A combination of one or more alkylamidothiazoles, tocopherol, and 3-O-ethyl ascorbic acid, and cosmetic formulations containing such combinations.

Abstract

The present invention relates to the field of cosmetics and to a combination of the active ingredients a) one or more alkylamidothiazoles, b) tocopherol, and c) 3-O-ethyl ascorbic acid, as well as cosmetic formulations containing such combinations. It has been found that the combination of active ingredients of the present invention can prevent or reduce the degradation of alkylamidothiazoles caused by oxidation processes and / or heat and / or UV light in cosmetic formulations containing one or more alkylamidothiazoles.

Description

Technical Field

[0001] The present invention belongs to the field of cosmetics, and specifically relates to a combination of one or more alkylamidothiazoles, tocopherol, and 3-O-ethylascorbic acid, and a cosmetic preparation containing such a combination.

[0002] Background Art Generally, cosmetics not only serve to make people look beautiful and attractive, but also clearly contribute to the improvement of people's self-affirmation and well-being through their effects. Therefore, a variety of cosmetics are used for the daily cleaning and care of human skin. For example, according to German Patent Application Publication No. 102011083259, a cosmetic preparation for human skin care containing alkylamidothiazole is known.

[0003] The alkylamidothiazole used is used in cosmetic preparations to suppress and prevent undesirable pigmentation of the skin. In this way, the skin color of the user can be clearly improved.

[0004] Also, according to German Patent Application Publication No. 102013226711, it is known that alkylamidothiazole can be used in cosmetic preparations or skin preparations for the prevention and treatment of sensitive skin, pruritus, dry skin, and inflammatory symptoms related to human skin. This specification discloses various cosmetic O / W emulsions for application to human skin.

[0005] Furthermore, German Patent Application Publication No. 1٠2013204110 discloses a number of cosmetic preparations for human skin care containing alkylamidothiazole.

[0006] The use of a combination of alkylamidothiazole and one or more cyclodextrins particularly effectively brightens human skin.

[0007] However, the fact that cosmetic formulations containing alkylamidothiazole are well known to those skilled in the art should not be overlooked, as it does not mean that many problems arise when compounding cosmetic or topical formulations.

[0008] For example, a drawback is that newly manufactured cosmetic or topical formulations may discolor during storage. This is more pronounced when the formulation is exposed to light.

[0009] This situation creates significant difficulties for manufacturers of cosmetic formulations, as it necessitates studies on the color stability of those formulations.

[0010] This often requires multiple approaches, and therefore the development costs of cosmetics increase significantly.

[0011] Therefore, it is desirable to provide systems and methods that effectively prevent or minimize the degradation process of cosmetic or topical formulations in order to minimize development costs. The problem of the degradation process of cosmetic or topical formulations also concerns consumers.

[0012] Products are often chosen based on how they look on consumers' skin. However, if a product's white appearance deteriorates during storage, it no longer meets the decisive purchase criteria, which usually leaves consumers confused.

[0013] The color stability of cosmetic or topical formulations can, in principle, be evaluated by a specially trained inspector comparing the color of a newly prepared formulation (within 24 hours of preparation) with the color after the corresponding storage time. However, product discoloration is often very difficult to judge. Therefore, it is advantageous to use a special device called DigiEye for discoloration detection.

[0014] Summary of the Invention Therefore, one object of the present invention was to provide a method for particularly effectively preventing or minimizing the degradation process in cosmetics so as to ensure color stability.

[0015] The purpose is the active ingredient a) One or more alkylamidothiazoles, b) Tocopherol, and c) 3-O-ethyl ascorbic acid This is achieved through a combination of the following:

[0016] Surprisingly, the combination of tocopherol and 3-O-ethyl ascorbic acid works synergistically compared to the substances alone, preventing or reducing the degradation of alkylamidothiazole caused by oxidation processes and / or heat and / or UV light.

[0017] Another embodiment of the present invention is a cosmetic formulation containing such a combination.

[0018] A further embodiment of the present invention is an active ingredient for preventing or reducing the degradation of alkylamidothiazoles caused by oxidation processes and / or heat and / or UV light in a cosmetic formulation containing one or more alkylamidothiazoles. b) Tocopherol, and c) 3-O-ethyl ascorbic acid This is a combination of usage.

[0019] 3-O-ethyl ascorbic acid is a well-known antioxidant and free radical scavenger. It not only protects skin from sun exposure damage but can also repair existing skin damage. 3-O-ethyl ascorbic acid reliably improves collagen synthesis, promotes wrinkle reduction, and also has a skin-brightening effect.

[0020] An advantageous embodiment of the present invention is also a cosmetic or topical formulation containing such a combination of active ingredients, and the use thereof for brightening human skin.

[0021] In order to provide a cosmetic formulation, it is advantageous that the formulation according to the present invention includes a formulation in which the total amount of one or more alkylamidothiazoles is, for example, 0.00001% to 10% by weight, preferably 0.001% to 5% by weight, and particularly 0.005% to 3% by weight, based on the total weight of the formulation.

[0022] To provide a cosmetic formulation, it is advantageous that the formulation according to the present invention includes a formulation in which the total amount of tocopherol is, for example, 0.00001% to 10% by weight, preferably 0.001% to 5% by weight, and particularly 0.005% to 3% by weight, based on the total weight of the formulation.

[0023] In order to provide a cosmetic formulation, it is advantageous that the formulation according to the present invention includes a formulation in which the total amount of 3-O-ethyl ascorbic acid is, for example, 0.00001% to 10% by weight, preferably 0.001% to 5% by weight, and particularly 0.005% to 3% by weight, based on the total weight of the formulation.

[0024] An advantageous alkylamide thiazole in the context of the present invention is a general formula: [ka] (In the formula, R1, R2, X, and Y may be different, partially identical, or completely identical, and may be independent of each other: R1 may mean -C1-C24-alkyl (linear and branched), -C1-C24-alkenyl (linear and branched), -C1-C8-cycloalkyl, -C1-C8-cycloalkyl-alkyl-hydroxy, -C1-C24-alkyl-hydroxy (linear and branched), -C1-C24-alkylamine (linear and branched), -C1-C24-alkylaryl (linear and branched), -C1-C24-alkylaryl-alkyl-hydroxy (linear and branched), -C1-C24-alkylheteroaryl (linear and branched), -C1-C24-alkyl-O-C1-C24-alkyl (linear and branched), -C1-C24-alkyl-morpholino, -C1-C24-alkyl-piperidino, -C1-C24-alkyl-piperazino, -C1-C24-alkyl-piperazino-N-alkyl, R2 may mean H, -C1-C24-alkyl (linear and branched), -C1-C24-alkenyl (linear and branched), -C1-C8-cycloalkyl, -C1-C24-hydroxyalkyl (linear and branched), -C1-C24-alkylaryl (linear and branched), -C1-C24-alkylheteroaryl (linear and branched), X may mean -H, -C1-C24-alkyl (linear and branched), -C1-C24-alkenyl (linear and branched), -C1-C8-cycloalkyl, (optionally mono- or polysubstituted with -OH, -F, -Cl, -Br, -I, -OMe, -NH2, -CN) -C1-C24-aryl, (optionally mono- or polysubstituted with -OH, -F, -Cl, -Br, -I, -OMe, -NH2, -CN) -C1-C24-heteroaryl, -C1-C24-alkylaryl (linear and branched), -C1-C24-alkylheteroaryl (linear and branched), (optionally mono- or polysubstituted with -OH, -F, -Cl, -Br, -I, -OMe, -NH2, -CN) -aryl, -phenyl, -2,4-dihydroxyphenyl, -2,3-dihydroxyphenyl, -2,4-dimethoxyphenyl, -2,3-dimethoxyphenyl, Y may represent H, -C1-C24-alkyl (linear and branched), -C1-C24-alkenyl (linear and branched), -C1-C8-cycloalkyl, -C1-C24-aryl, -C1-C24-heteroaryl, -C1-C24-alkylaryl (linear and branched), -C1-C24-alkylheteroaryl (linear and branched), -aryl, -phenyl, -2,4-dihydroxyphenyl, -2,3-dihydroxyphenyl, -2,4-dimethoxyphenyl, -2,3-dimethoxyphenyl, -COO-alkyl, -COO-alkenyl, -COO-cycloalkyl, -COO-aryl, -COO-heteroaryl, and X and Y may optionally also be fused aromatics, where X and Y can form an aromatic or aliphatic monocyclic or polycyclic system of single or hetero rings having up to n ring-forming atoms with each other, where the number n can take values from 5 to 8, and each ring system may optionally be substituted with up to n-1 alkyl groups, hydroxyl groups, carboxyl groups, amino groups, nitrile functional groups, sulfur-containing substituents, ester groups and / or ether groups) is a substance of

[0025] The thiazole may be in the form of either the free base or a salt, for example in the form of fluoride, chloride, bromide, iodide, sulfate, carbonate, ascorbate, acetate or phosphate. In particular, it may be in the form of a halogen salt, for example chloride and bromide.

[0026] Furthermore, the present invention is advantageously realized in a cosmetic preparation or a skin preparation having an effective content of one or more of the aforementioned alkylamidothiazoles.

[0027] Also according to the present invention, the aforementioned alkylamidothiazole is used for the treatment and / or prevention of unwanted skin pigmentation.

[0028] Here, the treatment and / or prevention of unwanted skin pigmentation is possible in both the fields of cosmetics and pharmaceuticals.

[0029] In this context, medicinal (or topical) treatments are understood to be primarily for skin in diseased conditions, while the cosmetic treatment and / or prevention of undesirable skin pigmentation primarily concerns healthy skin.

[0030] Advantageously, X is selected from the group of substituted phenyl compounds, in which case the substituent (Z) can be selected from the group of -H, -OH, -F, -Cl, -Br, -I, -OMe, -NH2, -CN, and acetyl, and may be the same or different. [ka]

[0031] Particularly advantageous is that X is selected from the group of phenyl groups substituted with one or more hydroxyl groups, in which case the substituent (Z) can be selected from the group of -H, -OH, -F, -Cl, -Br, -I, -OMe, -NH2, -CN, and acetyl, as shown in the following general structure [ka] (In the formula, Y, R1, and R2 may have the same definitions as above.) It is preferable.

[0032] In particular, in advantageous compounds, X is [ka] And, Y is H, R1 is -C1~C24-alkyl (linear and branched), -C1~C24-alkenyl (linear and branched), -C1~C8-cycloalkyl, -C1~C8-cycloalkyl-alkylhydroxy, -C1~C24-alkylhydroxy (linear and branched), -C1~C24-alkylamine (linear and branched), -C1~C24-alkylaryl (linear and branched), -C1~C24 These are alkylaryl-alkyl-hydroxy (linear and branched), -C1~C24-alkylheteroaryl (linear and branched), -C1~C24-alkyl-O-C1~C24-alkyl (linear and branched), -C1~C24-alkyl-morpholino, -C1~C24-alkyl-piperidino, -C1~C24-alkyl-piperazino, and -C1~C24-alkyl-piperazino-N-alkyl. R2 is H, -C1~C24-alkyl (linear and branched), and Z is -H, -OH, -F, -Cl, -Br, -I, -OMe, -NH2, -CN, or acetyl.

[0033] Of particular preference are compounds whose images are included in the "original document". X is [ka] And, Y is H, R1 is -C1~C24-alkyl (linear and branched), -C1~C24-alkenyl (linear and branched), -C1~C8-cycloalkyl, -C1~C8-cycloalkyl-alkylhydroxy, -C1~C24-alkylhydroxy (linear and branched), -C1~C24-alkylamine (linear and branched), -C1~C24-alkylaryl (linear and branched), -C1~C24 These are alkyl-aryl-alkyl-hydroxy (linear and branched), -C1~C24-alkylheteroaryl (linear and branched), -C1~C24-alkyl-O-C1~C24-alkyl (linear and branched), -C1~C24-alkyl-morpholino, -C1~C24-alkyl-piperidino, -C1~C24-alkyl-piperazino, and -C1~C24-alkyl-piperazino-N-alkyl. R2 is H.

[0034] The most preferred compound within the scope of the present invention is: [ka] [ka] [ka] It is a compound of [the compound].

[0035] Cosmetic or topical formulations containing alkylamidothiazole, and their use for the treatment and / or prevention of undesirable skin pigmentation, are also advantageous embodiments of the present invention.

[0036] Such cosmetic or topical preparations are particularly advantageous if they contain one or more alkylamidothiazoles used in the present invention in an amount of 0.000001% to 10% by weight, especially 0.0001% to 3% by weight, and even more especially 0.001% to 1% by weight, based on the total weight of the preparation.

[0037] The cosmetic and topical formulations according to the present invention can take various forms. Therefore, they may be, for example, solutions, anhydrous preparations, water-in-oil (W / O) or oil-in-water (O / W) emulsions or microemulsions, multilayer emulsions, such as water-in-oil-in-water (W / O / W) emulsions, gels, solid sticks, balms, or other aerosols. According to the present invention, it is also advantageous to administer the substances and / or derivatives used herein in encapsulated forms, such as encapsulated in a collagen matrix and other conventional encapsulating materials, such as cellulose, gelatin, or liposomes.

[0038] In the context of the present invention, it is also possible and advantageous to add the substances and / or derivatives used in the present invention to aqueous or surfactant formulations for cleansing skin and hair.

[0039] The cosmetic and skin formulations according to the present invention may contain cosmetic additives conventionally used in such formulations, such as preservatives, bactericides, fragrances, anti-foaming substances, dyes, pigments having coloring effects, thickeners, surfactants, emulsifiers, softening, wetting and / or moisturizing substances, fats, oils, waxes, or other conventional components of cosmetic or skin formulations, such as alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents, or silicone derivatives.

[0040] The lipid phase can be advantageously selected from the group consisting of: mineral oils, mineral wax oils such as capric or caprylic triglycerides, and natural oils such as castor oil; fats, waxes, and other natural and synthetic fats, preferably esters of fatty acids with low-carbon alcohols such as isopropanol, propylene glycol, or glycerol, or esters of fatty alcohols with low-carbon alkanic acids, or esters of fatty alcohols with fatty acids; alkyl benzoates; silicone oils, such as dimethylpolysiloxane, diethylpolysiloxane, diphenylpolysiloxane, and mixtures thereof.

[0041] In the context of the present invention, the oil phase of an emulsion, oleogel, or aqueous or oil dispersion is advantageously selected from the group of esters of aromatic carboxylic acids and esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids having a chain length of 3 to 30 carbon atoms, and esters of saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of 3 to 30 carbon atoms. Such ester oils can be advantageously 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-octyldodecyl palmitate, oleyl oleate, oleyl erucate, erucyl oleate, and synthetic, semi-synthetic, and natural mixtures of these esters, such as jojoba oil.

[0042] The aqueous phase of the preparation according to the present invention optionally and advantageously comprises a humectant, such as propylene glycol, panthenol, or hyaluronic acid, and one or more thickeners, particularly advantageously selected from the group consisting of silicon dioxide, aluminum silicate, and hydroxypropyl methylcellulose, and especially advantageously polyacrylate, such as carbopol grade 980, either individually or in combination in any case.

[0043] In particular, a mixture of the above solvents is used. In the case of an alcoholic solvent, water may be an additional component.

[0044] The emulsion according to the present invention is advantageous and comprises, for example, certain fats, oils, waxes and other fatty bodies, as well as water and emulsifiers commonly used for such types of formulations.

[0045] The gel according to the present invention typically contains a low-carbon alcohol, such as ethanol, propylene glycol, and water or the aforementioned oil in the presence of a thickening agent, the thickening agent of which is preferably silicon dioxide or aluminum silicate in the case of an oily alcoholic gel, and preferably polyacrylate in the case of an aqueous alcoholic gel or an alcoholic gel.

[0046] Suitable propellants for the preparations according to the present invention, which can be sprayed from an aerosol container, are typically known, easily volatile liquefied propellants, such as hydrocarbons (propane, butane, isobutane), which can be used alone or in mixtures of each other. Compressed air can also be used advantageously.

[0047] To provide cosmetic formulations that protect hair and / or skin from UV light in the entire range, the formulations according to the present invention are more advantageous in that they contain a substance that absorbs UV light in the UVB range, and the total amount of such filtering substance is advantageous in that it is, for example, 0.1% to 30% by weight, preferably 0.5% to 10% by weight, and particularly 1.0% to 6.0% by weight, based on the total weight of the formulation. These can also function as sunscreens for hair or skin.

[0048] Furthermore, the formulation according to the present invention may advantageously further contain a substance that masks the unpleasant odor inherent in the remaining raw materials used, and in order to provide a cosmetic formulation, the total amount of fragrance components is, for example, 0.001% to 30% by weight, preferably 0.05% to 10% by weight, and particularly 0.1% to 5.0% by weight, based on the total weight of the formulation.

[0049] Examples The following examples are intended to illustrate the invention without limiting it. Unless otherwise specified, all quantities, fractions and percentages are based on the weight and total volume of the preparation, or on the total weight.

[0050] Combination example Table 1

[0051] Table 2

Claims

1. The active ingredient a) One or more alkylamidothiazoles, b) Tocopherol, and c) 3-O-ethyl ascorbic acid A combination.

2. A cosmetic formulation containing the combination described in claim 1.

3. In a cosmetic formulation containing one or more alkylamidothiazoles, the active ingredient is for preventing or reducing the degradation of alkylamidothiazoles caused by oxidation processes and / or heat and / or UV light. b) Tocopherol, and c) 3-O-ethyl ascorbic acid Use in combination.

4. The cosmetic preparation according to claim 2, or the use according to claim 3, characterized in that the total amount of one or more alkylamidothiazoles is 0.00001% to 10% by weight, preferably 0.001% to 5% by weight, and particularly 0.005% to 3% by weight, based on the total weight of the preparation.

5. The cosmetic preparation according to claim 2 or 4, characterized in that the total amount of tocopherol is 0.00001% to 10% by weight, preferably 0.001% to 5% by weight, and particularly 0.005% to 3% by weight, based on the total weight of the preparation.

6. The cosmetic preparation according to claim 2, 4, or 5, characterized in that the total amount of 3-O-ethyl ascorbic acid is, for example, 0.00001% to 10% by weight, preferably 0.001% to 5% by weight, and particularly 0.005% to 3% by weight, based on the total weight of the preparation.

7. The one or more alkylamidothiazoles mentioned above 【Chemistry 1-1】 【Chemistry 1-2】 [Chemistry 1-3] A combination of active ingredients according to claim 1, characterized by being selected from the group consisting of the following substances, or a cosmetic formulation according to claim 2, 4, 5, or 6.

Images