WO2003011241A1 - Utilization of creatinine and/or creatinine derivatives in cosmetic and dermatological preparations - Google Patents

Utilization of creatinine and/or creatinine derivatives in cosmetic and dermatological preparations Download PDF

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Publication number
WO2003011241A1
WO2003011241A1 PCT/EP2002/008124 EP0208124W WO03011241A1 WO 2003011241 A1 WO2003011241 A1 WO 2003011241A1 EP 0208124 W EP0208124 W EP 0208124W WO 03011241 A1 WO03011241 A1 WO 03011241A1
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WIPO (PCT)
Prior art keywords
skin
derivatives
prophylaxis
preparations
changes
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PCT/EP2002/008124
Other languages
German (de)
French (fr)
Other versions
WO2003011241A8 (en
Inventor
Helga Biergiesser
Thomas Blatt
Inge Kruse
Melanie Schmidt
Uwe SCHÖNROCK
Franz STÄB
Original Assignee
Beiersdorf Ag
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Application filed by Beiersdorf Ag filed Critical Beiersdorf Ag
Priority to EP02760258A priority Critical patent/EP1414401A1/en
Priority to JP2003516473A priority patent/JP2004538299A/en
Publication of WO2003011241A1 publication Critical patent/WO2003011241A1/en
Publication of WO2003011241A8 publication Critical patent/WO2003011241A8/en
Priority to US10/767,962 priority patent/US20040241197A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/44Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/43Guanidines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4946Imidazoles or their condensed derivatives, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/007Preparations for dry skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/008Preparations for oily skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • A61Q5/006Antidandruff preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair
    • A61Q5/008Preparations for oily hair
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00Preparations for affecting hair growth

Definitions

  • the present invention relates to the use of combinations of creatinine and / or creatinine derivatives with creatine and / or its derivatives in cosmetic or dermatological preparations for the treatment and prophylaxis of the symptoms of UV and / or ozone-induced skin damage as well as inflammatory and degenerative skin conditions.
  • Cosmetic skin care is understood primarily to strengthen or restore the skin's natural function as a barrier against environmental influences (e.g., dirt, chemicals, microorganisms) and against the loss of endogenous substances (e.g., water, natural fats, electrolytes).
  • environmental influences e.g., dirt, chemicals, microorganisms
  • endogenous substances e.g., water, natural fats, electrolytes
  • 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.
  • skin care products to protect against environmental influences, especially from the sun and wind, and delay the aging of the skin.
  • the chronological skin aging is caused eg by endogenous, genetically determined factors.
  • the epidermis and der is due to aging, for example, the following structural damage and dysfunction, which may also fall under the term "senile xerosis”: a) dryness, roughness and development of dryness wrinkles; b) itching; and c) reduced rehydration through sebaceous glands (eg after washing).
  • Exogenous factors such as UV light and chemical noxae can be cumulatively effective and e.g. accelerate or supplement endogenous aging processes.
  • exogenous factors occur, e.g. on the following structural damage and dysfunction in the skin that go beyond the extent and quality of the damage caused by chronological aging:
  • the present invention relates in particular to products for the care of naturally aged skin, as well as for the treatment of the consequential damages of photoageing, in particular of the phenomena listed under a) to g).
  • Products for the care of aged skin are known per se. They contain e.g. 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 acid-containing products often causes severe erythematous skin irritation. Retinoids can therefore only be used in low concentrations.
  • the present invention relates to cosmetic preparations with effective protection against harmful oxidation processes in the skin, but also to protect cosmetic preparations themselves or to protect the ingredients of cosmetic preparations from harmful oxidation processes.
  • UVC range rays with a wavelength less than 290 nm
  • UVB range rays in the range between 290 nm and 320 nm, the so-called UVB range, cause erythema simple sunburn or even more or less severe burns.
  • UVA range it is important to have available filter substances, since its rays can cause reactions in photosensitive skin. It has been proven that UVA radiation leads to damage of the elastic and collagenous fibers of the connective tissue, which causes the skin to age prematurely, and that it is to be regarded as the cause of numerous phototoxic and photoallergic reactions. The damaging influence of UVB radiation can be amplified by UVA radiation.
  • UV radiation can also lead to photochemical reactions, in which case the photochemical reaction products intervene in the skin metabolism.
  • such photochemical reaction products are free-radical compounds, for example hydroxy radicals.
  • Undefined radical photoproducts which are formed in the skin itself, can also show uncontrolled sequelae due to their high reactivity.
  • singlet oxygen a non-radical excited state of the oxygen molecule can occur on UV irradiation, as well as short-lived epoxides and many others. singlet For example, it is distinguished from the normally present triplet oxygen (radical ground state) by increased reactivity. However, there are also excited, reactive (radical) triplet states of the oxygen molecule.
  • UV radiation counts as ionizing radiation. There is thus the risk that ionic species may also be formed on exposure to UV radiation, which in turn may intervene oxidatively in the biochemical processes.
  • antioxidants and / or radical scavengers can be incorporated in the cosmetic or dermatological formulations.
  • vitamin E a substance with known antioxidant effect in sunscreen formulations, yet here again, the effect achieved far below the hoped for.
  • the object of the invention was therefore also to provide cosmetic, dermatological and pharmaceutical active ingredients and preparations as well as sunscreen formulations which are used for the prophylaxis and treatment of photosensitive skin, in particular photodermatoses, preferably PLD.
  • Mainly antioxidants are used as protective substances against spoilage of preparations containing them. Nevertheless, it is known that undesirable oxidation processes can also occur in human and animal skin. Such processes play an essential role in skin aging.
  • antioxidants and radical scavengers are known.
  • the object of the present invention was therefore to find ways that avoid the disadvantages of the prior art.
  • the effect of repairing the damage associated with endogenous, chronological and exogenous skin aging and the prophylaxis should be permanent, sustainable and without the risk of side effects.
  • Creatinine is included in meat extract and meatballs.
  • Creatine is formed in aqueous solution. In the organism it is formed by transamidation of L-arginine to glycine to guanidinoacetic acid and their subsequent methylation by means of S-adenosylmethionine (by guanidinoacetate methyltransferase). Creatine is thought to be an appetizing ingredient in beef and meat extract. Creatine supplementation increases physical performance.
  • Cosmetic or dermatological preparations according to the invention preferably comprise an active ingredient combination of 0.001-50% by weight, particularly preferably 0.01-15% by weight, very particularly preferably 0.1-8% by weight, of creatine and / or creatine derivatives with 0.001-50% by weight, particularly preferably 0.01-15% by weight, very particularly preferably 0.1-8% by weight of creatinine and / or creatinine derivatives, based on the total composition of the preparations. It is advantageous to choose the weight ratio of creatinine to creatine from the range of 50: 1 to 1:50, preferably from 10: 1 to 1:10, particularly preferably from 2: 1 to 1: 2.
  • Preferred derivative is the creatine phosphate, which has the following structure: and which is widespread in fresh muscle where it plays an important role as an energy-storing phosphate (Phosphagen).
  • Phosphagen an energy-storing phosphate
  • creatine phosphate with adenosine 5'-diphosphate under the influence of the enzyme creatine kinase, releases adenosine 5'-triphosphate (ATP) and creatine; in the resting muscle the reverse reaction takes place.
  • ATP adenosine 5'-triphosphate
  • JP2000 / 247866 describes skin cosmetics containing creatine and / or creatinine, which can be used as a cream or as a milky lotion, the preparations in question are said to have excellent skin-care properties.
  • this document could not pave the way for the present invention.
  • WO00 / 33787 describes the use of creatinine as an effective ingredient of deodorants. Even this document could not pave the way to the present invention.
  • EP-A 565 010 describes hair-growing and hair-dyeing preparations containing creatinine phosphate. Even this document could not pave the way to the present invention.
  • an effective way is surprisingly achieved Treatment, but also prophylaxis of deficient, sensitive or hypoactive skin conditions or deficient, sensitive or hypoactive states of skin attachment of premature aging of the skin (eg wrinkles, age spots, telangiectasias) and / or skin appendages, of environmental (smoking, smog , reactive oxygen species, free radicals) and in particular light-induced negative changes of the skin and the skin appendages, of light-induced skin damage from pigmentation disorders, itching, dry skin conditions and horny layer barrier disorders, hair loss and for improved hair growth of inflammatory skin conditions and atopic eczema, seborrheic dermatitis, polymorphic Light dermatosis, psoriasis, vitiligo possible.
  • combination of active ingredients also surprisingly serves to soothe sensitive or irritated skin to stimulate the collagen, hyaluronic acid, elastin synthesis to stimulate intracellular DNA synthesis, especially in deficient or hypoactive skin conditions.
  • to increase the cell renewal and regeneration of the skin to increase the skin's own protective and repair mechanisms (for example for dysfunctional enzymes, DNA, lipids, proteins) for the pre- and post-treatment in topical application of laser and Abschleifnessen z.
  • As the reduction of skin wrinkles and scars serve to counteract the resulting skin irritation and promote the regeneration processes in the injured skin.
  • the active ingredient combination or cosmetic or topical dermatological preparations used according to the invention with an effective content of active ingredient combination used according to the invention for cosmetic or dermatological treatment or prophylaxis. desired skin conditions to use.
  • preparations containing the active compound combinations according to the invention can be used with customary antioxidants.
  • the antioxidants are selected from the group consisting of amino acids (eg glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (eg urotanic acid) and derivatives thereof, peptides such as D, L-camosine, D-carnosine, L- Camosin and its derivatives (eg anserine), carotenoids, carotenes (eg ⁇ -carotene, ⁇ -carotene, lycopene) and their derivatives, lipoic acid and its derivatives (eg dihydrolipoic acid), rothioglucose, propylthiouracil and other thiols (eg thioredoxin, glutathione , Cysteine, cystine, cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl
  • ⁇ -hydroxyfatty acids eg citric acid, lactic acid, malic acid
  • humic acid eg citric acid, lactic acid, malic acid
  • bile acid bile extracts
  • bilirubin biliverdin
  • EDTA EDTA
  • EGTA EGTA and their derivatives
  • unsaturated fatty acids and their derivatives eg ⁇ -linolenic acid, linoleic acid, oleic acid
  • folic acid and its derivatives alaninediacetic acid, flavonoids, polyphenols, catechins, vitamin C and derivatives (eg ascorbyl palmitate, magnesium).
  • benzoic acid rutinic acid and its derivatives
  • the amount of 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 particular 1 - 10 wt .-%, based on the total weight of the preparation.
  • the prophylaxis or the cosmetic or dermatological treatment with the active ingredient combinations used according to the invention or with the cosmetic or topical dermatological preparations with an effective content of the active ingredient combination used according to the invention is carried out in the usual way, 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.
  • the active ingredient combination used according to the invention can be incorporated into customary cosmetic and dermatological preparations which may be in various forms. So they can e.g. 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) or oil-in-water-in-oil (O / W / O), a hydrodispersion or lipodispersion, a gel, a solid stick or even an aerosol.
  • W / O water-in-oil
  • O / W oil-in-water
  • O oil-in-water-in-oil
  • Emulsions according to the invention for the purposes of the present invention are advantageous and contain e.g. Fats, oils, waxes and / or other fatty substances, as well as water and one or more emulsifiers, as are commonly used for such a type of formulation.
  • Medicinal topical compositions according to the present invention usually contain one or more drugs in effective concentration.
  • drugs for the sake of simplicity, reference is made to the clear distinction between cosmetic and medical use and corresponding products to the statutory provisions of the Federal Republic of Germany (for example, Cosmetics Regulation, Food and Medicines Act).
  • cosmetic or topical dermatological compositions according to the present invention depending on their structure, for example, be used as skin protection cream, cleansing milk, sunscreen lotion, nutritional cream, day or night cream, etc. It may be possible and advantageous to use the compositions of the invention as a basis for pharmaceutical formulations use.
  • cosmetic and dermatological preparations which are in the form of a sunscreen agent are also advantageous.
  • these preferably additionally contain at least one UVA filter substance and / or at least one UVB filter substance and / or at least one inorganic pigment.
  • compositions according to the invention can advantageously contain substances which absorb UV radiation in the UVB range, the total amount of the filter substances being, for example, 0.1% by weight to 30% by weight, preferably 0.5% to 10% by weight, in particular 1% to 6 wt .-%, based on the total weight of the preparations.
  • the UVB filters may be oil-soluble or water-soluble.
  • oil-soluble substances are e.g. to call:
  • 4-aminobenzoic acid derivatives preferably (2- ethylhexyl) 4- (dimethylamino) benzoate, 4- (dimethylamino) benzoic acid amyl ester;
  • Esters of cinnamic acid preferably 4-methoxycinnamic acid (2-ethylhexyl) ester, 4-methoxycinnamic acid isopentyl ester;
  • esters of salicylic acid preferably 2-ethylhexyl salicylate, salicylic acid
  • Esters of benzalmalonic acid preferably di (2-ethylhexyl) 4-methoxybenzalmalonate
  • Sulfonic acid derivatives of benzophenones preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts;
  • Sulfonic acid derivatives of the 3-benzylidene camphor e.g. 4- (2-oxo-3-bomylidene-methyl) benzenesulfonic acid, 2-methyl-5- (2-oxo-3-bomylidenemethyl) sulfonic acid and its salts.
  • UVB filters which can be used according to the invention should of course not be limiting.
  • the invention also relates to the combination of a UVA film according to the invention ters with a UVB filter or a cosmetic or dermatological preparation according to the invention which also contains a UVB filter.
  • UVA filters in formulations according to the invention which are customarily contained in cosmetic and / or dermatological preparations.
  • Such filter substances are preferably derivatives of dibenzoylmethane, in particular 1- (4'-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1, 3-dione and 1-phenyl-3- ( 4'-isopropylphenyl) propane-1,3-dione.
  • preparations containing these combinations are the subject of the invention.
  • the same quantities of UVA filter substances which have been mentioned for UVB filter substances can be used.
  • Cosmetic and / or dermatological preparations according to the present invention may also contain inorganic pigments which are commonly used in cosmetics to protect the skin from UV rays. These are oxides of titanium, zinc, iron, zirconium, silicon, manganese, aluminum, cerium and mixtures thereof, as well as modifications in which the oxides are the active agents. Particular preference is given to pigments based on titanium dioxide. The amounts mentioned for the above combinations may be used.
  • the cosmetic and dermatological preparations according to the invention may contain cosmetic active substances, auxiliaries and / or additives such as are customarily used in such preparations, e.g. Antioxidants, preservatives, bactericides, perfumes, foaming inhibitors, colorants, pigments that have coloring properties, thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, fats, oils, waxes or other conventional ingredients of a cosmetic or dermatological formulation such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
  • cosmetic active substances e.g. Antioxidants, preservatives, bactericides, perfumes, foaming inhibitors, colorants, pigments that have coloring properties, thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, fats, oils, waxes or other conventional ingredients of a cosmetic or dermatological formulation such as alcohol
  • the cosmetic or dermatological preparation in the sense of the present invention is a solution or emulsion or dispersion
  • solvent Water or aqueous solutions of oils, such as triglycerides of capric or caprylic acid, but preferably castor oil;
  • Fats, waxes and other natural and synthetic fats 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;
  • 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 ,
  • mixtures of the abovementioned solvents are used.
  • alcoholic solvents water can be another ingredient.
  • the oil phase of the emulsions, oleogels or hydrodispersions or lipodispersions in the context of the present 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 having a chain length of 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 from 3 to 30 carbon atoms. atoms.
  • ester oils can then advantageously be selected from the group consisting of 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 also synthetic, semisynthetic and natural mixtures of such esters, eg Jojoba oil.
  • the oil phase can advantageously be 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 saturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 8 to 24, in particular 12 to 18 carbon atoms.
  • the fatty acid triglycerides can be selected, for example, advantageously from the group of synthetic, semi-synthetic and natural oils, such as olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm oil and the like.
  • any mixtures of such oil and wax components are also advantageous to use in the context of the present invention. It may also be advantageous, if appropriate, to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.
  • the oil phase is advantageously selected from the group consisting of 2-ethylhexyl isostearate, octyldodanol, 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-Ethylhexylisostea- rat, mixtures of C 12-15 -alkyl benzoate and Isotridecylisononanoat and mixtures of C 12 .
  • hydrocarbons paraffin oil, squalane and squalene are to be used advantageously in the context of the present invention.
  • the oil phase can also have 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.
  • cyclomethicone octamethylcyclotetrasiloxane
  • silicone oils are also advantageous for the purposes of the present invention, for example hexamethylcyclotrisiloxane, polydimethylsiloxane, poly (methylphenylsiloxane).
  • the aqueous phase of the preparations according to the invention advantageously contains 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, di ethylene glycol monomethyl or monoethyl ether and analogous products, furthermore low C number alcohols, for example ethanol, isopropanol, 1,2-propanediol, glycerol, and in particular one or more thickening agents, which can be advantageously selected from the group silicon dioxide, aluminum silicates, Polysaccharides or their derivatives, for example
  • Gels used in the present invention usually contain low C number alcohols, e.g. Ethanol, isopropanol, 1, 2-propanediol, glycerol and water or an above-mentioned oil in the presence of a thickener which is preferably silica or an aluminosilicate in oily-alcoholic gels, in aqueous-alcoholic or alcoholic gels, preferably a polyacrylate.
  • a thickener which is preferably silica or an aluminosilicate in oily-alcoholic gels, in aqueous-alcoholic or alcoholic gels, preferably a polyacrylate.
  • Fixed pins contain e.g. natural or synthetic waxes, fatty alcohols or fatty acid esters.
  • Usual base materials which are suitable for use as cosmetic sticks in the context of the present invention are liquid oils (for example paraffin oils, castor oil, isopropyl myristate), semi-solid constituents (eg petrolatum, lanolin), solid constituents (eg beeswax, ceresin and microcrystalline Waxes or ozokerite) and high-melting waxes (eg carnauba wax, candelilla wax)
  • liquid oils for example paraffin oils, castor oil, isopropyl myristate
  • semi-solid constituents eg petrolatum, lanolin
  • solid constituents eg beeswax, ceresin and microcrystalline Waxes or ozokerite
  • high-melting waxes eg carnauba wax, candelilla wax
  • Suitable propellants for sprayable from aerosol containers cosmetic and / or dermatological preparations in the context of the present invention the usual known volatile, liquefied propellants, such as hydrocarbons (propane, butane, isobutane) are suitable, which can be used alone or in mixture with each other. Also, compressed air is advantageous to use.
  • hydrocarbons propane, butane, isobutane
  • compressed air is advantageous to use.
  • propellants which would be useful in the practice of the present invention in the form of aerosol preparations, but which should be avoided due to adverse environmental effects or other concomitant conditions, especially fluorocarbons and chlorofluorocarbons (US Pat. CFC).
  • Cosmetic preparations for the purposes of the present invention may also be present as gels which, in addition to an effective content of the active ingredient according to the invention and solvents used for this purpose, preferably water, are also organic thickeners, e.g. Gum arabic, xanthan gum, sodium alginate, cellulose derivatives, preferably methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose or inorganic thickeners, e.g. For example, aluminum silicates such as bentonites, or a mixture of polyethylene glycol and polyethylene glycol stearate or distearate.
  • the thickening agent is present in the gel e.g. in an amount of between 0.1 and 30% by weight, preferably between 0.5 and 15% by weight.

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Abstract

The invention relates to cosmetic or dermatological preparations containing a combination of active ingredients consisting of creatinine and creatine.

Description

Beiersdorf Aktiengesellschaft Hamburg Beiersdorf Aktiengesellschaft Hamburg
Beschreibungdescription
VERWENDUNG VON KREATININ UND/ODER KREATININDERIVATEN IN KOSMETISCHEN ODER DERMATOLOGISCHEN ZUBEREITUNGENUSE OF CREATININE AND / OR CREATINE DERIVATIVES IN COSMETIC OR DERMATOLOGICAL PREPARATIONS
Die vorliegende Erfindung betrifft die Verwendung von Kombinationen von Kreatinin und/oder Kreatininderivaten mit Kreatin und/oder seinen Derivaten in kosmetischen oder dermatologischen Zubereitungen zur Behandlung und Prophylaxe der Symptome von UV- und oder Ozon- induzierten Hautschäden sowie von entzündlichen und degenerativen Hautzuständen.The present invention relates to the use of combinations of creatinine and / or creatinine derivatives with creatine and / or its derivatives in cosmetic or dermatological preparations for the treatment and prophylaxis of the symptoms of UV and / or ozone-induced skin damage as well as inflammatory and degenerative skin conditions.
Unter kosmetischer Hautpflege ist in erster Linie zu verstehen, daß die natürliche Funktion der Haut als Barriere gegen Umwelteinflüsse (z.B. Schmutz, Chemikalien, Mikroorganismen) und gegen den Verlust von körpereigenen Stoffen (z.B. Wasser, natürliche Fette, Elektrolyte) gestärkt oder wiederhergestellt wird.Cosmetic skin care is understood primarily to strengthen or restore the skin's natural function as a barrier against environmental influences (e.g., dirt, chemicals, microorganisms) and against the loss of endogenous substances (e.g., water, natural fats, electrolytes).
Wird diese Funktion gestört, kann es zu verstärkter Resorption toxischer oder allergener Stoffe oder zum Befall von Mikroorganismen und als Folge zu toxischen oder allergischen Hautreaktionen kommen.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.
Ziel der Hautpflege ist es ferner, den durch tägliche Waschen verursachten Fett- und Wasserverlust der Haut auszugleichen. Dies ist gerade dann wichtig, wenn das natürliche Regenerationsvermögen nicht ausreicht. Außerdem sollen Hautpflegeprodukte vor Umwelteinflüssen, insbesondere vor Sonne und Wind, schützen und die Hautalterung verzögern.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.
Die chronologische Hautalterung wird z.B. durch endogene, genetisch determinierte Faktoren verursacht. In Epidermis und Der is kommt es alterungsbedingt z.B. zu folgenden Strukturschäden und Funktionsstörungen, die auch unter den Begriff „Senile Xerosis" fallen können: a) Trockenheit, Rauhigkeit und Ausbildung von Trockenheitsfältchen, b) Juckreiz und c) verminderte Rückfettung durch Talgdrüsen (z.B. nach Waschen).The chronological skin aging is caused eg by endogenous, genetically determined factors. In the epidermis and der is is due to aging, for example, the following structural damage and dysfunction, which may also fall under the term "senile xerosis": a) dryness, roughness and development of dryness wrinkles; b) itching; and c) reduced rehydration through sebaceous glands (eg after washing).
Exogene Faktoren, wie UV-Licht und chemische Noxen, können kumulativ wirksam sein und z.B. die endogenen Alterungsprozesse beschleunigen bzw. sie ergänzen. In Epidermis und Dermis kommt es insbesondere durch exogene Faktoren z.B. zu folgenden Strukturschäden- und Funktionsstörungen in der Haut, die über Maß und Qualität der Schäden bei chronologischer Alterung hinausgehen:Exogenous factors such as UV light and chemical noxae can be cumulatively effective and e.g. accelerate or supplement endogenous aging processes. In epidermis and dermis, exogenous factors occur, e.g. on the following structural damage and dysfunction in the skin that go beyond the extent and quality of the damage caused by chronological aging:
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).d) Visible vascular dilations (telangiectasias, cuperosis); e) slackness and formation of wrinkles; f) local hyper-, hypo- and false pigmentation (e.g., age spots) and g) increased susceptibility to mechanical stress (e.g., cracking).
Die vorliegende Erfindung betrifft insbesondere Produkte zur Pflege der auf natürliche Weise gealterten Haut, sowie zur Behandlung der Folgeschäden der Lichtalterung, insbesondere der unter a) bis g) aufgeführten Phänomene.The present invention relates in particular to products for the care of naturally aged skin, as well as for the treatment of the consequential damages of photoageing, in particular of the phenomena listed under a) to g).
Produkte zur Pflege gealterter Haut sind an sich bekannt. Sie enthalten z.B. Retinoide (Vitamin A-Säure und/oder deren Derivate) bzw. Vitamin A und/oder dessen Derivate. Ihre Wirkung auf die Strukturschäden ist allerdings umfangsmäßig begrenzt. Daüber hinaus gibt es bei der Produktentwicklung erhebliche Schwierigkeiten, die Wirkstoffe in ausreichendem Maße gegen oxidativen Zerfall zu stabilisieren. Die Verwendung Vitamin A-Säure-haltiger Produkte bedingt darüber hinaus oft starke erythematöse Hautreizungen. Retinoide sind daher nur in geringen Konzentrationen einsetzbar.Products for the care of aged skin are known per se. They contain e.g. 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 acid-containing products often causes severe erythematous skin irritation. Retinoids can therefore only be used in low concentrations.
Insbesondere betrifft die vorliegende Erfindung kosmetische Zubereitungen mit einem wirksamen Schutz vor schädlichen Oxidationsprozessen in der Haut, aber auch zum Schütze kosmetischer Zubereitungen selbst bzw. zum Schütze der Bestandteile kosmetischer Zubereitungen vor schädlichen Oxidationsprozessen.In particular, the present invention relates to cosmetic preparations with effective protection against harmful oxidation processes in the skin, but also to protect cosmetic preparations themselves or to protect the ingredients of cosmetic preparations from harmful oxidation processes.
Die schädigende Wirkung des ultravioletten Teils der Sonnenstrahlung auf die Haut ist allgemein bekannt. Während Strahlen mit einer Wellenlänge, die kleiner als 290 nm ist (der sogenannte UVC-Bereich), von der Ozonschicht in der Erdatmosphäre absorbiert werden, verursachen Strahlen im Bereich zwischen 290 nm und 320 nm, dem sogenannten UVB-Bereich, ein Erythem, einen einfachen Sonnenbrand oder sogar mehr oder weniger starke Verbrennungen.The damaging effect of the ultraviolet part of solar radiation on the skin is well known. While rays with a wavelength less than 290 nm (the so-called UVC range) are absorbed by the ozone layer in the earth's atmosphere, rays in the range between 290 nm and 320 nm, the so-called UVB range, cause erythema simple sunburn or even more or less severe burns.
Als ein Maximum der Erythemwirksamkeit des Sonnenlichtes wird der engere Bereich um 308 nm angegeben.As a maximum of the erythema efficiency of sunlight, the narrower range around 308 nm is given.
Zum Schutz gegen UVB-Strahlung sind zahlreiche Verbindungen bekannt, bei denen es sich um Derivate des 3-Benzylidencamphers, der 4-Aminobenzoesäure, der Zimtsäure, der Salicylsäure, des Benzophenons sowie auch des 2-Phenylbenzimidazols handelt.For protection against UVB radiation, numerous compounds are known, which are derivatives of 3-Benzylidencamphers, 4-aminobenzoic acid, cinnamic acid, salicylic acid, benzophenone and also of 2-phenylbenzimidazole.
Auch für den Bereich zwischen etwa 320 nm und etwa 400 nm, des sogenannten UVA- Bereich, ist es wichtig, Filtersubstanzen zur Verfügung zu haben, da dessen Strahlen Reaktionen bei lichtempfindlicher Haut hervorrufen können. Es ist erwiesen, daß UVA- Strahlung zu einer Schädigung der elastischen und kollagenen Fasern des Bindegewebes führt, was die Haut vorzeitig altern läßt, und daß sie als Ursache zahlreicher phototoxischer und photoallergischer Reaktionen zu sehen ist. Der schädigende Einfluß der UVB-Strahlung kann durch UVA-Strahlung verstärkt werden.Also for the range between about 320 nm and about 400 nm, the so-called UVA range, it is important to have available filter substances, since its rays can cause reactions in photosensitive skin. It has been proven that UVA radiation leads to damage of the elastic and collagenous fibers of the connective tissue, which causes the skin to age prematurely, and that it is to be regarded as the cause of numerous phototoxic and photoallergic reactions. The damaging influence of UVB radiation can be amplified by UVA radiation.
Zum Schutz gegen die Strahlen des UVA-Bereichs werden daher gewisse Derivate des Dibenzoylmethans verwendet, deren Photostabilität (Int. J. Cosm. Science 10, 53 (1988)), nicht in ausreichendem Maße gegeben ist.For protection against the rays of the UVA range, therefore, certain derivatives of dibenzoylmethane are used whose photostability (Int J. Cosm. Science 10, 53 (1988)) is not sufficiently given.
Die UV-Strahlung kann aber auch zu photochemischen Reaktionen führen, wobei dann die photochemischen Reaktionsprodukte in den Hautmetabolismus eingreifen.However, the UV radiation can also lead to photochemical reactions, in which case the photochemical reaction products intervene in the skin metabolism.
Vorwiegend handelt es sich bei solchen photochemischen Reaktionsprodukten um radikalische Verbindungen, beispielsweise Hydroxyradikale. Auch Undefinierte radikalische Photoprodukte, welche in der Haut selbst entstehen, können aufgrund ihrer hohen Reaktivität unkontrollierte Folgereaktionen an den Tag legen. Aber auch Singulettsauerstoff, ein nichtradikalischer angeregter Zustand des Sauerstoffmoleküls kann bei UV- Bestrahlung auftreten, ebenso kurzlebige Epoxide und viele andere. Singulettsauerstoff beispielsweise zeichnet sich gegenüber dem normalerweise vorliegenden Triplettsauerstoff (radikalischer Grundzustand) durch gesteigerte Reaktivität aus. Allerdings existieren auch angeregte, reaktive (radikalische) Triplettzustände des Sauerstoffmoleküls.Predominantly, such photochemical reaction products are free-radical compounds, for example hydroxy radicals. Undefined radical photoproducts, which are formed in the skin itself, can also show uncontrolled sequelae due to their high reactivity. But also singlet oxygen, a non-radical excited state of the oxygen molecule can occur on UV irradiation, as well as short-lived epoxides and many others. singlet For example, it is distinguished from the normally present triplet oxygen (radical ground state) by increased reactivity. However, there are also excited, reactive (radical) triplet states of the oxygen molecule.
Ferner zählt UV-Strahlung zur ionisierenden Strahlung. Es besteht also das Risiko, daß auch ionische Spezies bei UV-Exposition entstehen, welche dann ihrerseits oxidativ in die biochemischen Prozesse einzugreifen vermögen.Furthermore, UV radiation counts as ionizing radiation. There is thus the risk that ionic species may also be formed on exposure to UV radiation, which in turn may intervene oxidatively in the biochemical processes.
Um diesen Reaktionen vorzubeugen, können den kosmetischen bzw. dermatologischen Formulierungen zusätzliche Antioxidantien und/oder Radikalfänger einverleibt werden.In order to prevent these reactions, additional antioxidants and / or radical scavengers can be incorporated in the cosmetic or dermatological formulations.
Es ist bereits vorgeschlagen worden, Vitamin E, eine Substanz mit bekannter antioxida- tiver Wirkung in Lichtschutzformulierungen einzusetzen, dennoch bleibt auch hier die erzielte Wirkung weit hinter der erhofften zurück.It has already been proposed to use vitamin E, a substance with known antioxidant effect in sunscreen formulations, yet here again, the effect achieved far below the hoped for.
Aufgabe der Erfindung war es daher auch, kosmetische, dermatologische und pharmazeutische Wirkstoffe und Zubereitungen sowie Lichtschutzformulierungen zu schaffen, die zur Prophylaxe und Behandlung lichtempfindlicher Haut, insbesondere Photo- dermatosen, bevorzugt PLD dienen.The object of the invention was therefore also to provide cosmetic, dermatological and pharmaceutical active ingredients and preparations as well as sunscreen formulations which are used for the prophylaxis and treatment of photosensitive skin, in particular photodermatoses, preferably PLD.
Weitere Bezeichnungen für die polymorphe Lichtdermatose sind PLD, PLE, Mallorca- Akne und eine Vielzahl von weiteren Bezeichnungen, wie sie in der Literatur (z.B. A. Voelckel et al, Zentralblatt Haut- und Geschlechtskrankheiten (1989), 156, S.2), angegeben sind.Other names for polymorphic light dermatosis are PLD, PLE, Mallorca- acne and a variety of other names, as in the literature (eg, A. Voelckel et al, Zentralblatt skin and venereal diseases (1989), 156, p.2), are indicated.
Hauptsächlich werden Antioxidantien als Schutzsubstanzen gegen den Verderb der sie enthaltenden Zubereitungen verwendet. Dennoch ist bekannt, daß auch in der menschlichen und tierischen Haut unerwünschte Oxidationsprozesse auftreten können. Solche Prozesse spielen eine wesentliche Rolle bei der Hautalterung.Mainly antioxidants are used as protective substances against spoilage of preparations containing them. Nevertheless, it is known that undesirable oxidation processes can also occur in human and animal skin. Such processes play an essential role in skin aging.
Im Aufsatz "Skin Diseases Associated with Oxidative Injury" in "Oxidative Stress in Der- matology", S. 323 ff. (Marcel Decker Inc., New York, Basel, Hong Kong, Herausgeber: Jürgen Fuchs, Frankfurt, und Lester Packer, Berkeley/Californien), werden oxidative Schäden der Haut und ihre näheren Ursachen aufgeführt. Auch aus dem Grunde, solchen Reaktionen vorzubeugen, können kosmetischen oder dermatologischen Formulierungen zusätzlich Antioxidantien und/oder Radikalfänger einverleibt werden.In the article "Skin Diseases Associated with Oxidative Injury" in "Oxidative Stress in Dermatology", p. 323 et seq. (Marcel Decker Inc., New York, Basel, Hong Kong, publishers: Jürgen Fuchs, Frankfurt, and Lester Packer, Berkeley, California), oxidative damage to the skin and its nearer causes are listed. Also, for the purpose of preventing such reactions, antioxidants and / or radical scavengers may additionally be incorporated into cosmetic or dermatological formulations.
Zwar sind einige Antioxidantien und Radikalfänger bekannt. So ist bereits in den US-Patentschriften 4,144,325 und 4,248,861 sowie aus zahlreichen anderen Dokumenten vorgeschlagen worden, Vitamin E, eine Substanz mit bekannter antioxidativer Wirkung in Lichtschutzformulierungen einzusetzen, dennoch bleibt auch hier die erzielte Wirkung weit hinter der erhofften zurück.Although some antioxidants and radical scavengers are known. For example, it has already been proposed in US Pat. Nos. 4,144,325 and 4,248,861 as well as numerous other documents to use vitamin E, a substance with known antioxidant activity in sunscreen formulations, but the effect achieved here also remains far behind the hoped-for effect.
Aufgabe der vorliegenden Erfindung war es somit, Wege zu finden, die die Nachteile des Standes der Technik vermeiden. Insbesondere soll die Wirkung der Behebung der mit der endogenen, chronologischen und exogenen Hautalterung verbundenen Schäden und die Prophylaxe dauerhaft, nachhaltig und ohne das Risiko von Nebenwirkungen sein.The object of the present invention was therefore to find ways that avoid the disadvantages of the prior art. In particular, the effect of repairing the damage associated with endogenous, chronological and exogenous skin aging and the prophylaxis should be permanent, sustainable and without the risk of side effects.
Diesen Übelständen abzuhelfen, war Aufgabe der vorliegenden Erfindung.To remedy these evils was the object of the present invention.
Es hat sich überraschenderweise herausgestellt, daß die Verwendung von Kreatinin und/oder Kreatininderivaten mit Kreatin und/oder seinen Derivaten in kosmetischen oder dermatologischen Zubereitungen zur Behandlung und Prophylaxe der Symptome von UV- und oder Ozon- induzierten Hautschäden sowie von entzündlichen und degenerativen Hautzuständen den Nachteilen das Standes der Technik abhilft und gleichzeitig der Gehalt an Kreatinin die Stabilität von Kreatin in kosmetischen oder dermatologischen Zubereitungen erhöht.It has surprisingly been found that the use of creatinine and / or creatinine derivatives with creatine and / or its derivatives in cosmetic or dermatological preparations for the treatment and prophylaxis of the symptoms of UV- and ozone-induced skin damage as well as inflammatory and degenerative skin conditions the disadvantages The prior art helps and at the same time the content of creatinine increases the stability of creatine in cosmetic or dermatological preparations.
Kreatinin (von grch.: τo κpεotς = „das Fleisch") ist durch folgende Struktur gekennzeichnetCreatinine (from Greek: τo κpεotς = "the flesh") is characterized by the following structure
Figure imgf000006_0001
und entsteht im Organismus durch nichtenzymatische Umwandlung aus Kreatinphosphat gemäß
Figure imgf000007_0001
und wird über die Niere ausgeschieden. Die Menge der Kreatininausscheidung ist der Muskelmasse proportional und für das jeweilige Individuum annähernd konstant. Kreatinin ist in Fleischextrakt und Fleischbrühwürfeln enthalten.
Figure imgf000006_0001
and arises in the organism by nonenzymatic transformation from creatine phosphate according to
Figure imgf000007_0001
and is excreted via the kidney. The amount of creatinine excretion is proportional to muscle mass and approximately constant for the individual. Creatinine is included in meat extract and meatballs.
Kreatin (ebenfalls von grch.: τo pεας = „das Fleisch") zeichnet sich durch folgende Struktur aus:Creatine (also from Greek: τo pεας = "the flesh") is characterized by the following structure:
Figure imgf000007_0002
Figure imgf000007_0002
Es findet sich im Muskelsaft der Wirbeltiere zu 0,05-0,4%, in geringen Mengen auch im Gehirn und Blut. Als Monohydrat stellt es ein farbloses, kristallines Pulver dar. In wäßriger Lösung wird Kreatinin gebildet. Im Organismus entsteht es durch Transamidi- nierung von L-Arginin auf Glycin zu Guanidinoessigsäure und deren anschließende Me- thylierung mittels S-Adenosylmethionin (durch Guanidinoacetat-Methyltransferase). Man hält Kreatin für einen appetitfördernden Bestandteil von Rindfleisch und Fleischextrakt. Kreatinzusatz zur Nahrung verstärkt die körperliche Leistungsfähigkeit .It is found in the muscle juice of vertebrates to 0.05-0.4%, in small quantities in the brain and blood. As a monohydrate, it is a colorless, crystalline powder. Creatine is formed in aqueous solution. In the organism it is formed by transamidation of L-arginine to glycine to guanidinoacetic acid and their subsequent methylation by means of S-adenosylmethionine (by guanidinoacetate methyltransferase). Creatine is thought to be an appetizing ingredient in beef and meat extract. Creatine supplementation increases physical performance.
Bevorzugt enthalten kosmetische oder dermatologische Zubereitungen gemäß der Erfindung eine Wirkstoffkombination aus 0,001 - 50 Gew.-%, besonders bevorzugt 0,01 - 15 Gew.-%, ganz besonders bevorzugt 0,1 - 8 Gew.-% an Kreatin und/oder Kreatinderivaten mit 0,001 - 50 Gew.-%, besonders bevorzugt 0,01 - 15 Gew.-%, ganz besonders bevorzugt 0,1 - 8 Gew.-% an Kreatinin und/oder Kreatininderivaten, bezogen auf die Gesamtzusammensetzung der Zubereitungen. Dabei ist es von Vorteil, das Gewichtsverhältnis von Kreatinin zu Kreatin aus dem Bereich von 50 : 1 bis 1 : 50, bevorzugt von 10 : 1 bis 1 : 10, insbesondere bevorzugt von 2 : 1 bis 1 : 2 zu wählen.Cosmetic or dermatological preparations according to the invention preferably comprise an active ingredient combination of 0.001-50% by weight, particularly preferably 0.01-15% by weight, very particularly preferably 0.1-8% by weight, of creatine and / or creatine derivatives with 0.001-50% by weight, particularly preferably 0.01-15% by weight, very particularly preferably 0.1-8% by weight of creatinine and / or creatinine derivatives, based on the total composition of the preparations. It is advantageous to choose the weight ratio of creatinine to creatine from the range of 50: 1 to 1:50, preferably from 10: 1 to 1:10, particularly preferably from 2: 1 to 1: 2.
Bevorzugtes Derivat ist das Kreatinphosphat, welches folgende Struktur aufweist:
Figure imgf000008_0001
und welches im frischen Muskel verbreitet ist und dort als energiespeicherndes Phosphat (Phosphagen) eine wichtige Rolle spielt. Im arbeitenden Muskel gibt Kreatinphosphat mit Adenosin-5'-diphosphat unter dem Einfluß des Enzyms Kreatin-Kinase Adenosin-5'- triphosphat (ATP) und Kreatin; im ruhenden Muskel läuft die umgekehrte Reaktion ab.
Preferred derivative is the creatine phosphate, which has the following structure:
Figure imgf000008_0001
and which is widespread in fresh muscle where it plays an important role as an energy-storing phosphate (Phosphagen). In working muscle, creatine phosphate with adenosine 5'-diphosphate, under the influence of the enzyme creatine kinase, releases adenosine 5'-triphosphate (ATP) and creatine; in the resting muscle the reverse reaction takes place.
Aber auch Kreatinsulfat, Kreatinacetat, Kreatinascorbat und die an der Carboxylgruppe mit mono- oder polyfunktionalen Alkoholen veresterten Derivate führen zu vorteilhaften Ausführungsformen der Erfindung.But also creatine sulfate, creatine acetate, creatine ascorbate and esterified at the carboxyl group with mono- or polyfunctional alcohols derivatives lead to advantageous embodiments of the invention.
Zwar beschreibt die JP2000/247866 Hautkosmetika mit einem Gehalt an Kreatin und/oder Kreatinin, welche als Creme oder als milchige Lotion verwendet werden können, wobei den betreffenden Zubereitungen vorzügliche hautpflegende Eigenschaften zugeschrieben werden. Diese Schrift konnte jedoch nicht den Weg zur vorliegenden Erfindung ebnen.Although JP2000 / 247866 describes skin cosmetics containing creatine and / or creatinine, which can be used as a cream or as a milky lotion, the preparations in question are said to have excellent skin-care properties. However, this document could not pave the way for the present invention.
Ferner beschreibt die WO00/33787 die Verwendung von Kreatinin als wirksamen Bestandteil von Desodorantien. Auch diese Schrift konnte nicht den Weg zur vorliegenden Erfindung ebnen.Further, WO00 / 33787 describes the use of creatinine as an effective ingredient of deodorants. Even this document could not pave the way to the present invention.
Weiterhin beschreibt die EP-A 565 010 Haarwuchs- und Haarfärbezubereitungen mit einem Gehalt an Kreatininphosphat. Auch diese Schrift konnte nicht den Weg zur vorliegenden Erfindung ebnen.Furthermore, EP-A 565 010 describes hair-growing and hair-dyeing preparations containing creatinine phosphate. Even this document could not pave the way to the present invention.
Schließlich werden in der US-A 4,590,067 und der EP-A-178 602 die Verwendung von Kreatin bzw. Kreatinin zur Herstellung von Zubereitungen mit antiinflammatorischer Wirksamkeit beschrieben. Auch diese Schriften konnten nicht den Weg zur vorliegenden Erfindung ebnen.Finally, US Pat. No. 4,590,067 and EP-A-178 602 describe the use of creatine or creatinine for the preparation of preparations with antiinflammatory activity. These writings could not pave the way to the present invention.
Bei Anwendung der erfindungsgemäß verwendeten Wirkstoffkombination bzw. kosmetischer oder topischer dermatologischer Zubereitungen mit einem wirksamen Gehalt an erfindungsgemäßer Wirkstoffkombination ist in überraschender Weise eine wirksame Behandlung, aber auch eine Prophylaxe von defizitären, sensitiven oder hypoaktiven Hautzuständen oder defizitären, sensitiven oder hypoaktiven Zustände von Hautanhangsgebilden von Erscheinungen vorzeitiger Alterung der Haut (z.B. Falten, Altersflecken, Tele- angiektasien) und/oder der Hautanhangsgebilde, von umweltbedingten (Rauchen, Smog, reaktive Sauerstoffspecies, freie Radikale) und insbesondere lichtbedingten negativen Veränderungen der Haut und der Hautanhangsgebilde, von lichtbedingten Hautschäden von Pigmentierungsstörungen, von Juckreiz, von trockenen Hautzuständen und Hornschichtbarrierestörungen, von Haarausfall und für verbessertes Haarwachstum von entzündlichen Hautzuständen sowie atopischem Ekzem, seborrhoischem Ekzem, polymorpher Lichtdermatose, Psoriasis, Vitiligo möglich. Die erfindungsgemäße Wirkstoffkombination bzw. kosmetische oder topische dermatologische Zubereitungen mit einem wirksamen Gehalt an erfindungsgemäßerWhen using the combination of active substances used according to the invention or cosmetic or topical dermatological preparations having an effective content of the combination of active substances according to the invention, an effective way is surprisingly achieved Treatment, but also prophylaxis of deficient, sensitive or hypoactive skin conditions or deficient, sensitive or hypoactive states of skin attachment of premature aging of the skin (eg wrinkles, age spots, telangiectasias) and / or skin appendages, of environmental (smoking, smog , reactive oxygen species, free radicals) and in particular light-induced negative changes of the skin and the skin appendages, of light-induced skin damage from pigmentation disorders, itching, dry skin conditions and horny layer barrier disorders, hair loss and for improved hair growth of inflammatory skin conditions and atopic eczema, seborrheic dermatitis, polymorphic Light dermatosis, psoriasis, vitiligo possible. The active ingredient combination according to the invention or cosmetic or topical dermatological preparations with an effective content of inventive
Wirkstoffkombination dient aber auch in überraschender Weise zur Beruhigung von empfindlicher oder gereizter Haut zur Stimulation der Kollagen-, Hyaluronsäure-, Elastinsynthese zur Stimulation der intrazellulären DNA-Synthese, insbesondere bei defizitären o- der hypoaktiven Hautzuständen. zur Steigerung der Zellerneuerung und Regeneration der Haut zur Steigerung der hauteigenen Schutz- und Reparaturmechanismen (beispielsweise für dysfunktionelle Enzyme, DNA, Lipide, Proteine) zur Vor- und Nachbehandlung bei topischer Anwendung von Laser- und Abschleifbehandlungen, die z. B. der Reduzierung von Hautfalten und Narben dienen, um den resultierenden Hautreizungen entgegenzuwirken und die Regenerationsprozesse in der verletzten Haut zu fördern.However, combination of active ingredients also surprisingly serves to soothe sensitive or irritated skin to stimulate the collagen, hyaluronic acid, elastin synthesis to stimulate intracellular DNA synthesis, especially in deficient or hypoactive skin conditions. to increase the cell renewal and regeneration of the skin to increase the skin's own protective and repair mechanisms (for example for dysfunctional enzymes, DNA, lipids, proteins) for the pre- and post-treatment in topical application of laser and Abschleifbehandlungen z. As the reduction of skin wrinkles and scars serve to counteract the resulting skin irritation and promote the regeneration processes in the injured skin.
Es ist erfindungsgemäß insbesondere äußerst vorteilhaft, die erfindungsgemäß verwendete Wirkstoffkombination bzw. kosmetische oder topische dermatologische Zubereitungen mit einem wirksamen Gehalt an erfindungsgemäß verwendeter Wirkstoffkombination zur kosmetischen oder dermatologischen Behandlung oder Prophylaxe uner- wünschter Hautzustände zu verwenden.It is particularly advantageous according to the invention, the active ingredient combination or cosmetic or topical dermatological preparations used according to the invention with an effective content of active ingredient combination used according to the invention for cosmetic or dermatological treatment or prophylaxis. desired skin conditions to use.
Erfindungsgemäß können Zubereitungen, welche die erfindungsgemäßen Wirkstoffkombinationen enthalten, übliche Antioxidantien eingesetzt werden.According to the invention, preparations containing the active compound combinations according to the invention can be used with customary antioxidants.
Vorteilhaft werden die Antioxidantien gewählt aus der Gruppe bestehend aus Aminosäuren (z.B. Glycin, Histidin, Tyrosin, Tryptophan) und deren Derivate, Imidazole (z.B. Uro- caninsäure) und deren Derivate, Peptide wie D,L-Camosin, D-Carnosin, L-Camosin und deren Derivate (z.B. Anserin), Carotinoide, Carotine (z.B. α-Carotin, ß-Carotin, Lycopin) und deren Derivate, Liponsäure und deren Derivate (z.B. Dihydroliponsäure), Au- rothioglucose, Propylthiouracil und andere Thiole (z.B. Thioredoxin, Glutathion, Cystein, Cystin, Cystamin und deren Glycosyl-, N-Acetyl-, Methyl-, Ethyl-, Propyl-, Amyl-, Butyl- und Lauryl-, Palmitoyl-, Oleyl-, γ-Linoleyl-, Cholesteryl- und Glycerylester) sowie deren Salze, Dilaurylthiodipropionat, Distearylthiodipropionat, Thiodipropionsäure und deren Derivate (Ester, Ether, Peptide, Lipide, Nukleotide, Nukleoside und Salze) sowie Sulf- oximinverbindungen (z.B. Buthioninsulfoximine, Homocysteinsulfoximin, Buthioninsul- fone, Penta-, Hexa-, Heptathioninsulfoximin) in sehr geringen verträglichen Dosierungen (z.B. pmol bis μmol/kg), ferner (Metall)-Chelatoren (z.B. α-Hydroxyfettsäuren, Palmitin- säure, Phytinsäure, Lactoferrin), α-Hydroxysäuren (z.B. Citronensäure, Milchsäure, Apfelsäure), Huminsäure, Gallensäure, Gallenextrakte, Bilirubin, Biliverdin, EDTA, EGTA und deren Derivate, ungesättigte Fettsäuren und deren Derivate (z.B. γ-Linolensäure, Li- nolsäure, Ölsäure), Folsäure und deren Derivate, Alanindiessigsäure, Flavonoide, Po- lyphenole, Catechine, Vitamin C und Derivate (z.B. Ascorbylpalmitat, Mg-Ascor- bylphosphat, Ascorbylacetat), Tocopherole und Derivate (z.B. Vitamin-E-acetat), sowie Koniferylbenzoat des Benzoeharzes, Rutinsäure und deren Derivate, Ferulasäure und deren Derivate, Butylhydroxytoluol, Butylhydroxyanisol, Nordihydroguajakharzsäure, Nor- dihydroguajaretsäure, Trihydroxybutyrophenon, Harnsäure und deren Derivate, Mannose und deren Derivate, Zink und dessen Derivate (z.B. ZnO, ZnS0 ) Selen und dessen Derivate (z.B. Selenmethionin), Stilbene und deren Derivate (z.B. Stilbenoxid, Trans-Stilben- oxid) und die erfindungsgemäß geeigneten Derivate (Salze, Ester, Ether, Zucker, Nukleotide, Nukleoside, Peptide und Lipide) dieser genannten Wirkstoffe.Advantageously, the antioxidants are selected from the group consisting of amino acids (eg glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (eg urotanic acid) and derivatives thereof, peptides such as D, L-camosine, D-carnosine, L- Camosin and its derivatives (eg anserine), carotenoids, carotenes (eg α-carotene, β-carotene, lycopene) and their derivatives, lipoic acid and its derivatives (eg dihydrolipoic acid), rothioglucose, 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, homocysteinesulfoximine, buthionine sulfones, penta, hexa, heptathionine sulfo ximin) 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 (eg ascorbyl palmitate, magnesium). Ascorbyl phosphate, ascorbyl acetate), tocopherols and derivatives (eg vitamin E acetate), and benzylic resin, benzoic acid, rutinic acid and its derivatives, ferulic acid and its derivatives, butylhydroxytoluene, butylhydroxyanisole, nordihydroguaiacetic acid, norhydrohydroguajaretic acid, trihydroxybutyrophenone, uric acid and derivatives thereof , Mannose and its derivatives, zinc and its derivatives (eg ZnO, ZnS0) selenium and its derivatives (eg selenium methionine), stilbenes and de ren derivatives (for example 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.
Die Menge der Antioxidantien (eine oder mehrere Verbindungen) in den Zubereitungen beträgt vorzugsweise 0,001 bis 30 Gew.-%, besonders bevorzugt 0,05 - 20 Gew.-%, ins- besondere 1 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitung.The amount of 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 particular 1 - 10 wt .-%, based on the total weight of the preparation.
Die Prophylaxe bzw. die kosmetische oder dermatologische Behandlung mit dem erfindungsgemäß verwendeten Wirkstoffkombinationen bzw. mit den kosmetischen oder topischen dermatologischen Zubereitungen mit einem wirksamen Gehalt an erfindungsgemäß verwendeter Wirkstoffkombination erfolgt in der üblichen Weise, und zwar dergestalt, daß der erfindungsgemäß verwendete Wirkstoff bzw. die kosmetischen oder topischen dermatologischen Zubereitungen mit einem wirksamen Gehalt an erfindungsgemäß verwendetem Wirkstoff auf die betroffenen Hautstellen aufgetragen wird.The prophylaxis or the cosmetic or dermatological treatment with the active ingredient combinations used according to the invention or with the cosmetic or topical dermatological preparations with an effective content of the active ingredient combination used according to the invention is carried out in the usual way, 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.
Vorteilhaft kann die erfindungsgemäß verwendete Wirkstoffkombination eingearbeitet werden in übliche kosmetische und dermatologische Zubereitungen, welche in verschiedenen Formen vorliegen können. So können sie z.B. eine Lösung, eine Emulsion vom Typ Wasser-in-öl (W/O) oder vom Typ öl-in-Wasser (O/W), oder eine multiple E- mulsionen, beispielsweise vom Typ Wasser-in-ÖI-in-Wasser (W/O/W) oder öl-in- Wasser-in-ÖI (O/W/O), eine Hydrodispersion oder Lipodispersion, ein Gel, einen festen Stift oder auch ein Aerosol darstellen.Advantageously, the active ingredient combination used according to the invention can be incorporated into customary cosmetic and dermatological preparations which may be in various forms. So they can e.g. 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) or oil-in-water-in-oil (O / W / O), a hydrodispersion or lipodispersion, a gel, a solid stick or even an aerosol.
Erfindungsgemäße Emulsionen im Sinne der vorliegenden Erfindung, z.B. in Form einer Creme, einer Lotion, einer kosmetischen Milch sind vorteilhaft und enthalten z.B. Fette, Öle, Wachse und/oder andere Fettkörper, sowie Wasser und einen oder mehrere Emul- gatoren, wie sie üblicherweise für einen solchen Typ der Formulierung verwendet werden.Emulsions according to the invention for the purposes of the present invention, e.g. in the form of a cream, a lotion, a cosmetic milk are advantageous and contain e.g. Fats, oils, waxes and / or other fatty substances, as well as water and one or more emulsifiers, as are commonly used for such a type of formulation.
Es ist auch möglich und vorteilhaft im Sinne der vorliegenden Erfindung, die erfindungsgemäß verwendete Wirkstoffkombination in wäßrige Systeme bzw. Tensidzubereitungen zur Reinigung der Haut und der Haare einzufügen.It is also possible and advantageous for the purposes of the present invention to incorporate the active ingredient combination used according to the invention in aqueous systems or surfactant preparations for cleaning the skin and hair.
Es ist dem Fachmanne natürlich bekannt, daß anspruchsvolle kosmetische Zusammensetzungen zumeist nicht ohne die üblichen Hilfs- und Zusatzstoffe denkbar sind. Darunter zählen beispielsweise Konsistenzgeber, Füllstoffe, Parfüm, Farbstoffe, Emulgatoren, zusätzliche Wirkstoffe wie Vitamine oder Proteine, Lichtschutzmittel, Stabilisatoren, In- sektenrepellentien, Alkohol, Wasser, Salze, antimikrobiell, proteolytisch oder keratoly- tisch wirksame Substanzen usw. Mutatis mutandis gelten entsprechende Anforderungen an die Formulierung medizinischer Zubereitungen.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 keratolytically active substances, etc. Mutatis mutandis, corresponding requirements apply to the formulation of medical preparations.
Medizinische topische Zusammensetzungen im Sinne der vorliegenden Erfindung enthalten in der Regel ein oder mehrere Medikamente in wirksamer Konzentration. Der Einfachheit halber wird zur sauberen Unterscheidung zwischen kosmetischer und medizinischer Anwendung und entsprechenden Produkten auf die gesetzlichen Bestimmungen der Bundesrepublik Deutschland verwiesen (z.B. Kosmetikverordnung, Lebensmittel- und Arzneimittelgesetz).Medicinal topical compositions according to the present invention usually contain one or more drugs in effective concentration. For the sake of simplicity, reference is made to the clear distinction between cosmetic and medical use and corresponding products to the statutory provisions of the Federal Republic of Germany (for example, Cosmetics Regulation, Food and Medicines Act).
Es ist dabei ebenfalls von Vorteil, die erfindungsgemäß verwendete Wirkstoffkombination als Zusatzstoff zu Zubereitungen zu geben, die bereits andere Wirkstoffe für andere Zwecke enthalten.It is also advantageous to add the active ingredient combination used according to the invention as an additive to preparations which already contain other active ingredients for other purposes.
Entsprechend können kosmetische oder topische dermatologische Zusammensetzungen im Sinne der vorliegenden Erfindung, je nach ihrem Aufbau, beispielsweise verwendet werden als Hautschutzcreme, Reinigungsmilch, Sonnenschutzlotion, Nährcreme, Tagesoder Nachtcreme usw. Es ist gegebenenfalls möglich und vorteilhaft, die erfindungsgemäßen Zusammensetzungen als Grundlage für pharmazeutische Formulierungen zu verwenden.Accordingly, cosmetic or topical dermatological compositions according to the present invention, depending on their structure, for example, be used as skin protection cream, cleansing milk, sunscreen lotion, nutritional cream, day or night cream, etc. It may be possible and advantageous to use the compositions of the invention as a basis for pharmaceutical formulations use.
Günstig sind gegebenenfalls auch solche kosmetischen und dermatologischen Zubereitungen, die in der Form eines Sonnenschutzmittels vorliegen. Vorzugsweise enthalten diese neben der erfindungsgemäß verwendeten Wirkstoffkombination zusätzlich mindestens eine UVA-Filtersubstanz und/oder mindestens eine UVB-Filtersubstanz und/oder mindestens ein anorganisches Pigment.If appropriate, cosmetic and dermatological preparations which are in the form of a sunscreen agent are also advantageous. In addition to the combination of active substances used according to the invention, these preferably additionally contain at least one UVA filter substance and / or at least one UVB filter substance and / or at least one inorganic pigment.
Es ist aber auch vorteilhaft im Sinne der vorliegenden Erfindungen, solche kosmetischen und dermatologischen Zubereitungen zu erstellen, deren hauptsächlicher Zweck nicht der Schutz vor Sonnenlicht ist, die aber dennoch einen Gehalt an UV-Schutzsubstanzen enthalten. So werden beispielsweise in Tagescremes gewöhnlich UV-A- bzw. UV-B- Filtersubstanzen eingearbeitet. Vorteilhaft können erfindungsgemäße Zubereitungen Substanzen enthalten, die UV- Strahlung im UVB-Bereich absorbieren, wobei die Gesamtmenge der Filtersubstanzen z.B. 0,1 Gew.-% bis 30 Gew.-%, vorzugsweise 0,5 bis 10 Gew.-%, insbesondere 1 bis 6 Gew.-% beträgt, bezogen auf das Gesamtgewicht der Zubereitungen.However, it is also advantageous in the context of the present inventions to prepare such cosmetic and dermatological preparations whose main purpose is not the protection from sunlight, but which nevertheless contain a content of UV protective substances. Thus, for example, UV-A or UV-B filter substances are usually incorporated in day creams. Compositions according to the invention can advantageously contain substances which absorb UV radiation in the UVB range, the total amount of the filter substances being, for example, 0.1% by weight to 30% by weight, preferably 0.5% to 10% by weight, in particular 1% to 6 wt .-%, based on the total weight of the preparations.
Die UVB-Filter können öllöslich oder wasserlöslich sein. Als öllösliche Substanzen sind z.B. zu nennen:The UVB filters may be oil-soluble or water-soluble. As oil-soluble substances are e.g. to call:
3-Benzylidencampher und dessen Derivate, z.B. 3-(4-Methylbenzyliden)campher,3-benzylidene camphor and its derivatives, e.g. 3- (4-methylbenzylidene) camphor,
4-Aminobenzoesäure-Derivate, vorzugsweise 4-(Dimethylamino)-benzoesäure(2- ethylhexyl)ester, 4-(Dimethylamino)benzoesäureamylester;4-aminobenzoic acid derivatives, preferably (2- ethylhexyl) 4- (dimethylamino) benzoate, 4- (dimethylamino) benzoic acid amyl ester;
Ester der Zimtsäure, vorzugsweise 4-Methoxyzimtsäure(2-ethylhexyl)ester, 4-Meth- oxyzimtsäureisopentylester;Esters of cinnamic acid, preferably 4-methoxycinnamic acid (2-ethylhexyl) ester, 4-methoxycinnamic acid isopentyl ester;
Ester der Salicylsäure, vorzugsweise Salicylsäure(2-ethylhexyl)ester, Salicylsäure-Esters of salicylic acid, preferably 2-ethylhexyl salicylate, salicylic acid
(4-isopropylbenzyl)ester, Salicylsäurehomomenthylester;(4-isopropylbenzyl) ester, salicylic acid homomenthyl ester;
Derivate des Benzophenons, vorzugsweise 2-Hydroxy-4-methoxybenzophenon, 2-Derivatives of benzophenone, preferably 2-hydroxy-4-methoxybenzophenone, 2-
Hydroxy-4-methoxy-4'-methylbenzophenon, 2,2'-Dihydroxy-4-methoxybenzophe- non;Hydroxy-4-methoxy-4'-methylbenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone;
Ester der Benzalmalonsäure, vorzugsweise 4-Methoxybenzalmalonsäuredi(2-ethyl- hexyl)ester;Esters of benzalmalonic acid, preferably di (2-ethylhexyl) 4-methoxybenzalmalonate;
2,4,6-Thanilino-(p-carbo-2'-ethyl-1 '-hexyloxy)-1 ,3,5-triazin.2,4,6-Thanilino- (p-carbo-2'-ethyl-1'-hexyloxy) -1,3,5-triazine.
Als wasserlösliche Substanzen sind vorteilhaft:As water-soluble substances are advantageous:
2-Phenylbenzimidazol-5-sulfonsäure und deren Salze, z.B. Natrium-, Kalium- oder2-phenylbenzimidazole-5-sulfonic acid and its salts, e.g. Sodium, potassium or
Triethanolammonium-Salze,Triethanolammonium salts,
Sulfonsäure-Derivate von Benzophenonen, vorzugsweise 2-Hydroxy-4-methoxy- benzophenon-5-sulfonsäure und ihre Salze;Sulfonic acid derivatives of benzophenones, preferably 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid and its salts;
Sulfonsäure-Derivate des 3-Benzylidencamphers, wie z.B. 4-(2-Oxo-3-bornyliden- methyl)benzolsulfonsäure, 2-Methyl-5-(2-oxo-3-bornylidenmethyl)sulfonsäure und ihre Salze.Sulfonic acid derivatives of the 3-benzylidene camphor, e.g. 4- (2-oxo-3-bomylidene-methyl) benzenesulfonic acid, 2-methyl-5- (2-oxo-3-bomylidenemethyl) sulfonic acid and its salts.
Die Liste der genannten UVB-Filter, die erfindungsgemäß Verwendung finden können, soll selbstverständlich nicht limitierend sein.The list of said UVB filters which can be used according to the invention should of course not be limiting.
Gegenstand der Erfindung ist auch die Kombination eines erfindungsgemäßen UVA-Fil- ters mit einem UVB-Filter bzw. eine erfindungsgemäßes kosmetische oder dermatologische Zubereitung, welche auch einen UVB-Filter enthält.The invention also relates to the combination of a UVA film according to the invention ters with a UVB filter or a cosmetic or dermatological preparation according to the invention which also contains a UVB filter.
Es kann auch von Vorteil sein, in erfindungsgemäßen Zubereitungen UVA-Filter einzusetzen, die üblicherweise in kosmetischen und/oder dermatologischen Zubereitungen enthalten sind. Bei solchen Filtersubstanzen handelt es sich vorzugsweise um Derivate des Dibenzoylmethans, insbesondere um 1-(4'-tert.Butylphenyl)-3-(4'-methoxyphenyl)- propan-1 ,3-dion und um 1-Phenyl-3-(4'-isopropylphenyl)propan-1 ,3-dion. Auch Zubereitungen, die diese Kombinationen enthalten, sind Gegenstand der Erfindung. Es können die gleichen Mengen an UVA-Filtersubstanzen verwendet werden, welche für UVB- Filtersubstanzen genannt wurden.It may also be advantageous to use UVA filters in formulations according to the invention which are customarily contained in cosmetic and / or dermatological preparations. Such filter substances are preferably derivatives of dibenzoylmethane, in particular 1- (4'-tert-butylphenyl) -3- (4'-methoxyphenyl) propane-1, 3-dione and 1-phenyl-3- ( 4'-isopropylphenyl) propane-1,3-dione. Also preparations containing these combinations are the subject of the invention. The same quantities of UVA filter substances which have been mentioned for UVB filter substances can be used.
Kosmetische und/oder dermatologische Zubereitungen im Sinne der vorliegenden Erfindung können auch anorganische Pigmente enthalten, die üblicherweise in der Kosmetik zum Schütze der Haut vor UV-Strahlen verwendet werden. Dabei handelt es sich um Oxide des Titans, Zinks, Eisens, Zirkoniums, Siliciums, Mangans, Aluminiums, Cers und Mischungen davon, sowie Abwandlungen, bei denen die Oxide die aktiven Agentien sind. Besonders bevorzugt handelt es sich um Pigmente auf der Basis von Titandioxid. Es können die für die vorstehenden Kombinationen genannten Mengen verwendet werden.Cosmetic and / or dermatological preparations according to the present invention may also contain inorganic pigments which are commonly used in cosmetics to protect the skin from UV rays. These are oxides of titanium, zinc, iron, zirconium, silicon, manganese, aluminum, cerium and mixtures thereof, as well as modifications in which the oxides are the active agents. Particular preference is given to pigments based on titanium dioxide. The amounts mentioned for the above combinations may be used.
Die erfindungsgemäßen kosmetischen und dermatologischen Zubereitungen können kosmetische Wirk-, Hilfs- und/oder Zusatzstoffe enthalten, wie sie üblicherweise in solchen Zubereitungen verwendet werden, z.B. Antioxidationsmittel, Konservierungsmittel, Bakterizide, Parfüme, Substanzen zum Verhindern des Schäumens, Farbstoffe, Pigmente, die färbende Wirkung haben, Verdickungsmittel, oberflächenaktive Substanzen, Emulgatoren, weichmachende, anfeuchtende und/oder feuchthaltende Substanzen, Fette, Öle, Wachse oder andere übliche Bestandteile einer kosmetischen oder dermatologischen Formulierung wie Alkohole, Polyole, Polymere, Schaumstabilisatoren, Elek- trolyte, organische Lösungsmittel oder Silikonderivate.The cosmetic and dermatological preparations according to the invention may contain cosmetic active substances, auxiliaries and / or additives such as are customarily used in such preparations, e.g. Antioxidants, preservatives, bactericides, perfumes, foaming inhibitors, colorants, pigments that have coloring properties, thickeners, surface-active substances, emulsifiers, softening, moisturizing and / or moisturizing substances, fats, oils, waxes or other conventional ingredients of a cosmetic or dermatological formulation such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives.
Sofern die kosmetische oder dermatologische Zubereitung im Sinne der vorliegenden Erfindung eine Lösung oder Emulsion oder Dispersion darstellt, können als Lösungsmittel verwendet werden: Wasser oder wäßrige Lösungen öle, wie Triglyceride der Caprin- oder der Caprylsäure, vorzugsweise aber Rizinusöl;If the cosmetic or dermatological preparation in the sense of the present invention is a solution or emulsion or dispersion, it is possible to use as solvent: Water or aqueous solutions of oils, such as triglycerides of capric or caprylic acid, but preferably castor oil;
Fette, Wachse und andere natürliche und synthetische Fettkörper, vorzugsweise Ester von Fettsäuren mit Alkoholen niedriger C-Zahl, z.B. mit Isopropanol, Pro- pylenglykol oder Glycerin, oder Ester von Fettalkoholen mit Alkansäuren niedriger C-Zahl oder mit Fettsäuren;Fats, waxes and other natural and synthetic fats, 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;
Alkohole, Diole oder Polyole niedriger C-Zahl, sowie deren Ether, vorzugsweise Ethanol, Isopropanol, Propylenglykol, Glycerin, Ethylenglykol, Ethylenglykol- monoethyl- oder -monobutylether, Propylenglykolmonomethyl, -monoethyl- oder - monobutylether, Diethylenglykolmonomethyl- oder -monoethylether und analoge Produkte.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 ,
Insbesondere werden Gemische der vorstehend genannten Lösungsmittel verwendet. Bei alkoholischen Lösungsmitteln kann Wasser ein weiterer Bestandteil sein.In particular, mixtures of the abovementioned solvents are used. For alcoholic solvents, water can be another ingredient.
Die Ölphase der Emulsionen, Oleogele bzw. Hydrodispersionen oder Lipodispersionen im Sinne der vorliegenden Erfindung wird vorteilhaft gewählt aus der Gruppe der Ester aus gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkancar- bonsäuren einer Kettenlänge von 3 bis 30 C-Atomen und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C- Atomen, aus der Gruppe der Ester aus aromatischen Carbonsäuren und gesättigten und/oder ungesättigten, verzweigten und/oder unverzweigten Alkoholen einer Kettenlänge von 3 bis 30 C-Atomen. Solche Esteröle können dann vorteilhaft gewählt werden aus der Gruppe Isopropylmyristat, Isopropylpalmitat, Isopropylstearat, Isopropyl- oleat, n-Butylstearat, n-Hexyllaurat, n-Decyloleat, Isooctylstearat, Isononylstearat, Iso- nonylisononanoat, 2-Ethylhexylpalmitat, 2-Ethylhexyllaurat, 2-Hexyldecylstearat, 2-Oc- tyldodecylpalmitat, Oleyloleat, Oleylerucat, Erucyloleat, Erucylerucat sowie synthetische, halbsynthetische und natürliche Gemische solcher Ester, z.B. Jojobaöl.The oil phase of the emulsions, oleogels or hydrodispersions or lipodispersions in the context of the present 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 having a chain length of 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 from 3 to 30 carbon atoms. atoms. Such ester oils can then advantageously be selected from the group consisting of 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 also synthetic, semisynthetic and natural mixtures of such esters, eg Jojoba oil.
Ferner kann die ölphase vorteilhaft gewählt werden aus der Gruppe der verzweigten und unverzweigten Kohlenwasserstoffe und -wachse, der Silkonöle, der Dialkylether, der Gruppe der gesättigten oder ungesättigten, verzweigten oder unverzweigten Alkohole, sowie der Fettsäuretriglyceride, namentlich der Triglycerinester gesättigter und/oder un- gesättigter, verzweigter und/oder unverzweigter Alkancarbonsäuren einer Kettenlänge von 8 bis 24, insbesondere 12 - 18 C-Atomen. Die Fettsäuretriglyceride können beispielsweise vorteilhaft gewählt werden aus der Gruppe der synthetischen, halbsynthetischen und natürlichen Öle, z.B. Olivenöl, Sonnenblumenöl, Sojaöl, Erdnußöl, Rapsöl, Mandelöl, Palmöl, Kokosöl, Palmkemöl und dergleichen mehr.Furthermore, the oil phase can advantageously be 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 saturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 8 to 24, in particular 12 to 18 carbon atoms. The fatty acid triglycerides can be selected, for example, advantageously from the group of synthetic, semi-synthetic and natural oils, such as olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, palm oil, coconut oil, palm oil and the like.
Auch beliebige Abmischungen solcher Öl- und Wachskomponenten sind vorteilhaft im Sinne der vorliegenden Erfindung einzusetzen. Es kann auch gegebenenfalls vorteilhaft sein, Wachse, beispielsweise Cetylpalmitat, als alleinige Lipidkomponente der Ölphase einzusetzen.Any mixtures of such oil and wax components are also advantageous to use in the context of the present invention. It may also be advantageous, if appropriate, to use waxes, for example cetyl palmitate, as the sole lipid component of the oil phase.
Vorteilhaft wird die Ölphase gewählt aus der Gruppe 2-Ethylhexylisostearat, Octyldo- decanol, Isotridecylisononanoat, Isoeicosan, 2-Ethylhexylcocoat, C12-15-Alkylbenzoat, Capryl-Caprinsäure-triglycerid, Dicaprylylether.The oil phase is advantageously selected from the group consisting of 2-ethylhexyl isostearate, octyldodanol, isotridecyl isononanoate, isoeicosane, 2-ethylhexyl cocoate, C 12-15 -alkyl benzoate, caprylic-capric acid triglyceride, dicaprylyl ether.
Besonders vorteilhaft sind Mischungen aus C12-15-Alkybenzoat und 2-Ethylhexylisostea- rat, Mischungen aus C12-15-Alkybenzoat und Isotridecylisononanoat sowie Mischungen aus C12.15-Alkybenzoat, 2-Ethylhexylisostearat und Isotridecylisononanoat.Particularly advantageous are mixtures of C 12-15 -alkyl benzoate and 2-Ethylhexylisostea- rat, mixtures of C 12-15 -alkyl benzoate and Isotridecylisononanoat and mixtures of C 12 . 15- alkyl benzoate, 2-ethylhexyl isostearate and isotridecyl isononanoate.
Von den Kohlenwasserstoffen sind Paraffinöl, Squalan und Squalen vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden.Of the hydrocarbons, paraffin oil, squalane and squalene are to be used advantageously in the context of the present invention.
Vorteilhaft kann die ölphase ferner einen Gehalt an cyclischen oder linearen Silikonölen aufweisen oder vollständig aus solchen ölen bestehen, wobei allerdings bevorzugt wird, außer dem Silikonöl oder den Silikonölen einen zusätzlichen Gehalt an anderen ölpha- senkomponenten zu verwenden.Advantageously, the oil phase can also have 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.
Vorteilhaft wird Cyclomethicon (Octamethylcyclotetrasiloxan) als erfindungsgemäß zu verwendendes Silikonöl eingesetzt. Aber auch andere Silikonöle sind vorteilhaft im Sinne der vorliegenden Erfindung zu verwenden, beispielsweise Hexamethylcyclotrisiloxan, Polydimethylsiloxan, Poly(methylphenylsiloxan).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).
Besonders vorteilhaft sind ferner Mischungen aus Cyclomethicon und Isotridecylisononanoat, aus Cyclomethicon und 2-Ethylhexylisostearat. Die wäßrige Phase der erfindungsgemäßen Zubereitungen enthält gegebenenfalls vorteilhaft Alkohole, Diole oder Polyole niedriger C-Zahl, sowie deren Ether, vorzugsweise Ethanol, Isopropanol, Propylenglykol, Glycerin, Ethylenglykol, Ethylenglykolmonoethyl- oder -monobutylether, Propylenglykolmonomethyl, -monoethyl- oder -monobutylether, Di- ethylenglykolmonomethyl- oder -monoethylether und analoge Produkte, ferner Alkohole niedriger C-Zahl, z.B. Ethanol, Isopropanol, 1 ,2-Propandiol, Glycerin sowie insbesondere ein oder mehrere Verdickungsmittel, welches oder welche vorteilhaft gewählt werden können aus der Gruppe Siliciumdioxid, Aluminiumsilikate, Polysaccharide bzw. deren Derivate, z.B. Hyaluronsäure, Xanthangummi, Hydroxypropylmethylcellulose, besonders vorteilhaft aus der Gruppe der Polyacrylate, bevorzugt ein Polyacrylat aus der Gruppe der sogenannten Carbopole, beispielsweise Carbopole der Typen 980, 981 , 1382, 2984, 5984, jeweils einzeln oder in Kombination.Also particularly advantageous are mixtures of cyclomethicone and isotridecyl isononanoate, cyclomethicone and 2-ethylhexyl isostearate. If appropriate, the aqueous phase of the preparations according to the invention advantageously contains 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, di ethylene glycol monomethyl or monoethyl ether and analogous products, furthermore low C number alcohols, for example ethanol, isopropanol, 1,2-propanediol, glycerol, and in particular one or more thickening agents, which can be advantageously selected from the group silicon dioxide, aluminum silicates, Polysaccharides or their derivatives, for example hyaluronic acid, xanthan gum, hydroxypropylmethylcellulose, particularly advantageously from the group of polyacrylates, preferably a polyacrylate from the group of so-called carbopols, for example Carbopols of types 980, 981, 1382, 2984, 5984, in each case individually or in combination ,
Erfindungsgemäß verwendete Gele enthalten üblicherweise Alkohole niedriger C-Zahl, z.B. Ethanol, Isopropanol, 1 ,2-Propandiol, Glycerin und Wasser bzw. ein vorstehend genanntes Öl in Gegenwart eines Verdickungsmittels, das bei ölig-alkoholischen Gelen vorzugsweise Siliciumdioxid oder ein Aluminiumsilikat, bei wäßrig-alkoholischen oder alkoholischen Gelen vorzugweise ein Polyacrylat ist.Gels used in the present invention usually contain low C number alcohols, e.g. Ethanol, isopropanol, 1, 2-propanediol, glycerol and water or an above-mentioned oil in the presence of a thickener which is preferably silica or an aluminosilicate in oily-alcoholic gels, in aqueous-alcoholic or alcoholic gels, preferably a polyacrylate.
Feste Stifte enthalten z.B. natürliche oder synthetische Wachse, Fettalkohole oder Fettsäureester.Fixed pins contain e.g. natural or synthetic waxes, fatty alcohols or fatty acid esters.
Übliche Grundstoffe, welche für die Verwendung als kosmetische Stifte im Sinne der vorliegenden Erfindung geeignet sind, sind flüssige Öle (z.B. Paraffinöle, Ricinusöl, Iso- propylmyristat), halbfeste Bestandteile (z.B. Vaseline, Lanolin), feste Bestandteile (z.B. Bienenwachs, Ceresin und Mikrokristalline Wachse bzw. Ozokerit) sowie hochschmelzende Wachse (z.B. Camaubawachs, Candelillawachs)Usual base materials which are suitable for use as cosmetic sticks in the context of the present invention are liquid oils (for example paraffin oils, castor oil, isopropyl myristate), semi-solid constituents (eg petrolatum, lanolin), solid constituents (eg beeswax, ceresin and microcrystalline Waxes or ozokerite) and high-melting waxes (eg carnauba wax, candelilla wax)
Als Treibmittel für aus Aerosolbehältern versprühbare kosmetische und/oder dermatologische Zubereitungen im Sinne der vorliegenden Erfindung sind die üblichen bekannten leichtflüchtigen, verflüssigten Treibmittel, beispielsweise Kohlenwasserstoffe (Propan, Butan, Isobutan) geeignet, die allein oder in Mischung miteinander eingesetzt werden können. Auch Druckluft ist vorteilhaft zu verwenden. Natürlich weiß der Fachmann, daß es an sich nichttoxische Treibgase gibt, die grundsätzlich für die Verwirklichung der vorliegenden Erfindung in Form von Aerosolpräparaten geeignet wären, auf die aber dennoch wegen bedenklicher Wirkung auf die Umwelt oder sonstiger Begleitumstände verzichtet werden sollte, insbesondere Fluorkohlenwasserstoffe und Fluorchlorkohlenwasserstoffe (FCKW).Suitable propellants for sprayable from aerosol containers cosmetic and / or dermatological preparations in the context of the present invention, the usual known volatile, liquefied propellants, such as hydrocarbons (propane, butane, isobutane) are suitable, which can be used alone or in mixture with each other. Also, compressed air is advantageous to use. Of course, those skilled in the art will recognize that there are inherently nontoxic propellants which would be useful in the practice of the present invention in the form of aerosol preparations, but which should be avoided due to adverse environmental effects or other concomitant conditions, especially fluorocarbons and chlorofluorocarbons (US Pat. CFC).
Kosmetische Zubereitungen im Sinne der vorliegenden Erfindung können auch als Gele vorliegen, die neben einem wirksamen Gehalt am erfindungsgemäßen Wirkstoff und dafür üblicherweise verwendeten Lösungsmitteln, bevorzugt Wasser, noch organische Ver- dickungsmittel, z.B. Gummiarabikum, Xanthangummi, Natriumalginat, Cellulose- Derivate, vorzugsweise Methylcellulose, Hydroxymethylcellulose, Hydroxyethylcellulose, Hydroxypropylcellulose, Hydroxypropylmethylcellulose oder anorganische Ver- dickungsmittel, z. B. Aluminiumsilikate wie beispielsweise Bentonite, oder ein Gemisch aus Polyethylenglykol und Polyethylenglykolstearat oder -distearat, enthalten. Das Verdi- ckungsmittel ist in dem Gel z.B. in einer Menge zwischen 0,1 und 30 Gew.-%, bevorzugt zwischen 0,5 und 15 Gew.-%, enthalten.Cosmetic preparations for the purposes of the present invention may also be present as gels which, in addition to an effective content of the active ingredient according to the invention and solvents used for this purpose, preferably water, are also organic thickeners, e.g. Gum arabic, xanthan gum, sodium alginate, cellulose derivatives, preferably methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose or inorganic thickeners, e.g. For example, aluminum silicates such as bentonites, or a mixture of polyethylene glycol and polyethylene glycol stearate or distearate. The thickening agent is present in the gel e.g. in an amount of between 0.1 and 30% by weight, preferably between 0.5 and 15% by weight.
Die nachfolgenden Beispiele sollen die vorliegende Erfindung verdeutlichen. The following examples are intended to illustrate the present invention.
1. PIT - Emulsionen1. PIT emulsions
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Figure imgf000025_0002
Figure imgf000026_0001

Claims

Patentansprüche: Claims:
1. Kosmetische oder dermatologische Zubereitungen mit einem Gehalt an einer Wirkstoffkombination aus Kreatinin und /oder dessen Derivaten mit Kreatin und/oder dessen Derivaten.1. Cosmetic or dermatological preparations containing an active ingredient combination of creatinine and / or its derivatives with creatine and / or its derivatives.
2. Verwendung von Zubereitungen nach Anspruch 1 zur Prophylaxe und/oder Behandlung von entzündlichen Hautzuständen und/oder zum Hautschutz bei empfindlich determinierter und trockener Haut (wie z. B. atopisches Ekzem, seborrhoisches Ekzem, polymorphe Lichtdermatose, Psoriasis, Vitiligo, Wundheilungsstörungen, Juckreiz, empfindlicher oder gereizter Haut, lichtbedingte Hautschäden und UV-induzierte Im- munsuppression, Veränderungen der Desquamation, Veränderungen der normalen Fibroblasten- und Keratinozytenproliferation.Veränderungen der normalen Fibroblasten- und Keratinozytendifferenzierung defizitären sensitiven oder hypoaktiven Hautzustände oder defizitären sensitiven oder hypoaktiven Zustände von Hautanhangsgebilden und zur Verringerung der Hautdicke).2. Use of preparations according to claim 1 for the prophylaxis and / or treatment of inflammatory skin conditions and / or for skin protection in sensitive and dry skin (such as atopic eczema, seborrheic eczema, polymorphic light dermatosis, psoriasis, vitiligo, wound healing disorders, itching , sensitive or irritated skin, light-induced skin damage and UV-induced immunosuppression, changes in desquamation, changes in normal fibroblast and keratinocyte proliferation Reduction in skin thickness).
3. Verwendung von Zubereitungen nach Anspruch 1 zur Behandlung und Prophylaxe der Symptome der intrinsischen und/oder extrinsischen Hautalterung sowie zur Behandlung und Prophylaxe der schädlichen Auswirkungen ultravioletter Strahlung auf die Haut, (wie z. B. degenerative Erscheinungen der Haut (wie Altersflecken, Falten, Teleangiektasien, Hautschlaffheit, Elastizitätsverlust, sowie Schwund der epidermalen und dermalen Zellschichten, der Bestandteile des Bindegewebes, der Retezapfen und Kapillargefässe), sogenannte Skin luster und fatigue (Hauterschlaffung und/oder Hautermüdung), gesteigerte Aktivierung proteolytischer Enzyme in der Haut wie z. B. Metalloproteinasen, Störungen der normalen Kollagen-, Hyaluronsäure-, Elastin- und Glykosaminoglycan-Homeostase und der normalen Hautregeneration, Veränderungen der normalen Fibroblasten- und Keratinozytenproliferation.Veränderungen der normalen Fibroblasten- und Keratinozytendifferenzierung, Mangelerscheinungen der intrazellulären DNS-Synthese (insbesondere bei defizitären oder hypoaktiven Hautzuständen), umweltbedingte (durch Rauchen, Smog, reaktive Sauerstoffspecies, freie Radikale und dergleichen verursachte) negative Veränderungen der Haut und/oder der Hautanhangsgebilde).3. Use of preparations according to claim 1 for the treatment and prophylaxis of the symptoms of intrinsic and / or extrinsic skin aging and for the treatment and prophylaxis of the harmful effects of ultraviolet radiation on the skin, (such as, for example, degenerative symptoms of the skin (such as age spots, wrinkles , Telangiectasias, sagging skin, loss of elasticity, as well as loss of the epidermal and dermal cell layers, the components of the connective tissue, the reticles and capillary vessels), so-called skin luster and fatigue (skin slackening and / or skin fatigue), increased activation of proteolytic enzymes in the skin such as e.g. Metalloproteinases, disorders of normal collagen, hyaluronic acid, elastin and glycosaminoglycan homeostasis and normal skin regeneration, changes in normal fibroblast and keratinocyte proliferation. Changes in normal fibroblast and keratinocyte differentiation, deficiency symptoms of intracellular D NS synthesis (especially in deficient or hypoactive skin conditions), environmental (through smoking, smog, reactive oxygen species, free Radicals and the like caused negative changes in the skin and / or the appendages of the skin).
4. Verwendung von Zubereitungen nach Anspruch 1 zur Behandlung und/oder Prophylaxe von Pigmentierungsstörungen.4. Use of preparations according to claim 1 for the treatment and / or prophylaxis of pigmentation disorders.
5. Verwendung von Zubereitungen nach Anspruch 1 zur Steigerung der Ceramidbio- synthese (wie z.B. Veränderungen des Ceramid-, Lipid- und Energiestoffwechsels der gesunden Haut).5. Use of preparations according to claim 1 to increase ceramide biosynthesis (such as changes in the ceramide, lipid and energy metabolism of healthy skin).
6. Verwendung von Zubereitungen nach Anspruch 1 zur Stärkung der Barrierefunktion der Haut (wie z. B. Hornschichtbarrierestörungen, Veränderungen der normalen ü- pidperoxidationen, Veränderungen des transepidermalen Wasserverlustes und des normalen Feuchtigkeitsgehaltes der Haut).6. Use of preparations according to claim 1 for strengthening the barrier function of the skin (such as eg horny layer barrier disorders, changes in normal epidperoxidations, changes in transepidermal water loss and the normal moisture content of the skin).
7. Verwendung von Zubereitungen nach Anspruch 1 zur Behandlung und/oder Prophylaxe von Störungen des normalen Haut-pH-Werts und der Osmolytbalance.7. Use of preparations according to claim 1 for the treatment and / or prophylaxis of disorders of normal skin pH and the osmolytic balance.
8. Verwendung von Zubereitungen nach Anspruch 1 zur Behandlung und/oder Prophylaxe von Abweichungen von der normalen Zell-Zell-Kommunikation in der Haut (z.B. interzelluläre Kommunikationen über Mediatoren und/ oder über mechanische/ physiologische Verbindungen).8. Use of preparations according to claim 1 for the treatment and / or prophylaxis of deviations from normal cell-cell communication in the skin (e.g. intercellular communication via mediators and / or via mechanical / physiological connections).
9. Verwendung von Zubereitungen nach Anspruch 1 zur Behandlung und/oder Prophylaxe von funktioneilen Störungen der Hautanhangsgebilde (z.B. Haarausfall, verbessertes Haarwachstum, seborrhoischer Erscheinungen, fettige Haut, fettiges Haar, Komedonen, aber auch Kopfschuppen).9. Use of preparations according to claim 1 for the treatment and / or prophylaxis of functional disorders of the skin appendages (e.g. hair loss, improved hair growth, seborrheic symptoms, oily skin, oily hair, comedones, but also dandruff).
10. Zubereitungen nach Anspruch 1 und Verwendung nach Anspruch 2 bis 9, dadurch gekennzeichnet, dass der Gehalt an Kreatinin und/oder dessen Derivaten 0,001 - 50 Gew.-% , vorzugsweise 0,1 - 10 Gew.-% sowie der Gehalt an Kreatin und dessen Derivaten 0,001 - 50 Gew.-% , vorzugsweise 0,1 - 10 Gew.-%, bezogen auf das Gesamtgewicht der Zubereitungen, beträgt. 10. Preparations according to claim 1 and use according to claims 2 to 9, characterized in that the content of creatinine and / or its derivatives 0.001 - 50 wt .-%, preferably 0.1 - 10 wt .-% and the content of creatine and its derivatives is 0.001-50% by weight, preferably 0.1-10% by weight, based on the total weight of the preparations.
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