryer, Biochemistry, Spektrum Akademischer Verlag GmbH, Heidelberg 1991, p. 482.

Phosphodiesterase inhibitors preferred according to the invention are xanthine or methylxanthines, whereby a methylxanthine is a xanthine derivative in which one or more hydrogen atoms of the xanthine by methyl groups are replaced. Theophylline, theobromine and caffeine are preferred as methylxanthines, and caffeine is particularly preferred.

As a further component, the preparations according to the invention contain one or more substances with an anti-estrogenic effect. Anti-estrogenic substances are substances that act in the organism as antagonists of estrogenic substances. This can happen, for example, in that an anti-estrogenic substance binds to estrogen receptors without, however, triggering an estrogenic effect. The selection of anti-estrogenic substances is possible for the person skilled in the art by simple routine experiments and can be carried out, for example, by examining tissue and cell cultures that are sensitive to estrogen. Such experiments are described, for example, in Estrogen agonistic / antagonistic effects of miproxifene phosphate (TAT-59), Cancer Chemother. Pharmacol. 45 (2000), pp. 133-141 and J. Shibata et al., Hormonally active agents in food: Symposium Deutsche Forschungsgemeinschaft, Verlag Wiley-VCH GmbH, Weinheim 1998, chap. 7, p. 4, 91, 93.

Examples of anti-estrogenic substances in the sense of the invention are tamoxifen, aminoglutethimide, clomiphene, testosterone, androsterone, isoflavones and isoflavone glycosides. In the literature, isoflavones are attributed to estrogenic effects, which is why they are also called phytoestrogens, but these substances are also known to have anti-estrogenic effects under certain conditions and in certain concentrations (hormonally active agents in food: symposium / German Research Foundation, Verlag Wiley-VCH, Weinheim 1998, pp. 25, 93). In the preparations according to the invention they are preferably used in a concentration in which they exert an anti-estrogenic effect.

Preferred anti-estrogenic substances are isoflavones, isoflavone glycosides, tamoxifen and mixtures thereof. For the purposes of the present invention, isoflavones are understood to mean substances which are hydrogenation, oxidation or substitution products of 3-phenyl-4H-1-benzopyran, where hydrogenation can be present in the 2,3-position of the carbon skeleton, oxidation under Formation of a carbonyl group may be in the 4-position, and substitution is to be understood as the replacement of one or more hydrogen atoms by hydroxyl or methoxy groups. The isoflavones according to the invention include, for example, daidzein, genistein, prunetin, biochanin, Orobol, Santal, pratensein, irigenin, glycitein, biochanin A and formononetin. Daidzein, genistein, glycitein and formononetin are preferred as isoflavones.

In the isoflavone glycosides according to the invention, the isoflavones are glycosidically linked to at least one sugar via at least one hydroxyl group. Suitable sugars are mono- or oligosaccharides, in particular D-glucose, D-galactose, D-glucuronic acid, D-galacturonic acid, D-xylose, D-apiose, L-rhamnose, L-arabinose and rutinose. Preferred examples of the isoflavone glycosides according to the invention are daidzin and genistin.

It is further preferred according to the invention if the isoflavones and / or their glycosides are contained in the preparations as constituents of a mixture of substances obtained from a plant, in particular a plant extract. Such vegetable substance mixtures can be obtained in a manner familiar to the person skilled in the art, for example by pressing or extracting them from plants such as soybean, red clover or chickpeas. Isoflavones or isoflavone glycosides in the form of extracts obtained from soy are particularly preferably used in the preparations according to the invention, such as those known under the product name Soy Protein Isolate SPI (Protein Technology International, St. Louis) or Soy Phytochemicals Concentrate SPC (Archer Daniels Midland, Decatur) are commercially available.

Water, alcohols and mixtures thereof can be used as extractants for the production of the plant extracts mentioned. Among the alcohols are lower alcohols such as especially ethanol and isopropanol, and polyvalent

Alcohols such as ethylene glycol, propylene glycol and butylene glycol, both as the sole extracting agent and in a mixture with water, are preferred. The

Steam distillation is one of the preferred in the present invention

Extraction process.

Alcoholic extraction is preferred according to the invention.

Furthermore, it may be preferred to use mixtures of several, in particular two, different plant extracts in the agents according to the invention.

It was surprisingly found that the triple combinations of active substances according to the invention show an unexpectedly high activity in the treatment of cellulite, as can only be explained by a synergistic effect of the components.

The active ingredients are used in the cosmetic or pharmaceutical preparations according to the invention in a concentration which is at most equal to the toxicologically permissible use concentration.

According to the invention, the cosmetic or pharmaceutical preparations contain

(a) 0.0001 to 3% by weight of one or more substances which stimulate and / or depolarize the C-nerve fibers

(b) 1 to 15% by weight of one or more phosphodiesterase inhibitors

(c) 0.1 to 20% by weight of one or more substances with an anti-estrogenic effect, in each case based on the total weight of the preparation.

The cosmetic preparations preferably contain

(d) 0.005 to 0.5% by weight of one or more substances that stimulate and / or depolarize the C-nerve fibers

(e) 5 to 10% by weight of one or more phosphodiesterase inhibitors (f) 1 to 10% by weight of one or more substances with an anti-estrogenic

Effect, based on the total weight of the preparation.

The physiologically acceptable carrier of the cosmetic or pharmaceutical preparations comprises one or more auxiliaries, as are usually used in such preparations, such as. B. fats, oils, waxes, silicones, emulsifiers, alcohols, polyols, thickeners, moisturizing and / or moisturizing substances, polymers, surfactants, plasticizers, foam retardants, alkalizing or acidifying agents, softeners, adsorbents, light stabilizers, electrolytes, sequestering agents, organic solvents , Preservatives, bactericides, antioxidants, vitamins, fragrances, flavors, sweeteners, colors and pigments.

The cosmetic preparations according to the invention are preferably suitable for the cosmetic treatment of cellulite and local excess fat, but also for so-called "slimming products" or skin-tightening products for legs, cleavage, neck or the face area.

When applied topically, the cosmetic and pharmaceutical preparations according to the invention are advantageously in the form of a liquid or solid oil-in-water emulsion, water-in-oil emulsion, multiple emulsion, microemulsion, PIT emulsion or Pickering emulsion, a hydrogel, an alcoholic gel, a lipogel, a single or multi-phase solution, a foam, an ointment, a plaster, a suspension, a powder or a mixture with at least one polymer suitable as a medical adhesive. The skin treatment agents according to the invention can also be administered in anhydrous form, such as, for example, an oil or a balm. The carrier can be a vegetable or animal oil, a mineral oil, a synthetic oil or a mixture of such oils. In a particular embodiment of the agents according to the invention, the agents are in the form of a microemulsion. In the context of the invention, microemulsions are understood to mean not only the thermodynamically stable microemulsions but also the so-called “PIT” emulsions. These emulsions are systems with the 3 components water, oil and emulsifier, which are present as an oil-in-water emulsion at room temperature. When these systems are warmed up, microemulsions form in a certain temperature range (referred to as phase inversion temperature or “PIT”), which convert to water-in-oil (W / 0) emulsions when heated further. Upon subsequent cooling, O / W emulsions are again formed, but these are also present at room temperature as microemulsions or as very fine-particle emulsions with an average particle diameter below 400 nm and in particular from about 100-300 nm. According to the invention, those micro- or "PIT" emulsions can be preferred which have an average particle diameter of approximately 200 nm. Details regarding these "PIT emulsions" e.g. B. the publication Angew. Chem. 97, 655-669 (1985).

The effect of the cosmetic and pharmaceutical preparations according to the invention can be further optimized by the suitable choice of the fatty substances. Suitable fat substances are for example:

vegetable oils, such as sunflower oil, olive oil, soybean oil, rapeseed oil, almond oil, jojoba oil, orange oil, wheat germ oil, peach seed oil and the liquid components of coconut oil,

- liquid paraffin oils, isoparaffin oils and synthetic hydrocarbons, e.g. B. 1, 3-di- (2-ethyl-hexyl) cyclohexane (Cetiol ^® S) or polydecene,

- Di-n-alkyl ethers with a total of 12 to 36, in particular 12 to 24 carbon atoms, for. As di-n-octyl ether (Cetiol ^® OE), di-n-n-hexyl-n-octyl ether and n-octyl-n-decyl ether.

- fatty acids, particularly linear and / or branched, saturated and / or unsaturated C _8- 3o fatty acids. Cιo- ₂₂ fatty acids are preferred. Examples are the isostearic acids and isopalmitic acids such as the fatty acids sold under the trade name Edenor ^® . Other typical examples of such Fatty acids are caprylic acid, 2-ethylhexanoic, capric acid, lauric acid, isotridecanoic, myristic acid, palmitic acid, stearic acid, isostearic acid, oleic acid, elaidic, Petroselin acid, linoleic acid, linolenic acid, eleostearic acid, arachidonic acid, Gadoleinsäure, behenic acid and erucic acid and technical mixtures. The fatty acid cuts that are obtainable from coconut oil or palm oil are usually particularly preferred; the use of stearic acid is particularly preferred.

Fatty alcohols, especially saturated, mono- or polyunsaturated, branched or unbranched fatty alcohols with 6 - 30, preferably 10 - 22 and very particularly preferably 12 - 22 carbon atoms. For the purposes of the invention, z. B. decanol, octanol, octenol, dodecenol, decenol, octadienol, dodecadienol, decadienol, oleyl alcohol, eruca alcohol, ricinol alcohol, stearyl alcohol, isostearyl alcohol, cetyl alcohol, lauryl alcohol, myristyl alcohol, arachidyl alcohol, linoleic alcohol, capryl alcohol, capryl alcohol as well as their Guerbet alcohols, e.g. B. 2-ethylhexanol, this list should have exemplary and non-limiting character.

Esteröle, that is, esters of C ₆ - ₃ o-fatty acids with C _2-3 o-fatty alcohols. The monoesters of fatty acids with alcohols having 2 to 24 carbon atoms are preferred. The above-mentioned substances can be used as alcohol and acid components of the ester oils. According to the invention particularly preferably isopropyl myristate, isononanoic acid C-ι -i ₆ ₈ -alkyl esters, 2-ethylhexyl palmitate, stearic acid-2-ethylhexyl ester, cetyl oleate, glycerol tricaprylate / caprylate Kokosfettalkoholcaprinat, n-butyl stearate, oleyl erucate, isopropyl palmitate, oleyl oleate, hexyl laurate , Di-n-butyl adipate, myristyl myristate, cetearyl isononanoate and oleic acid decyl ester.

Hydroxycarboxylic acid alkyl esters, wherein the Vollester of glycolic acid, lactic acid, malic acid, tartaric acid or citric acid are preferred, but also esters of beta-hydroxypropionic acid, tartronic acid, D-gluconic acid, saccharic acid, mucic acid or glucuronic acid are suitable and particularly preferred are the esters of Cι ₂ - Cι ₅ fatty alcohols, for. B. are the commercial products Cosmacol ^® from EniChem, Augusta Industriale, Dicarboxylic acid esters such as di-n-butyl adipate, di- (2-ethylhexyl) adipate, di- (2-ethylhexyl) succinate and di-isotridecyl acelate as well as diol esters such as ethylene glycol dioleate, ethylene glycol di-isotridecanoate, propylene glycol di (2-ethyl hexanoate), propylene glycol -di-isostearate, propylene glycol-di-pelargonate, butanediol-di-isostearate, neopentyl glycol dicaprylate, symmetrical, asymmetrical or cyclic esters of carbonic acid with fatty alcohols, e.g. B. glycerol carbonate or dicaprylyl carbonate (Cetiol ^® CC),

Mono, - di- and trifatty acid esters of saturated and / or unsaturated linear and / or branched fatty acids with glycerol, e.g. B. Monomuls ^® 90-018, Monomuls ^® 90-L12 or Cutina ^® MD,

Waxes, in particular insect waxes such as beeswax and bumblebee wax, plant waxes such as candelilla wax and carnauba wax, fruit waxes, ozone kerit, micro waxes, ceresin, paraffin, triglycerides saturated and optionally hydroxylated Ci ₆ - ₃ o-fatty acids, such as. B. hardened triglyceride fats (hydrogenated palm oil, hydrogenated coconut oil, hydrogenated castor oil), glyceryl tribehenate or glyceryl tri-12-hydroxystearate, synthetic full esters of fatty acids and glycols (e.g. Syncrowachs ^® ) or polyols with 2 - 6 C atoms.

- Silicone compounds selected from decamethylcyclopentasiloxane, dodecamethylcyclohexasiloxane and silicone polymers, which can, if desired, be cross-linked, e.g. B. polydialkylsiloxanes, polyalkylarylsiloxanes, ethoxylated polydialkylsiloxanes, preferably the substances with the INCI name Dimethicone Copolyol, and polydialkylsiloxanes containing amine and / or hydroxy groups.

The amount of fatty substances used is 0.1-50% by weight, preferably 0.1-20% by weight and particularly preferably 0.1-15% by weight, in each case based on the total composition.

The skin treatment compositions according to the invention can contain one or more surface-active substances as emulsifiers or dispersants. Emulsifiers cause the formation of water or oil-stable adsorption layers that protect the dispersed droplets against coalescence and thus stabilize the emulsion. Like surfactants, emulsifiers are therefore made up of a hydrophobic and a hydrophilic part of the molecule. Hydrophilic emulsifiers preferably form O / W emulsions and hydrophobic emulsifiers preferably form W / O emulsions. W / O emulsions which are stabilized without hydrophilic emulsifiers are disclosed in the published documents DE 19816665 A1 and DE 19801593 A1. An emulsion is to be understood as a droplet-like distribution (dispersion) of a liquid in another liquid with the use of energy to create stabilizing phase interfaces by means of surfactants. The selection of these emulsifying surfactants or emulsifiers is based on the substances to be dispersed and the particular external phase as well as the fine particle size of the emulsion.

Emulsifiers which can be used according to the invention are, for example

Addition products of 4 to 30 mol of ethylene oxide and / or 0 to 5 mol of propylene oxide with linear C ₈ -C ₂₂ fatty alcohols, with C ₂ -C ₂₂ fatty acids and with C ₈ -C ₅ alkylphenols,

- C ₂ -C ₂₂ fatty acid monoesters and diesters of adducts of 1 to 30 moles of ethylene oxide with C ₃ -C ₆ polyols, in particular with glycerol,

- Ethylene oxide and polyglycine adducts with methyl glucoside fatty acid esters, fatty acid alkanolamides and fatty acid glucamides,

C ₈ -C ₂₂ alkyl mono- and oligoglycosides and their ethoxylated analogs, degrees of oligomation of 1.1 to 5, in particular 1.2 to 2.0, and glucose as the sugar component being preferred,

- Mixtures of alkyl (oligo) glucosides and fatty alcohols, e.g. B. the commercially available product Montanov ^® 68,

Adducts of 5 to 60 moles of ethylene oxide with castor oil and hardened castor oil, Partial esters of polyols with 3-6 carbon atoms with saturated C ₈ -C ₂₂ fatty acids,

- Non-estrogenic sterols (sterols). Sterols are understood to be a group of steroids which carry a hydroxyl group on the C atom 3 of the steroid structure and are isolated both from animal tissue (zoosterols) and from vegetable fats (phytosterols). Examples of zoosterols are cholesterol and lanosterol. Examples of suitable phytosterols are beta-sitosterol, stigmasterol, campesterol and ergosterol. Sterols, the so-called mycosterols, are also isolated from fungi and yeasts.

- Phospholipids, especially the glucose phospholipids, which, for. B. as lecithins or phosphatidylcholines from z. B. egg yolk or plant seeds (e.g. soybeans) are obtained,

Fatty acid esters of sugars and sugar alcohols such as sorbitol,

- polyglycerols and polyglycerol, preferably Polyglyceryl-2-dipolyhydroxy- stearate (commercial product Dehymuls ^® PGPH) and polyglyceryl-3 diisostearate (Lameform ^® TGI commercial product)

- Linear and branched C ₈ -C ₃₀ fatty acids and their Na, K, ammonium, Ca, Mg and Zn salts.

The cosmetic and pharmaceutical preparations according to the invention preferably contain the emulsifiers in amounts of 0.1 to 25% by weight, in particular 0.5-15% by weight, based on the total composition.

The skin treatment agents according to the invention contain organic or mineral or modified mineral light protection filters. The light protection filters are substances which are liquid or crystalline at room temperature and are able to absorb ultraviolet rays and absorb the energy in the form of longer-wave radiation, e.g. B. to release heat again. A distinction is made between UVA filters and UVB filters. The UVA and UVB filters can be used both individually and in mixtures. The use of filter mixtures is preferred according to the invention. The organic UV filters used according to the invention are selected from the derivatives of dibenzoylmethane, cinnamic acid esters, diphenylacrylic acid esters, benzophenone, camphor, p-aminobenzoic acid esters, o-aminobenzoic acid esters, salicylic acid esters, benzimidazoles, 1, 3,5-triazines, monomeric and oligomeric 4,4- Diaryl butadiene carboxylic acid esters and carboxamides,

Ketotricyclo (5.2.1.0) decane, benzalmalonic acid esters and any mixtures of the components mentioned. The organic UV filters can be oil-soluble or water-soluble. According to the invention particularly preferred oil-soluble UV filters are 1- (4-tert-butylphenyl) -3- (4'methoxyphenyl) propane-1, 3-dione (Parsol ^® 1789), 1-phenyl-3- (4'-isopropylphenyl ) -propane-1, 3-dione, 3- (4 ^' -methylbenzylidene) -D, L-camphor, 4- (dimethylamino) -benzoic acid-2-ethylhexyl ester, 4- (dimethylamino) benzoic acid-2-octyl ester, 4- (Dimethylamino) benzoic acid amyl ester, 4-methoxycinnamic acid, 2-ethylhexyl ester, 4-methoxycinnamic acid propyl ester, 4-methoxycinnamic acid, isopentyl ester, 2-cyano-3,3-phenylcinnamic acid, 2-ethylhexyl ester (octocrylene), salicylic acid, 2-ethylhexyl ester -isopropylbenzyl ester, salicylic acid homomethyl ester (3,3,5-trimethylcyclohexyl salicylate), 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone, 4- Di-2-ethylhexyl methoxybenzmalonate, 2,4,6-trianilino- (p-carbo-2'-ethyl-1'-hexyloxy) -1, 3,5-triazine (octyl triazone) and dioctyl butamido triazone (Uvasorb ^® HEB) as well as any mixtures of components mentioned.

Preferred water-soluble UV filters are 2-phenylbenzimidazole-5-sulfonic acid and its alkali, alkaline earth, ammonium, alkylammonium, alkanolammonium and glucammonium 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-bornylidene methyl) benzenesulfonic acid and 2-methyl-5- (2-oxo-3-bornylidene) sulfonic acid and their salts.

The inorganic light protection pigments preferred according to the invention are finely dispersed metal oxides and metal 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 between 5 and 50 nm and in particular between 15 and 30 nm. They can have a spherical shape, but it is also possible to use particles which have an ellipsoidal shape or a shape which differs from the spherical shape in some other way. The pigments can also be surface-treated, ie hydrophilized or hydrophobicized. Typical examples are coated titanium dioxide, such as. B. Titanium dioxide T 805 (Degussa) or Eusolex ^® T2000 (Merck). Silicones, and in particular trialkoxyoctylsilanes or simethicones, are particularly suitable as hydrophobic coating agents. So-called micro- or nanopigments are preferably used in sunscreens. Micronized zinc oxide is preferably used.

Furthermore, the skin treatment agents according to the invention

Contain protein hydrolyzates or their derivatives. According to the invention, both vegetable and animal protein hydrolyzates can be used. Animal protein hydrolyzates are e.g. B. elastin, collagen, keratin, silk and milk protein protein hydrolyzates, which may also be in the form of salts. Vegetable protein hydrolyzates, e.g. B. soy, wheat, almond, pea, potato and rice protein hydrolyzates. Corresponding commercial products are e.g. B. DiaMin ^® (Diamalt), Gluadin ^® (Cognis), Lexein ^® (Inolex) and Crotein ^® (Croda).

Although the use of the additional protein hydrolyzates as such is preferred, amino acid mixtures or individual amino acids, such as arginine, lysine, histidine or pyrroglutamic acid, which have been obtained in some other way can also be used instead of them. It is also possible to use derivatives of protein hydrolyzates, e.g. B. in the form of their fatty acid condensation products. Corresponding commercial products are e.g. B. Lamepon ^® (Cognis), Gluadin ^® (Cognis), Lexein ^® (Inolex), Crolastin ^® or Crotein ^® (Croda).

In the cosmetic and pharmaceutical preparations according to the invention, the additional protein hydrolyzates and their derivatives are in amounts of 0.01-10 % By weight based on the total composition. Amounts of 0.1 to 5% by weight, in particular 0.1 to 3% by weight, are particularly preferred.

The skin treatment compositions according to the invention can furthermore contain mono-, oligo- or polysaccharides or their derivatives.

Suitable monosaccharides according to the invention are e.g. B. glucose, fructose, galactose, arabinose, ribose, xylose, lyxose, allose, old rose, mannose, gulose, idose and talose, the deoxy sugar fucose and rhamnose and amino sugar such as. B. glucosamine or galactosamine. Glucose, fructose, galactose, arabinose and fucose are preferred; Glucose is particularly preferred.

Suitable oligosaccharides according to the invention are composed of two to ten monosaccharide units, for. B. sucrose, lactose or trehalose. A particularly preferred oligosaccharide is sucrose. The use of honey, which predominantly contains glucose and sucrose, is also particularly preferred.

Polysaccharides suitable according to the invention are composed of more than ten monosaccharide units. Preferred polysaccharides are the starches made up of α-D-glucose units and starch degradation products such as amylose, amylopectin and dextrins. Chemically and / or thermally modified starches, eg. B. hydroxypropyl starch phosphate, dihydroxypropyl distarch phosphate or the commercial products Dry Flo ^® . Dextrans and their derivatives, e.g. B. dextran sulfate. Also preferred are nonionic cellulose derivatives, such as methyl cellulose, hydroxypropyl cellulose or hydroxyethyl cellulose, and cationic cellulose derivatives, e.g. B. the commercial products Celquat ^® and Polymer JR ^® , and preferably Celquat ^® H 100, Celquat ^® L 200 and Polymer JR ^® 400 (Poryquaternium-10) and Polyquaternium-24. Further preferred examples are polysaccharides from fucose units, e.g. B. the commercial product Fucogel ^® . The polysaccharides composed of amino sugar units, in particular chitins and their deacetylated derivatives, the chito- sane, and mucopolysaccharides. The preferred mucopoly saccharides according to the invention include hyaluronic acid and its derivatives, e.g. B. sodium hyaluronate or dimethylsilanol hyaluronate, and chondroitin and its derivatives, e.g. B. chondroitin sulfate.

The cosmetic and pharmaceutical preparations according to the invention can contain further plant extracts. They are usually produced by extracting the entire 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, the extracts from the meristem, i.e. the divisible educational tissue of the plants, and special plants such as green tea, witch hazel, chamomile, calendula, peony, aloe vera, horse chestnut, sage, willow bark, hawthorn, linden flowers, almonds, spruce needles, sandalwood , Coconut, kiwi, guava, lime, mango, apricot, wheat, melon, orange, grapefruit, avocado, rosemary, mallow, cuckoo flower, thyme, lemon balm, marshmallow (Althaea), mallow (Malva sylvestris), ginseng, lily of the valley and sweet potato are preferred , Algae extracts can also be used to advantage. The algae extracts used according to the invention come from green algae, brown algae, red algae or blue-green algae (cyanobacteria). The algae used for the extraction can be of natural origin as well as obtained through biotechnological processes and, if desired, can be changed compared to the natural form. The organisms can be changed genetically, by 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 Spirulina species, which were cultivated in a magnesium-enriched medium.

The extracts from chamomile, spirulina, green tea, aloe vera, meristem, lily of the valley, apricot, marigold, guava, sweet potato, lime, mango, kiwi, cucumber, mallow, marshmallow and witch hazel are particularly preferred. The cosmetic and pharmaceutical preparations according to the invention can also contain mixtures of several, in particular two, different plant extracts. The cosmetic and pharmaceutical preparations according to the invention can contain further active ingredients, auxiliaries and additives, for example:

Vitamins, provitamins and vitamin precursors from groups A, C, E and F, especially retinol (vitamin Ai) and its esters, e.g. the acetate and the palmitate, 3,4-didehydroretinol (vitamin A ₂ ), ß-carotene (provitamin des Vitamin A-ι), ascorbic acid (vitamin C), and the palmitic acid esters, glucosides or phosphates of ascorbic acid, tocopherols, especially α-tocopherol and its esters, for. B. the acetate, nicotinate, phosphate and succinate; also vitamin F, which is understood to mean essential fatty acids, in particular linoleic acid, linolenic acid and arachidonic acid;

allantoin,

bisabolol,

Antioxidants, for example amino acids (e.g. glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (e.g. urocanic acid) and their derivatives, peptides such as D, L-carnosine, D-carnosine, L- Carnosine and its derivatives (e.g. anserine), chlorogenic acid and its derivatives, lipoic acid and its derivatives (e.g. dihydroliponic acid), aurothioglucose, propylthiouracil and other thiols (e.g. thioredoxin, glutathione, cysteine, cystine, cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl, γ-linoleyl, cholesteryl and glyceryl esters) and their salts, dilauryl thiodipropionate, distearyl thiodipropionate , Thiodipropionic acid and its derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) as well as sulfoximine compounds (e.g. buthionine sulfoximines, homocysteine sulfoximine, butionic sulfones, penta-, hexa-, heptathione sulfoximine) in very low tolerable dosages (e.g. B. pmol to μmol / kg), further (Me tall) chelators (e.g. B. α-hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), humic acid, bile acid, bile extracts, bilirubin, biliverdin, EDTA, EGTA and their derivatives, unsaturated fatty acids and their derivatives (e.g. γ-linolenic acid, linoleic acid, oleic acid), folic acid and their derivatives, ubiquinone and ubiquinol and their derivatives, the coniferyl benzoate of benzoin, rutinic acid and derivatives thereof, α-glycosyl rutin, ferulic acid, Furfurylidenglucitol, carnosine, butyl hydroperoxide xytoluol, butylhydroxyanisole, Nordihydroguajakharzsäure, Nordihydro- guajaretsäure, trihydroxybutyrophenone, uric acid and derivatives thereof, catalase, superoxide dismutase, zinc and its derivatives (e.g. ZnO, ZnS0 ₄ ), selenium and its derivatives (e.g. selenium methionine), stilbenes and their derivatives (e.g. stilbene oxide, trans-stilbene oxide) and the derivatives suitable as antioxidants ( Salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) of these active substances,

Ceramides and pseudoceramides,

Triterpenes, especially triterpenic acids such as ursolic acid, rosmaric acid, betulinic acid, boswellic acid and bryonolic acid,

Monomeric catechins, especially catechin and epicatechin, leukoanthocyanidins, catechin polymers (catechin tannins) and gallotannins,

Thickeners, e.g. B. gelatin, vegetable gums such as agar agar, guar gum, alginates, xanthan gum, gum arabic, karaya gum or locust bean gum, natural and synthetic clays and layered silicates, e.g. B. bentonite, hectorite, montmorillonite or Laponite ^® , fully synthetic hydrocolloids such. B. polyvinyl alcohol, and also Ca, Mg or Zn soaps of fatty acids,

plant glycosides,

Structurants such as maleic acid and lactic acid,

dimethyl isosorbide,

Alpha, beta and gamma cyclodextrins, in particular for stabilizing retinol,

Solvents, swelling and penetration substances such as ethanol, isopropanol, ethylene glycol, propylene glycol, propylene glycol monoethyl ether, glycerin and diethylene glycol, carbonates, hydrogen carbonates, guanidines, ureas and primary, secondary and tertiary phosphates Perfume oils, pigments and dyes for coloring the agent, substances for adjusting the pH, e.g. B. α- and ß-hydroxycarboxylic acids, complexing agents such as EDTA, NTA, ß-alaninediacetic acid and phosphonic acids, - opacifiers such as latex, styrene / PVP and styrene / acrylamide copolymers, pearlescent agents such as ethylene glycol mono- and distearate and PEG-3 distearate , Blowing agents such as propane-butane mixtures, N ₂ 0, dimethyl ether, C0 ₂ and air.

Additives to the cosmetic or pharmaceutical skin treatment agents are selected from the vitamins, provitamins or vitamin precursors of the vitamin B group or their derivatives and the derivatives of 2-furanone.

The vitamin B group or the vitamin B complex include, among others

• Vitamin Bi, common name thiamine, chemical name 3 - [(4 ^' -amino-2 ^' - methyl-5 ^' -pyrimidinyl) -methyl] -5- (2-hydroxyethyl) -4-methylthiazolium chloride. Thiamine hydrochloride is preferably used in amounts of 0.05 to 1% by weight, based on the total agent.

• Vitamin B ₂ , common name riboflavin, chemical name 7,8-dimethyl-10- (1-D-ribityl) -benzo [g] pteridine-2,4 (3 / - /, 10 / - /) - dione. In free form, riboflavin comes e.g. B. in whey before, other riboflavin derivatives can be isolated from bacteria and yeast. A stereoisomer of riboflavin which is also suitable according to the invention is lyxoflavin which can be isolated from fishmeal or liver and which carries a D-arabityl radical instead of D-ribityl. Riboflavin or its derivatives are preferably used in amounts of 0.05 to 1% by weight, based on the total agent.

• Vitamin B ₃ . The compounds nicotinic acid and nicotinamide (niacinamide) are often listed under this name. The nicotinamide which is present in the cosmetic and pharmaceutical preparations according to the invention preferably in amounts of 0.05 to 1% by weight, based on the total composition, is preferred according to the invention. Vitamin B ₅ (pantothenic acid and panthenol). Panthenol is preferably used. Derivatives of panthenol which can be used according to the invention are, in particular, the esters and ethers of panthenol and cationically derivatized panthenols. In a further preferred embodiment of the invention, instead of and in addition to pantothenic acid or panthenol, derivatives of 2-furanone with the general structural formula (I) can also be used.

(I)

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 - hydrocarbon residue, a saturated or mono- or di-unsaturated, branched or linear mono-, di- or trihydroxy-C ₂ -C - hydrocarbon residue or a saturated or mono- or di-unsaturated, branched or linear mono-, di - Or triamino-C ₂ -C - hydrocarbon residue. Particularly preferred derivatives are the commercially available substances dihydro-3-hydroxy-4,4-dimethyl-2 (3H) -furanone with the common name pantolactone (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), where in formula (I) R ^{1 is} a hydroxyl group, R ^{2 is} a hydrogen atom, R ³ and R ^{4 represent} a methyl group and R ⁵ and R ^{6 represent} a hydrogen atom. The stereoisomer (R) - pantolactone is formed when pantothenic acid is broken down. The above-mentioned compounds of the vitamin B ₅ type and the 2-furanone derivatives are preferably present in the cosmetic and pharmaceutical preparations according to the invention in a total amount of 0.05 to 10% by weight, based on the total composition. Total amounts of 0.1 to 5% by weight are particularly preferred.

• Vitamin B ₆ , which does not mean a uniform substance, but rather the derivatives of 5-hydroxymethyl-2-methylpyridin-3-ol known under the trivial names pyridoxine, pyridoxamine and pyridoxal. Vitamin β is preferably present in the cosmetic and pharmaceutical preparations according to the invention in amounts of 0.0001 to 1.0% by weight, in particular in amounts of 0.001 to 0.01% by weight.

• Vitamin B ₇ (biotin), also known as vitamin H or "skin vitamin". Biotin is (3aS, 4S, 6a?) - 2-oxohexahydrothienol [3,4-c /] - imidazole-4-valeric acid. The cosmetic and pharmaceutical preparations according to the invention preferably contain biotin in amounts of 0.0001 to 1.0% by weight, in particular in amounts of 0.001 to 0.01% by weight.

Panthenol, pantolactone, nicotinamide and biotin are very particularly preferred according to the invention.

The skin treatment compositions according to the invention can contain one or more film-forming, emulsion-stabilizing, thickening or adhesive polymers selected from natural and synthetic polymers, which can be cationic, anionic, amphoteric or non-ionic.

Cationic, anionic and nonionic are preferred according to the invention

Polymers.

Preferred among the cationic polymers are polysiloxanes with quaternary groups, e.g. , The commercial products Q2-7224 (Dow Corning), Dow Corning ^® 929 Emulsion (with Amodimethicone), SM-2059 (General Electric), SLM-55067 (Wacker) and Abil ^® -Quat 3270 and 3272 (Th. Goldschmidt).

Preferred anionic polymers which can support the action of the active ingredient used according to the invention contain carboxylate and / or sulfonate groups and, for example, acrylic acid, methacrylic acid, crotonic acid, maleic anhydride and 2-acrylamido-2-methylpropanesulfonic acid as monomers. The acidic groups can be present in whole or in part as sodium, potassium, ammonium, mono- or triethanolammonium salt. Preferred monomers 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. In this embodiment, it is preferred to use copolymers of at least one anionic monomer and at least one nonionic monomer. With regard to 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 consists of 70 to 55 mol% of acrylamide and 30 to 45 mol% of 2-acrylamido-2-methylpropanesulfonic acid, the sulfonic acid groups being wholly or partly as sodium, potassium, ammonium, mono- or triethanolammonium Salt. This copolymer can also be crosslinked, the preferred crosslinking agents being polyolefinically unsaturated compounds such as tetraallyloxyethane, allyl sucrose, allylpentaerythritol and methylene bisacrylamide. Such a polymer is contained in the commercial product Sepigel ^® 305 from SEPPIC. The use of this compound has proven to be particularly advantageous in the context of the teaching according to the invention. Also known as compound with isohexadecane and sold under the name Simulgel® ^® 600 Polysorbate-80 sodium acryloyldimethyltaurate copoly- mers have proven effective as inventively particularly. Other particularly preferred anionic homopolymers and copolymers 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 ^® . A particularly preferred anionic copolymer contains as monomer to 80-98% unsaturated, optionally substituted C ₃ - ₆ carboxylic acid or its anhydride as well as 2-20% optionally substituted acrylate of saturated Cιo- ₃ o-carboxylic acids, wherein the copolymer having the The aforementioned networking agents can be networked. Corresponding commercial products are Pemulen ^® and the Carbopol ^® types 954, 980, 1342 and ETD 2020 (ex BF Goodrich).

Suitable nonionic polymers are, for example, polyvinyl alcohols, which can be partially saponified, e.g. B. the commercial products Mowiol ^® and vinyl pyrrolidone / vinyl ester copolymers and polyvinyl pyrrolidones, which, for. B. are sold under the trademark Luviskol ^® (BASF).

In addition to topical application, the pharmaceutical preparations according to the invention are also administered enterally, parenterally or rectally. For administration via the enteral route, the pharmaceutical preparations can be in the form of tablets, capsules, dragees, syrups, suspensions, solutions, powders, granules or emulsions. For parenteral administration, the preparations may be in the form of solutions or suspensions for perfusion or injection. The preparations can be in the form of suppositories for administration by the rectal route.

For the preparation of pharmaceutical preparations, the active ingredients, optionally in combination with other active substances, together with one or more inert customary carriers and / or diluents, for. B. with corn starch, milk sugar, cane sugar, sorbitol, microcrystalline cellulose, magnesium stearate, polyvinylpyrrolidone, citric acid, tartaric acid, water, water / ethanol, water / glycerol, water / sorbitol, water / polyethylene glycol, Incorporate propylene glycol, carboxymethyl cellulose or fat-containing substances such as hard fat or their suitable mixtures into conventional galenical preparations such as tablets, dragees, capsules, powders, suspensions, drops, ampoules, juices or suppositories. The daily dosage of the mixture of active substances required to achieve a corresponding effect in pharmaceutical applications consists of the substances with a stimulating and / or depolarizing effect on the C-nerve fibers, the phosphodiesterase inhibitors and the substances with an anti-estrogenic effect is expediently 0.1 to 10 mg / kg body weight, preferably 0.5 to 2 mg / kg body weight.

The pharmaceutical preparations according to the invention are preferably suitable for the therapeutic treatment of cellulite.

Another object of the invention is accordingly the use of a combination of active ingredients

(a) at least one substance that stimulates and / or depolarizes C-nerve fibers

(b) at least one phosphodiesterase inhibitor and

(c) at least one substance with an anti-estrogenic effect for producing a preparation for the therapeutic treatment of cellulite.

The compositions according to the invention are prepared in such a way that the aqueous phase, which contains water-soluble active ingredients and ingredients and, if appropriate, water-soluble emulsifiers, and the oil phase which contains fats, oils, oil-soluble active ingredients and optionally oil-soluble emulsifiers, at a temperature of 10 to 90 ° C are mixed intensively.

The following examples are intended to illustrate the present invention. Unless otherwise stated, all percentages are based on the total weight of the preparations. Examples:

Example 1: Cosmetic preparations

Anti-cellulite gels

Anti-cellulite creams

Anti-cellulite lotions

Example 2: Test results

In a four-week use test, the anti-cellulite gel according to Example 1 with the formulation Gel-5 was tested for its effectiveness in relation to the cellulite phenomenon and its cosmetic acceptance in 25 women (half-side test against placebo). The test participants were asked directly after the use test about the effectiveness of the product and the cosmetic acceptance in a standardized way.

Over 80% of the test subjects felt a tingling and warming skin feeling. After only four weeks of use, 28% of women noticed an improvement in cellulite symptoms and 40% of women reported an improvement in skin firmness. 84% were satisfied with the skin tolerance of the product and 72% could imagine using the product again.

Claims

claims

1. Comprehensive cosmetic or pharmaceutical preparation

(a) a substance that stimulates and / or depolarizes C-nerve fibers

(b) a phosphodiesterase inhibitor

(c) a substance with an anti-estrogenic effect in a physiologically acceptable carrier.

2. Preparation according to claim 1, characterized in that it is C-nerve fibers of the skin.

3. Preparation according to claim 2, characterized in that the stimulation and / or depolarization of the C-nerve fibers of the skin is carried out by stimulating the capsaicin receptors of the nerve fibers.

4. Preparation according to one of claims 1 to 3, characterized in that the C-nerve fiber stimulating substance is selected from the group formed by capsaicin, N-vanillyl-nonanamide, a glycoside of these substances, and mixtures thereof.

5. Preparation according to claim 1, characterized in that the phosphodiesterase inhibitor is selected from xanthine or a methylxanthine.

6. Preparation according to claim 1, characterized in that the substance with an anti-estrogenic effect is selected from the group formed by tamoxifen, aminoglutethimide, clomiphene, testosterone, androsterone, isoflavones, isoflavone glycosides and mixtures thereof.

7. Preparation according to claim 6, characterized in that the substance with an anti-estrogenic effect is selected from the group formed by an isoflavone, an isoflavone glycoside and mixtures thereof.

8. Preparation according to claim 7, characterized in that the isoflavone or isoflavone glycoside is contained as part of a substance mixture obtained from a plant.

9. Preparation according to claim 8, characterized in that the substance mixture is a soy extract.

10. Preparation according to one of claims 1 to 9, characterized in that the preparation

0.0001 to 3% by weight of component (a) 1 to 15% by weight of component (b) 0.1 to 20% by weight of component (c), each based on the total weight of the preparation ,

11. Preparation according to claim 10, characterized in that the preparation 0.005 to 0.5% by weight of component (a) 5 to 10% by weight of component (b) 1 to 10% by weight of component (c ), each based on the total weight of the preparation.

12. Preparation according to one of claims 1 to 11, characterized in that the physiologically compatible carrier comprises one or more customary cosmetic and / or pharmaceutical auxiliaries which are selected from fats, oils, waxes, silicones, emulsifiers, light protection filters, protein hydrolyzates, mono -, Oligo- and polysaccharides, plant extracts, antioxidants, vitamins, fragrances, dyes, thickeners, moisturizing and / or moisturizing substances, surfactants, flavors, sweeteners, adsorbents and other active ingredients and auxiliaries.

13. Preparation according to one of claims 1 to 12, characterized in that the physiologically compatible carrier one or more film-forming, emulsion-stabilizing, thickening or adhesive polymers selected from contains natural and synthetic polymers, which can be cationic, anionic, amphoteric or non-ionic.

14. Preparation according to one of claims 1 to 13, that the physiological carrier contains a substance selected from the vitamins, provitamins or vitamin precursors of the vitamin B group or their derivatives and the derivatives of 2-furanone.

15. Use of a preparation according to any one of claims 1 to 14 for the cosmetic treatment of cellulite or local excess fat or for cosmetic tightening of the skin.

16. Use according to claim 15, characterized in that the cosmetic preparation is in the form of an oil, an ointment, a gel or in the form of a creamy or milky oil-in-water or water-in-oil emulsion.

17. Use of a combination of active ingredients

(a) a substance that stimulates and / or depolarizes C-nerve fibers

(b) a phosphodiesterase inhibitor

(c) a substance with an anti-estrogenic effect for the manufacture of a pharmaceutical preparation for the therapeutic treatment of cellulite.

18. Use according to claim 17, characterized in that the preparation is a pharmaceutical preparation in the form of an emulsion, a gel, a suspension, a solution, a granulate, a powder or a syrup or in the form of capsules, dragees, suppositories, tablets or patches.

19. A method for producing a cosmetic or pharmaceutical preparation according to claims 1 to 18, characterized in that the aqueous phase and the oil phase are mixed intensively at a temperature of 10 to 90 ° C.