DE102012214034A1 - Use of cosmetic or dermatological formulation in the form of oil-water emulsion having active ingredient comprising urea, carnitine and/or acyl-carnitine for tightening and strengthening of skin and for treating and/or preventing cellulite - Google Patents

Abstract

Use of cosmetic or dermatological formulation, which is in the form of oil-water emulsion with a content of active ingredient comprising urea, carnitine and/or acyl-carnitine for tightening and/or strengthening of the skin, and for treating and/or preventing cellulite, is claimed.

Description

The present invention relates to cosmetic or dermatological dermatological preparations containing active ingredients for the care and protection of the skin, in particular the sensitive skin as well as especially in the foreground standing by intrinsic and / or extrinsic factors aged or aging skin and the use of such agents and Combinations of such active ingredients in the field of cosmetic and dermatological skin care.

Cosmetic skincare primarily means that the natural function of the skin acts as a barrier against environmental influences (eg dirt, chemicals, microorganisms) and against the loss of endogenous substances (eg water, natural fats, electrolytes) strengthened or restored.

If this function is disturbed, it may lead to increased absorption of toxic or allergenic substances or the infestation of microorganisms and as a result to toxic or allergic skin reactions.

The aim of skin care is also to compensate for the daily loss of fat and water loss of the skin. This is especially important when the natural regeneration capacity is insufficient. In addition, skin care products to protect against environmental influences, especially from the sun and wind, and delay the aging of the skin.

• a) Trockenheit, Rauhigkeit und Ausbildung von Trockenheitsfältchen,
• b) Juckreiz und
• c) verminderte Rückfettung durch Talgdrüsen (z. B. nach Waschen).

The chronological skin aging is z. B. caused by endogenous, genetically determined factors. In epidermis and dermis it comes due to aging z. As to the following structural damage and dysfunction, which may also fall under the term "senile xerosis":

• a) dryness, roughness and formation of dryness wrinkles,
• b) itching and
• c) diminished fatty acid regeneration (eg after washing).

• d) Sichtbare Gefäßerweiterungen (Teleangiektasien, Cuperosis);
• e) Schlaffheit und Ausbildung von Falten;
• f) lokale Hyper-, Hypo- und Fehlpigmentierungen (z. B. Altersflecken) und
• g) vergrößerte Anfälligkeit gegenüber mechanischem Stress (z. B. Rissigkeit).

Exogenous factors, such as UV light and chemical noxae, can be cumulatively effective and z. B. accelerate the endogenous aging processes or supplement them. In epidermis and dermis it comes in particular by exogenous factors z. As to the following structural damage and dysfunction in the skin, which go beyond the extent and quality of the damage in chronological aging:

• d) Visible vascular dilations (telangiectasias, cuperosis);
• e) slackness and formation of wrinkles;
• f) local hyper-, hypo- and false pigmentation (eg age spots) and
• g) increased susceptibility to mechanical stress (eg cracking).

The present invention relates in particular to products for the care of naturally aged skin, as well as the phenomena listed under a), e) and g).

Products for the care of relaxed, especially aged, skin are known per se. They contain z. As retinoids (vitamin A acid and / or derivatives thereof) or vitamin A and / or its derivatives. Their effect on the structural damage, however, is limited in scope. In addition, there are significant difficulties in product development in stabilizing the active ingredients sufficiently against oxidative degradation. In addition, the use of vitamin A acidic products often causes severe erythematous skin irritation. Retinoids can therefore only be used in low concentrations.

Often, a concomitant phenomenon of obesity and / or the so-called cellullite often associated with it is associated with the sagging skin.

The body awareness of consumers has increased significantly in recent years. In addition to cleaning and nurturing applications, measures are increasingly taken to improve the body silhouette. Cellulite - a widespread phenomenon - occupies a central position. The visible picture of cellulite is based on an increase in fat deposits in the subcutis (subcutaneous fatty tissue), a weakening of connective tissue and a reduction in the flow conditions in the blood and lymphatic channels. The cause is thus a partial plant-related weakening of the connective tissue with simultaneous occurrence of enlarged fatty cell chambers as a result of obesity, unbalanced diet, lack of exercise. The development of cellulite can also be attributed to an increased permeability of the capillary walls, which allows the penetration of water into the connective tissue.

In addition, there may be a local lack of testosterone on the affected areas of the skin. Anyway, cellulite is a phenomenon that is almost never seen in men.

The object of the present invention was therefore to find ways that avoid the disadvantages of the prior art. In particular, it was an object of the present invention to provide preparations which can bring about an advantageous tightening of softened skin.

It has surprisingly been found that the use of cosmetic or dermatological preparations in the form of O / W emulsions containing active ingredient combinations of urea and carnitine and / or one or more acyl carnitines for firming and / or strengthening the skin the disadvantages of State of the art helps.

Also advantageous according to the invention is the use of cosmetic or dermatological preparations in the form of O / W emulsions containing active ingredient combinations of urea and carnitine and / or one or more acyl carnitines for the cosmetic and / or dermatological treatment and / or prophylaxis of cellulite.

(Summenformel C₇H₁₅NO₃) auf.L-carnitine [3-hydroxy-4- (trimethylammonio) butyric betaine] has the structural formula

(Empirical formula C ₇ H ₁₅ NO ₃ ).

The L-form of carnitine is widely used in animal tissues, particularly striped muscle. It is used in fatty acid metabolism as a carrier for acyl groups through the mitochondrial membrane. These are transferred by an acyltransferase from acyl-coenzyme A to the hydroxy group of L-carnitine. The transport of L-carnitine and acyl-L-carnitine through the membrane takes place by mediating a transport protein (translocase). Both enantiomers (D and L form) are to be used advantageously in the context of the present invention. It may also be advantageous to use any mixtures of enantiomers, for example a racemate of D and L form.

wobei R gewählt wird aus der Gruppe der verzweigten und unverzweigten Alkylreste mit bis zu 10 Kohlenstoffatomen. Bevorzugt sind Propionylcarnitin und, ganz besonders bevorzugt, Acetylcarnitin. Beide Entantiomere (D- und L-Form) sind vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden. Es kann auch hier von Vorteil sein, beliebige Enantiomerengemische, beispielsweise ein Racemat aus D- und L-Form, zu verwenden.According to the invention acyl-carnitines are selected from the group of substances of the following general structural formula

wherein R is selected from the group of branched and unbranched alkyl radicals having up to 10 carbon atoms. Preference is given to propionyl carnitine and, most preferably, acetyl carnitine. Both enantiomers (D and L form) are to be used advantageously in the context of the present invention. It may also be advantageous here to use any enantiomer mixtures, for example a racemate of D and L form.

Advantageously, the preparations according to the invention contain from 0.001 to 10% by weight of carnitine and / or one or more acylcarnitines, based on the total weight of the preparations.

Cosmetic or dermatological preparations according to the invention advantageously contain 0.01 to 60 wt .-%, preferably 0.1 to 25 wt .-%, particularly preferably 1 to 10 wt .-% of urea, based on the total weight of the preparations.

According to the invention, preparations containing the active compound combinations according to the invention can be used with customary antioxidants.

Advantageously, the antioxidants are selected from the group consisting of amino acids (eg, glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (eg, urocanic acid) and derivatives thereof, peptides such as D, L-carnosine, D- Carnosine, L-carnosine and their derivatives (eg anserine), carotenoids, carotenes (eg α-carotene, β-carotene, lycopene) and their derivatives, lipoic acid and derivatives thereof (eg dihydrolipoic acid), Aurothioglucose, propylthiouracil and other thiols (eg 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 derivatives thereof (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) and sulfoximine compounds (eg buthionine sulfoximines, Homocysteine sulfoximine, buthionine sulfone, penta-, hexa-, heptathionine sul foximin) in very low tolerated dosages (e.g. Pmol to μmol / kg), furthermore (metal) chelators (eg α-hydroxyfatty acids, palmitic acid, phytic acid, lactoferrin), α-hydroxy acids (eg citric acid, lactic acid, malic acid), humic acid, bile acid, Bile extracts, bilirubin, biliverdin, EDTA, EGTA and their derivatives, unsaturated fatty acids and their derivatives (eg γ-linolenic acid, linoleic acid, oleic acid), folic acid and its derivatives, alaninediacetic acid, flavonoids, polyphenols, catechins, vitamin C and derivatives ( for example, ascorbyl palmitate, Mg ascorbyl phosphate, ascorbyl acetate), tocopherols and derivatives (eg, vitamin E acetate), benzoic resin koniferyl benzoate, rutinic acid and derivatives thereof, ferulic acid and its derivatives, butylhydroxytoluene, butylhydroxyanisole, nordihydroguaiacetic acid, nordihydroguiaretic acid , Trihydroxybutyrophenone, uric acid and its derivatives, mannose and its derivatives, zinc and its derivatives (eg ZnO, ZnSO ₄ ), selenium and its derivatives (eg selenomethionine), stilbenes and their derivatives (eg stilbene oxide, trans-stilbene oxide) and the derivatives suitable according to the invention (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) of these active substances mentioned.

The amount of the antioxidants (one or more compounds) in the preparations is preferably from 0.001 to 30% by weight, particularly preferably from 0.05 to 20% by weight, in particular from 1 to 10% by weight, based on the total weight of the preparation ,

The prophylaxis or the cosmetic or dermatological treatment with the active ingredient used according to the invention or with the cosmetic or topical dermatological preparations with an effective content of the active ingredient used according to the invention is carried out in the usual manner, in such a way that the active ingredient used according to the invention or the cosmetic or topical dermatological preparations having an effective content of active ingredient used according to the invention is applied to the affected skin areas.

According to the invention emulsions, z. As in the form of a cream, a lotion, a cosmetic milk are advantageous and contain z. As fats, oils, waxes and / or other fatty substances, and water and one or more emulsifiers, such as are commonly used for such a type of formulation.

It is also possible and advantageous in the context of the present invention to incorporate the active ingredient used according to the invention into aqueous systems or surfactant preparations for cleaning the skin and hair.

Of course, it is known to those skilled in the art that sophisticated cosmetic compositions are usually not conceivable without the customary auxiliaries and additives. These include, for example, bodying agents, fillers, perfume, dyes, emulsifiers, additional active ingredients such as vitamins or proteins, light stabilizers, stabilizers, insect repellents, alcohol, water, salts, antimicrobial, proteolytic or keratolytic substances, etc.

Mutatis mutandis apply corresponding requirements for the formulation of medicinal preparations.

Medicinal topical compositions according to the present invention usually contain one or more drugs in effective concentration. For the sake of simplicity, a clear distinction between cosmetic and medical use and corresponding products is made to the statutory provisions of the Federal Republic of Germany (eg Cosmetics Ordinance, Food and Medicinal Products Act).

It is also advantageous to add the active ingredient used according to the invention as an additive to preparations which already contain other active ingredients for other purposes.

The cosmetic and / or dermatological formulations according to the invention may be composed as usual and used for the treatment of the skin and / or the hair in the sense of a dermatological treatment or a treatment in the sense of nourishing cosmetics. But they can also be used in make-up products in decorative cosmetics or in the cosmetic and dermatological cleaning products.

If the cosmetic or dermatological preparation is a solution or lotion, the solvents used can be: water or aqueous solutions, furthermore oils, such as triglycerides of capric or caprylic acid, but preferably castor oil, fats, waxes and other natural and synthetic fatty substances, preferably Esters of fatty acids with lower C-number alcohols, e.g. With isopropanol, propylene glycol or glycerol, or esters of fatty alcohols with alkanoic acids of low C number or with fatty acids, but also alcohols, diols or polyols of low C number, and their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol, ethylene glycol, Ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and analogous products.

In particular, mixtures of the abovementioned solvents are used, as may be an advantageous further constituent of alcohol in the case of alcoholic solvents.

Cosmetic and dermatological preparations according to the invention, also z. As to protect the skin from UV rays, may be in various forms, such as. B. are usually used for this type of preparations. So they can z. Example, a solution, a water-in-oil (W / O) or oil-in-water (O / W) type emulsion, or a multiple emulsions, such as water-in-oil-in-water type (W / O / W), oil-in-water-in-oil (O / W / O), a gel, a hydrodispersion, a lamellar phase, a liquid isotropic solution phase, a micellar phase, a solid or dispersed one. or multiply hexagonal phase, a solid or dispersed single or multi-cubic phase, a lyotropic phase, a crystalline phase, a solid stick or even an aerosol.

The active compounds according to the invention can also be used particularly advantageously in microemulsions, for example as in the German Offenlegungsschrift DE-195 9 079 described, are used.

The oil phase of the preparations according to the invention is advantageously selected from the group of esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 3 to 30 carbon atoms and saturated and / or unsaturated, branched and / or unbranched alcohols of one chain length from 3 to 30 carbon atoms, from the group of esters of aromatic carboxylic acids and saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of 3 to 30 carbon atoms. Such ester oils can then be advantageously selected from the group isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl stearate, isononyl isononanoate, 2-ethylhexyl palmitate, 2-ethylhexyl laurate, 2-hexyldecyl stearate, 2 Octyl dodecyl palmitate, oleyl oleate, oleyl erucate, erucyl oleate, erucyl erucate and synthetic, semi-synthetic and natural mixtures of such esters, e.g. B. jojoba oil.

Furthermore, the oil phase can be advantageously selected from the group of branched and unbranched hydrocarbons and waxes, the silicone oils, the dialkyl ethers, the group of saturated or unsaturated, branched or unbranched alcohols, and the fatty acid triglycerides, in particular the triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids of a chain length of 8 to 24, in particular 12-18 C-atoms. The fatty acid triglycerides can be selected, for example, advantageously from the group of synthetic, semi-synthetic and natural oils, for. For example, olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm kernel oil and the like.

Any mixtures of such oil and wax components are also advantageous to use in the context of the present invention.

Advantageously, the oil phase is selected from the group consisting of 2-ethylhexyl isostearate, octyldodecanol, isotridecyl isononanoate, isoeicosane, 2-ethylhexyl cocoate, C _12-15 alkyl benzoate, caprylic capric acid triglyceride, dicaprylyl ether.

Particularly advantageous are mixtures of C _12-15 -alkyl benzoate and 2-ethylhexyl isostearate, mixtures of C _12-15 -alkyl benzoate and isotridecyl isononanoate and mixtures of C _12-15 -alkyl benzoate, 2-ethylhexyl isostearate and isotridecyl isononanoate.

Of the hydrocarbons, paraffin oil, squalane and squalene are to be used advantageously in the context of the present invention.

Advantageously, the oil phase may further comprise a content of cyclic or linear silicone oils or consist entirely of such oils, although it is preferred to use an additional content of other oil phase components in addition to the silicone oil or silicone oils.

Advantageously, cyclomethicone (octamethylcyclotetrasiloxane) is used as the silicone oil to be used according to the invention. However, other silicone oils are also advantageous for the purposes of the present invention, for example hexamethylcyclotrisiloxane, polydimethylsiloxane, poly (methylphenylsiloxane).

Also particularly advantageous are mixtures of cyclomethicone and isotridecyl isononanoate, cyclomethicone and 2-ethylhexyl isostearate.

Advantageously, the content of the oil phase is between 1 and 50 wt .-%, based on the total weight of the preparations, preferably 2.5-30 wt .-%, particularly preferably 5-15 wt .-%.

For use, the cosmetic and / or dermatological formulations according to the invention are applied to the skin in a sufficient amount in the manner customary for cosmetics and dermatological agents.

Beispielrezeptur 10 11 12 13 14 15 Aluminumstärkeoctenylsuccinat 1 1 1 Arginin HCL 0,5 1 1,5 Caprylic/Capric Triglycerid 1,5 1,5 1,5 Carbomer/Natriumpolyacrylat 0,2 0,2 0,2 Carnitin 0,125 0,25 1,5 1,5 1 1,5 Mikrokristallines Wachs + fl. Paraffin 2 2 2 Ceramid 3 0,005 0,05 0,5 Cetylstearyalkohol 0,5 0,5 0,5 2 2 2 Cetylstearyalkohol + PEG-40 Rizinusöl + Natriumceteralsulfat 3 3 3 Dicaprylylether 5 5 5 Ethylhexylcocoat 1,5 1,5 1,5 Glycerin 3,5 5 3,5 10 5 10 Glycerylglucosid 3 7 10 3 7 10 Harnstoff 10 20 40 5 10 20 1,2-Hexandiol 0,5 0,5 0,5 Hydrierte Kokosglyceride 2 2 2 Isopropylstearat 6 6 6 Kaliumsorbat 0,06 0,06 0,06 lineares Silikonöl 1 1 1 Mannitol + Serin + Sucrose + Citrulline + Glycogen + Histidin + Alanin + Threonin + Glutaminsäure + Lysin 0,1 1 5 Milchsäure 0,4 0,4 0,4 0,9 0,9 0,9 Natriumchlord 0,25 0,25 0,25 Natriumlactat 4,1 4,1 4,1 10 10 10 Nylon-12 1 1 1 Octyldodecanol 1,5 1,5 1,5 Parfum 0,4 0,4 0,4 Phenoxyethanol 0,5 0,5 0,5 0,8 0,8 0,8 Polyglyceryl-4 Stearat/Polyhydroxystearat/Sebacat 1 2 3 Propylparaben Sheabutter 2 2 2 Natrium PCA 1 1 1 Sorbitanstearat 1 1 1 Wasser, dest. AD 100 AD 100 AD 100 AD 100 AD 100 AD 100 The following examples are intended to illustrate the embodiments of the present inventions.

example recipe 10 11 12 13 14 15 Aluminumstärkeoctenylsuccinat 1 1 1 Arginine HCL 0.5 1 1.5 Caprylic / Capric triglyceride 1.5 1.5 1.5 Carbomer / sodium polyacrylate 0.2 0.2 0.2 carnitine 0,125 0.25 1.5 1.5 1 1.5 Microcrystalline wax + fl. Paraffin 2 2 2 Ceramide 3 0.005 0.05 0.5 Cetylstearyalkohol 0.5 0.5 0.5 2 2 2 Cetylstearyl alcohol + PEG-40 castor oil + sodium ceteral sulfate 3 3 3 dicaprylyl 5 5 5 ethylhexylcocoate 1.5 1.5 1.5 glycerin 3.5 5 3.5 10 5 10 Glycerylglucosid 3 7 10 3 7 10 urea 10 20 40 5 10 20 1,2-hexanediol 0.5 0.5 0.5 Hydrogenated coconut glycerides 2 2 2 isopropyl 6 6 6 potassium sorbate 0.06 0.06 0.06 linear silicone oil 1 1 1 Mannitol + serine + sucrose + citrulline + glycogen + histidine + alanine + threonine + glutamic acid + lysine 0.1 1 5 lactic acid 0.4 0.4 0.4 0.9 0.9 0.9 sodium Chlord 0.25 0.25 0.25 sodium lactate 4.1 4.1 4.1 10 10 10 Nylon-12 1 1 1 octyldodecanol 1.5 1.5 1.5 Perfume 0.4 0.4 0.4 phenoxyethanol 0.5 0.5 0.5 0.8 0.8 0.8 Polyglyceryl-4 stearate / polyhydroxystearate / sebacate 1 2 3 Propylparaben shea butter 2 2 2 Sodium PCA 1 1 1 sorbitan 1 1 1 Water, dist. AD 100 AD 100 AD 100 AD 100 AD 100 AD 100

QUOTES INCLUDE IN THE DESCRIPTION

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Cited patent literature

• DE 1959079 A [0034]

Claims (4)

Use of cosmetic or dermatological preparations in the form of O / W emulsions containing urea and carnitine active substance combinations and / or one or more acyl carnitines for firming and / or strengthening the skin. Use of cosmetic or dermatological preparations in the form of O / W emulsions containing active compound combinations of urea and carnitine and / or one or more acyl carnitines for the cosmetic and / or dermatological treatment and / or prophylaxis of cellulite. Use according to one of the preceding claims, characterized in that concentrations of 0.01-10% by weight of carnitine and / or one or more acylcarnitines are present in the finished preparations, based on the total weight of the preparations. Use according to one of the preceding claims, characterized in that present in the finished preparations concentrations of 0.01 to 60 wt .-%, preferably 0.1 to 40 wt .-%, particularly preferably 1 to 20 wt .-% of urea , based on the total weight of the preparations.