JPH10120542A - Use of tocopheryl feruliate for making skin less brown and preventing sunburn, in particular that caused by ultraviolet ray - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a method for producing a cosmetic or dermatological product which can prevent or treat undesirable pigmentation by use of tocopheryl ferulate. SOLUTION: This method uses tecopheryl ferulitate, preferably DL-alpha- tocopheryl ferulate, an active ingredient which can prevent or treat undesirable pigmentation, particularly effective against exasperated local pigmentation, and abnormal pigmentation, such as mole and freckles, and a sunburn caused by ultraviolet ray. Therefore, it is possible to produce a cosmetic or dermatological product for local use by incorporating 0.01 to 10wt.% of tecopheryl ferulate as its active ingredient. The cosmetic or dermatological product is also particularly suited for treatment of a senile mole.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

FIELD OF THE INVENTION The present invention relates to cosmetic and topical dermatological skin fading or to the prevention of sunburn of the skin, in particular the sunburn caused by UV radiation. The use of the active ingredients provided.

[0002] In a preferred embodiment, the present invention is directed to the prevention and treatment of cosmetic or dermatological changes in the skin, such as, for example, undesired pigmentation, for example local hyperpigmentation and hyperpigmentation (eg moles, freckles). Cosmetic and dermatological preparations for the discoloration of large areas of pigmented skin, purely cosmetic, for the purpose of, or for perfectly adapting to the skin type of the individual.

[0003]

BACKGROUND OF THE INVENTION Melanocytes cause pigmentation of the skin and, depending on the type of skin, as pigment-forming cells, which exist individually or in groups of various sizes,
Stratum basal layer of the lowest epidermal layer along the basal cells (Stratum
basale). Melanocytes contain, as characteristic organelles, melanosomes that form melanin in large amounts when stimulated by UV light.
This is transported into the keratinocytes, resulting in a more or less brownish to brown skin color.

[0004] Melanin is formed as the last step in the oxidation process, in which tyrosine, under the action of the enzyme tyrosine-degrading enzyme, 3,4-dihydroxyphenylalanine (dopa), dopaquinone, leucodopachrome, dopachrome, 5,6. -Finally converted to melanin via dihydroxyindole and indole-5,6-quinone.

[0005] The problems associated with hyperpigmentation of the skin have many different causes and are incidental phenomena of many biological processes, such as UV light [eg freckles, ( Epheli
des )], genetic tendency, healing or scarring of the skin and aging of the skin [eg senile moles ( Lentigines senile
s )) Abnormal skin pigmentation during period.

[0006] Active ingredients and preparations which counteract skin pigmentation are known. On the one hand, they show their effect only after a few weeks of administration, and on the other hand, their excessively long-term administration is dangerous for toxicological reasons, but practical use is essentially , Hydroquinone-based preparations. Although it has cosmetic and dermatological disadvantages, suppression of tyrosine-degrading enzymes by substances such as kojic acid, ascorbic acid and azelaic acid and their derivatives is also common.

[0007]

The object of the present invention was to solve these problems.

[0008]

DETAILED DESCRIPTION OF THE INVENTION Ferulic acid (4-hydroxy-3-methoxycinnamic acid, caffeic acid 3-methyl ether) is known to have antioxidant properties. It is a structural formula

[0009]

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It has the following features. It is very common in plants and, for example, the names of the Apiaceae plants Ferula asafoetida and Ferula
It is present in tubers, cereals and rubber resins of naltex ( Ferula nartex ). Form E is a colorless crystalline solid under normal conditions, and form Z is a yellowish oil under normal conditions.

Tocopherols and their esters with vitamin E activity are derived from the basic substance tocol [2-methyl-2- (4,8,12-trimethyltridecyl) chroman-6-ol] and have the following structure:

[0012]

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[0013]

K is either H or an acyl group;
R, R 'and R "are independently H or a methyl group, for example: R = R' = R" = K = H: tocol R = R '= R "= methyl, K = H: α-tocopherol R = R ″ = methyl, R ′ = K = H: β-tocopherol R ′ = R ″ = methyl, R = K = H: γ-tocopherol R ″ = methyl, R = R ′ = K = H: δ− Tocopherol R = methyl, R ′ = R ″ = K = H: ε-tocopherol R = R ′ = methyl, R ″ = K = H: ζ-tocopherol R ′ = methyl, R = R ″ = K = H: η -Tocopherol.

[0015] Most frequently and most importantly in nature, α-tocopherol has the 2R, 4'R, 8'R configuration. It is sometimes referred to as RRR-α-tocopherol.

Tocopheryl ferulate, depending on the isomeric form of ferulic acid or the various tocopherol bases,
Structural formula

[0017]

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Wherein R, R ′ and R ″ are as defined above.

The method for producing tocopheryl ferulate and its properties are described in Japanese Ichimaru Pharmaceutical Company (Ichimaru Pharcos K).
K), JP-A-60-222476, and
It is described in the related JP-A-86-052151. In particular, reference is made to the above-mentioned references for the use of tocopheryl ferulate in cosmetics and for its properties as antioxidants.

Conversely, the use of tocopheryl ferulate for the undesirable pigmentation of the skin or the use of cosmetic or dermatological preparations containing an effective amount of tocopheryl ferulate for the unwanted pigmentation of the skin has It is surprising to rectify the disadvantages of the art and has been foreseen by those skilled in the art.

As a result, tocopheryl ferulate, whether it is a single substance, or a mixture of isomers, or a mixture of different tocopheryl ferulates, is collectively referred to as "the tocopheryl used according to the present invention. Active ingredients, which are also referred to as "active ingredients", are excellent active ingredients in both a preventive and therapeutic sense against unwanted pigmentation, especially local hyperpigmentation, and against tanning caused by UV light. Turned out to be.

Preferred α-tocopheryl ferulate [synonym: vitamin E ferulate, chemical name (4 "-hydroxy-3" -methoxycinnamic acid) for the purpose of the present invention
2,5,7,8-tetramethyl-2- (4 ′, 8 ′, 1
2′-trimethyltridecyl) -6-chromanyl] is
Previously 17175-Chemical Abstracts as Registry Number 21290-29-9.
56-3.

[0023] DL-α-tocopheryl ferulate is particularly preferred. Isomers of the E and Z configurations of the ferulic acid group are equally effective.

JP-A-60-222476 and the related JP-A-86-052151 disclose specific synthesis methods for all possible tocopheryl ferulates which can be advantageously used for the purposes of the present invention. Although not described, those skilled in the art will be able to use the information in these specifications and furthermore, with the knowledge of the general expert, for example, to determine the starting tocopherols published in the specification We know how to obtain the desired individual products by substituting them with starting tocopherols which may not have been published and otherwise by carrying out similar procedures.

Depending on the configuration of the ferulic acid groups, preferred materials according to the invention have the structure, given the configuration of the asymmetric center on the tocopheryl group,

[0026]

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Has the following.

According to the invention, the content of active ingredient used according to the invention in cosmetic or topical dermatological preparations is from 0.01 to 10% by weight, preferably from 0.1 to 10% by weight, of the total weight of the preparation. To 5% by weight, especially 0.2 to 2.0% by weight.

Surprisingly, it has been found that the active ingredients used according to the invention achieve the purpose for which the invention is aimed. By using a cosmetic or topical dermatological preparation containing an active ingredient used according to the invention or an active amount of an active ingredient used according to the invention, an effective prevention against unwanted pigmentation is achieved. For example, unwanted pigmentation due to the effects of UV light can be prevented. However, it is also possible to use the active ingredients used according to the invention, or cosmetic or topical dermatological preparations containing active amounts of the active ingredients used according to the invention, for undesired skin pigmentation, such as senile moles, Use according to the invention for cosmetic or dermatological treatments is also particularly suitable.

Prevention by a cosmetic or topical dermatological preparation containing the active ingredient used according to the invention, or an active amount of the active ingredient used according to the invention, or cosmetic or dermatological treatment comprises: The active ingredient used according to the invention, or a cosmetic or topical dermatological preparation containing an active amount of the active ingredient used according to the invention, is administered in the usual manner by administering it to the site of disease on the skin Is done.

The active ingredients used according to the invention can be conveniently incorporated into conventional cosmetic and dermatological preparations, which can be in various forms.
They are, for example, solutions, water-in-oil (W / O) or oil-in-water (O / W) emulsions, or double emulsions, such as water-in-oil-in-water (W / O / W) or oil-in-oil ( It can be an emulsion of the type (O / W / O), a hydrodispersion or a lipid dispersion, a gel, a solid stick or an aerosol.

Emulsions according to the invention in the context of the invention, for example in the form of creams, lotions or cosmetic emulsions, are advantageous and include, for example, fats, oils, waxes and / or other fatty substances, and water and Contains one or more emulsifiers, as traditionally used for the preparation of

For the purposes of the present invention, it is also possible and advantageous to add the active ingredients used according to the invention to aqueous systems or surfactant preparations for cleansing the skin and hair. .

The person skilled in the art, of course, knows that demanding cosmetic compositions are often not conceivable without the usual auxiliaries and additives. These are, for example, consistency regulators, fillers, fragrances, dyes, emulsifiers,
Contains additional active ingredients such as vitamins or proteins, light and other stabilizers, repellents, alcohol, water, salts, antibacterial, proteolytic or keratolytic substances, and the like.

The corresponding requirements for the preparation of pharmaceutical preparations apply mutatis mutandis.

[0036] Topical pharmaceutical compositions within the scope of the present invention generally contain effective concentrations of one or more pharmaceutical agents.
For the sake of simplicity, reference is made to the legislation of the Federal Republic of Germany (eg cosmetics regulations, food and pharmaceutical regulations) in order to clearly distinguish between cosmetics and pharmaceutical uses and the corresponding products.

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

Accordingly, cosmetic or topical dermatological compositions within the scope of the present invention, depending on their composition, include, for example,
It can be used as a cream for protecting the skin, an emulsion for cleansing, a sunscreen lotion, a nourishing cream, a daytime or nighttime cream, and the like. If desired, the compositions according to the invention can be advantageously used as a basis for pharmaceutical preparations.

If appropriate, cosmetic and dermatological preparations which are in the form of sunscreens are also preferred. In addition to the active ingredients used according to the invention, they also preferably contain at least one UVA filter substance and / or at least one UVB filter substance and / or at least one inorganic pigment.

However, it is also advantageous for the purposes of the present invention to provide cosmetic and dermatological preparations whose primary purpose is not protection against the sun, but which still contain anti-UV substances. Thus, for example, UV-A and UV-B filter substances are usually incorporated into day creams.

The preparations according to the invention are advantageously prepared with UVB
Can contain substances that absorb UV light in the area,
The total amount of the filter substance is, for example, from 0.1% to 30% by weight of the total weight of the preparation, preferably from 0.5 to 1%.
0% by weight, in particular 1 to 6% by weight.

The UVB filter may be oil-soluble or water-soluble. Examples of oil-soluble substances are: 3-benzylidene camphor and its derivatives, for example 3- (4-methylbenzylidene) camphor; 4-aminobenzoic acid derivatives, preferably 2-ethylhexyl 4- (dimethylamino) benzoate, 4 -Amyl (dimethylamino) benzoate;-esters of cinnamic acid, preferably 2-ethylhexyl 4-methoxycinnamate, isopentyl 4-methoxycinnamate;-esters of salicylic acid, preferably 2- salicylic acid.
Ethylhexyl, 4-isopropylbenzyl salicylate, homomenthyl salicylate; derivatives of benzophenone, preferably 2-hydroxy-4-methoxybenzophenone, 2-hydroxy-4
-Methoxy-4'-methylbenzophenone, 2,2'-
Dihydroxy-4-methoxybenzophenone;-an ester of benzalmalonic acid, preferably di (2-ethylhexyl) 4-methoxybenzalmalonate;-2,4,6-trianilino- (p-carbo-2'-
Ethyl-1′-hexyloxy) -1,3,5-triazine.

The water-soluble substances are advantageously: 2-phenylbenzimidazole-5-sulfonic acid and its salts, such as sodium, potassium or triethanolammonium salts, sulfonic acid derivatives of benzophenone, preferably 2
-Hydroxy-4-methoxybenzophenone-5-sulfonic acid and salts thereof; -sulfonic acid derivative of 3-benzylidenecamphor,
For example, 4- (2-oxo-3-bornylidenemethyl)
Benzenesulfonic acid, 2-methyl-5- (2-oxo-
3-bornylidenemethyl) sulfonic acid and its salts.

The above list of UVB filters which can be used according to the invention is of course not intended to be limited to them.

The present invention also relates to the combination of a UVA filter according to the invention with a UVB filter or with a cosmetic or dermatological preparation according to the invention which also contains a UVB filter.

In the preparations according to the invention, it may also be advantageous to use UVA filters, which are usually present 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 also the subject matter of the present invention. The same amount of UVA filter material as given for the UVB filter material can be used.

The cosmetic and / or dermatological preparations within the scope of the present invention can also contain inorganic pigments which protect the skin against UV radiation and are commonly used in the cosmetics industry. These are oxides of titanium, zinc, iron, zirconium, silicon, manganese, aluminum, cerium and mixtures thereof, and derivatives in which the oxides are the active substances. Pigments based on titanium dioxide are particularly preferred. The amounts described for the above combinations can be used. The cosmetic and dermatological preparations according to the invention contain cosmetic active ingredients, adjuvants and / or additives, such as antioxidants, preservatives, preservatives, bactericides, fragrances as usually used in such preparations. , Foam inhibitor, dye, pigment with coloring effect,
Thickeners, surfactants, emulsifiers, plasticizers, moisturizing and / or moisturizing substances, fats, oils, waxes or alcohols, polyols, polymers, foam stabilizers, electrolytes, organic solvents or silicone derivatives, It may contain other common ingredients of cosmetic or dermatological preparations.

It is likewise advantageous to add customary antioxidants to the preparations according to the invention. According to the invention, said conventional antioxidants can be all antioxidants, suitable or traditional for cosmetic and / or dermatological applications.

Antioxidants include amino acids (eg, glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (eg, urocanic acid) and their derivatives in very small tolerated doses (eg, pmol to μmol / kg). Derivatives, D, L-carnosine,
Peptides such as D-carnosine, L-carnosine and their derivatives (eg anserine), carotenoids, carotene (eg α-carotene, β-carotene, lycopene) and their derivatives, lipoic acid and its derivatives (eg dihydrolipoic acid) , Aurothioglucose, propylthiouracil, and other thiols (eg, thioredoxin, glutathione, cysteine, cystine,
Cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl, gamma-linoleyl, cholesteryl and glyceryl esters) and their salts,
Dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acid and its derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts) and sulfoxyimine compounds (eg buthionine sulfoximine, homocysteine sulfoxy) Imine, buthionine sulfone, penta-, hexa-,
Heptathionine sulfoximine), (metal) chelating agents (eg, α-hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), α-hydroxy acids (eg, citric acid, lactic acid, malic acid), humic acid, bile acids, Bile extract, bilirubin, biliverdin,
EDTA, EGTA and derivatives thereof, unsaturated fatty acids and their derivatives (eg, γ-linolenic acid, linoleic acid, oleic acid), folic acid and its derivatives, alanine diacetate, flavonoids, polyphenols, catechol, ubiquinone and ubiquinol and their derivatives Derivatives, vitamin C and derivatives (eg ascorbyl palmitate, ascorbyl phosphate Mg, ascorbyl acetate), tocopherols and derivatives (eg vitamin E acetate), and benzoin coniferyl benzoate, rutinic ac
id) and its derivatives, ferulic acid and its derivatives, butylated hydroxytoluene, butylated hydroxyanisole, nordihydroguaiac resin acid, nordihydroguaiaretinic acid, trihydroxybutyrophenone, uric acid and its derivatives, mannose and its derivatives, zinc and its derivatives (e.g. ZnO, ZnSO _4), selenium and derivatives thereof (e.g. selenium methionine), stilbenes and derivatives thereof (e.g. stilbene oxide and oxide trans - stilbene) and, present invention by appropriate of these active ingredients Derivatives (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids).
The amount of antioxidant (one or more compounds) in the preparation is preferably from 0.001 to 30% by weight of the total weight of the preparation,
Particularly preferably, it is 0.05 to 20% by weight, particularly 1 to 10% by weight.

If vitamin E and / or its derivatives are used as antioxidant (s), their respective concentrations should be chosen within the range from 0.001 to 10% by weight of the total weight of the preparation. Is convenient.

When the cosmetic or dermatological preparations in the context of the present invention are solutions or emulsions or dispersions, the solvents used are: water or aqueous solutions oils such as capric or caprylic triglycerides, But preferably castor oil; fats, waxes and other natural and synthetic fatty substances, preferably low-carbon alcohols, such as isopropanol, propylene glycol or glycerol, esters of fatty acids, or low-carbon alkanoic acids. Or esters of fatty alcohols with fatty acids;-low carbon number alcohols, diols or polyols;
And their ethers, preferably ethanol, isopropanol, propylene glycol, glycerol,
It can be ethylene glycol, ethylene glycol monoethyl or monobutyl ether, propylene glycol monomethyl, monoethyl or monobutyl ether, diethylene glycol monomethyl or monoethyl ether and similar products.

In particular, mixtures of the abovementioned solvents are used. In the case of alcoholic solvents, water can be a further component.

The oily phase of the emulsions, oleogels or hydrodispersions or lipid dispersions within the scope of the invention is advantageously saturated and / or unsaturated, branched, having a chain length of from 3 to 30 carbon atoms. From the group of esters comprising saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of from 3 to 30 carbon atoms and / or unbranched alkanecarboxylic acids, It is selected from the group of esters consisting of carboxylic acids and saturated and / or unsaturated, branched and / or unbranched alcohols having a chain length of 3 to 30 carbon atoms. The oil of such an ester is then conveniently placed in isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl oleate, n-butyl stearate, n-laurate.
Hexyl, n-decyl oleate, isooctyl stearate, isononyl stearate, isononyl isononanoate, 2-ethylhexyl palmitate, lauric acid 2
-Ethylhexyl, 2-hexyldecyl stearate,
It may be selected from the group consisting of 2-octyldodecyl palmitate, oleyl oleate, oleyl erucate, ersyl oleate, ersyl erucate and mixtures of such esters, synthetic, semi-synthetic and natural, such as jojoba oil. it can.

In addition, the oily phase advantageously comprises a group consisting of branched and unbranched hydrocarbons and waxes, silicone oils, dialkyl ethers, saturated or unsaturated, branched or unbranched alcohols, and Fatty acid triglycerides, in particular from triglycerol esters of saturated and / or unsaturated, branched and / or unbranched alkanecarboxylic acids having a chain length of from 8 to 24, in particular from 12 to 18, carbon atoms. You can choose. The fatty acid triglycerides are advantageously used, for example, in synthetic, semi-synthetic and natural oils,
For example, it can be selected from the group consisting of olive oil, sunflower oil, soybean oil, peanut oil, rapeseed oil, almond oil, coconut oil, coconut oil, coconut oil and the like.

Any desired mixtures of such oil and wax components can also be used advantageously for the purposes of the present invention. If desired, it may also be preferable to use a wax, for example cetyl palmitate, as the sole lipid component of the oily phase.

The oily phase is conveniently composed of isostearic acid 2
- ethylhexyl, octyl dodecanol, isotridecyl isononanoate, isoeicosane, cocoa, 2-ethylhexyl benzoate C _12-15 - alkyl, caprylic / capric acid triglyceride is selected from the group consisting of dicaprylyl ether.

Mixture of C _12-15 -alkyl benzoate and 2-ethylhexyl isostearate, C _12-15 benzoate
A mixture of alkyl and isotridecyl isononanoate, and C _12-15 -alkyl benzoate, isostearic acid 2
Mixtures of ethylhexyl and isotridecyl isononanoate are particularly advantageous.

Among the hydrocarbons, paraffin oil, squalane and squalene are advantageous for the purposes of the present invention.

Furthermore, the oily phase advantageously contains cyclic or linear silicone oils or, in addition to said silicone oils or silicone oils, it is possible to use additional amounts of other oily phase components. Preferred but can consist exclusively of such oils.

Cyclomethicone (octamethylcyclotetrasiloxane) is advantageously used as a silicone oil which can be used according to the invention. Alternatively, other silicone oils, such as hexamethylcyclotrisiloxane, polydimethylsiloxane, poly (methylphenylsiloxane) can be advantageously used for the purposes of the present invention.

Furthermore, mixtures of cyclomethicone with isotridecyl isononanoate and mixtures of cyclomethicone with 2-ethylhexyl isostearate are particularly advantageous. The gels used according to the invention are usually, for oil-alcoholic gels, preferably silicon dioxide or aluminum silicate, and for aqueous-alcoholic or alcoholic gels, preferably polyacrylates. In the presence of a thickening agent such as ethanol, isopropanol, 1,2-propanediol, glycerol and water or an oil as described above.

The solid sticks contain, for example, natural or synthetic waxes, fatty alcohols or fatty acid esters. Lip care sticks and body deodorant stick preparations are preferred.

Typical base materials suitable for use as cosmetic sticks within the scope of the present invention include fluid oils (eg, paraffin oil, castor oil, isopropyl myristate), semi-solid components (eg, petrolatum, lanolin), solid components (Eg, beeswax, ceresin and microcrystalline waxes and ozokerite) and high melting waxes (eg, carnauba wax,
Candelilla wax).

Propellants suitable for cosmetic and / or dermatological preparations within the scope of the present invention, which can be sprayed from aerosol containers, can be used on their own or as a mixture with one another. Normal, known,
Liquefied propellants that are easy to volatilize, for example hydrocarbons (propane, butane, isobutane). Compressed air is also advantageous.

Those of ordinary skill in the art will clearly appreciate that they are non-toxic in their own right and will, in principle, be appropriate for realizing the invention in the form of an aerosol preparation, but will not disturb their harm to the environment or other attendant circumstances. We know that there are propellants, especially fluorinated hydrocarbons and chlorofluorocarbons (CFCs), which must be avoided because of their influence.

The cosmetic preparations within the scope of the present invention also contain, in addition to an effective amount of the active ingredient according to the invention and the solvents usually used therefor, preferably water, organic thickeners such as gum arabic, xanthan gum, Sodium alginate,
Cellulose derivatives, preferably methylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, or inorganic thickeners, for example, aluminum silicate such as bentonite, or polyethylene glycol and stearic acid or polyethylene glycol distearate. Mixtures can also be present as gels. The thickener is, for example, 0.1
And between 30 and 30% by weight, preferably between 0.5 and 15% by weight in the gel.

The following examples are set forth to illustrate the invention.

[0068]

【Example】

(Example 1) W / O cream weight% paraffin oil (DAB9) 10.00 petrolatum 4.00 wool wax alcohol 1.00 PEG-7 hydrogenated castor oil 3.00 aluminum stearate 0.40 ferulic acid DL-α -Tocopheryl 0.50 Glycerol 2.00 Preservative, Dye, Fragrance Suitable amount Water Total 100.00 (Example 2) W / O lotion% by weight Paraffin oil (DAB9) 20.00 Petrolatum 4.00 Glucose sesqui-isostearate 2 0.000 aluminum stearate 0.40 DL-α-tocopheryl ferulate 0.50 α-tocopheryl acetate 1.00 glycerol 5.00 Preservative, dye, fragrance Water 100.00 (Example 3) O / W lotion Weight% paraffin oil (DAB9) 8.00 pal Isopropyl formate 3.00 Petrolatum 4.00 Cetylstearyl alcohol 2.00 PEG-40 castor oil 0.50 Cetylstearyl sodium sulfate 0.50 Carbomer sodium 0.40 DL-α-tocopheryl ferulate 0.50 Glycerol 3. 00 α-tocopherol 0.20 octyl methoxycinnamate 5.00 butyl methoxydibenzoylmethane 1.00 Preservative, dye, perfume water 100.00 (Example 4) O / W cream weight% paraffin oil (DAB9) 7.00 Avocado oil 4.00 Glyceryl monostearate 2.00 DL-α-tocopheryl ferulate 0.50 Titanium dioxide 1.00 Sodium lactate 3.00 Glycerol 3.00 Preservatives, dyes, fragrances Water 100 in total .00 (Example 5 Liposome-containing gel wt% lecithin 6.00 shea butter 3.00 DL-α-tocopheryl ferulate 0.50 α-tocopherol 0.20 biotin 0.08 sodium citrate 0.50 glycine 0.20 urea 0.20 PCA sodium 0.50 hydrolyzed collagen 2.00 xanthan gum 1.40 sorbitol 3.00 preservative, dye, flavor appropriate amount water total 100.00 (Example 6) sunscreen emulsion weight% cyclomethicone 2.00 cetyl dimethicone copolyol 0.20 PEG-22 dodecyl copolymer 3.00 paraffin oil (DAB9) 2.00 caprylic / capric triglyceride 5.80 octyl methoxycinnamate 5.80 butyl methoxydibenzoylmethane 4.00 DL-α ferulic acid − Ferryl 0.50 acetate α- tocopheryl 0.50 ZnSO ₄ 0.70 Na ₄ EDTA 0.30 preservative, dye, perfume qs water total 100.00 (Example 7) Sunscreen emulsion wt% cyclomethicone 2.00 Cetyl Stearyl alcohol + PEG-40 hydrogenated castor oil + sodium cetyl stearyl sulfate 2.50 glyceryl lanolinate 1.00 caprylic acid / capric triglyceride 0.10 lauryl methicone copolyol 2.00 octyl stearate 3.00 castor oil 4 0.000 glycerol 3.00 acrylamide / sodium acrylate copolymer 0.30 hydroxypropylmethylcellulose 0.30 octyl methoxycinnamate 5.00 butylmethoxydibenzoylmethane 0.50 ferulic acid DL-α -Tocopheryl 0.50 α-Tocopheryl acetate 1.00 Na ₄ HEDTA 1.50 Preservative, dye, perfume Appropriate amount of water 100.00 (Example 8) Sunscreen emulsion wt% Cyclomethicone 2.00 Cetylstearyl alcohol + PEG -40 hydrogenated castor oil + sodium cetylstearyl sulfate 2.50 glyceryl lanolinate 1.00 caprylic acid / capric acid triglyceride 0.10 laurylmethicone copolyol 2.00 octyl stearate 3.00 castor oil 4.00 glycerol 3 0.000 acrylamide / sodium acrylate copolymer 0.30 hydroxypropylmethylcellulose 0.30 octyl methoxycinnamate 5.00 butylmethoxydibenzoylmethane 0.75 DL-α-tocophere ferulate Le 0.50 Na ₄ HEDTA 1.50 preservatives, dyes, perfumes qs Water total 100.00 (Example 9) spray preparation wt% alpha-tocopherol 0.10 ferulic acid DL-alpha-tocopheryl 0.50 Ethanol 28 .20 preservatives, dyes, perfume Proper amount propane / butane 25/75 all 100.00 The main aspects according to the present invention are shown below.

1. Use of tocopheryl ferulate for unwanted pigmentation of the skin. 2. Use according to claim 1, characterized in that the tocopheryl ferulate is present in an effective amount in a cosmetic or dermatological preparation.

3. Use according to claim 1, characterized in that the selected tocopheryl ferulate is DL-α-tocopheryl ferulate.

4. The tocopheryl ferulate (s)
Is a cosmetic or topical dermatological preparation at a concentration of from 0.01 to 10%, preferably from 0.1 to 5%, in particular from 0.2 to 2.0% by weight of the total weight of the preparation Use according to claim 2, characterized in that it is present in

 ────────────────────────────────────────────────── ─── Continuing on the front page (72) Inventor Ube Sienlok Deutschland-23866 Nahe Lerchenbeck 33 (72) Inventor Heiner Machus Deutschland-22297 Hamburg Crof Manschjulase 82be (72) Inventor Ulrich Kukusu 8-2007, Akaikai, Urayasu City, Chiba Prefecture, Japan 8-72 (72) Inventor Kazuo Inoue 3-15 Shinyamashita Shinyamashita, Naka-ku, Yokohama-shi, Kanagawa Prefecture 3-201

Claims (1)

[Claims] 1. The method according to claim 1, wherein the pigmentation of the skin is
Use of tocopheryl ferulate.