WO2000059462A1

WO2000059462A1 - Composition for cosmetic and dermatological skin care

Info

Publication number: WO2000059462A1
Application number: PCT/CH2000/000184
Authority: WO
Inventors: Roland Jermann; Thomas Schreier
Original assignee: Pentapharm Ag
Priority date: 1999-03-31
Filing date: 2000-03-30
Publication date: 2000-10-12
Also published as: EP1173145A1; CN1345224A; JP2002541082A; KR20010102559A; AU3270200A

Abstract

The invention relates to a composition which is suitable for cosmetic and dermatological skin care. In particular, said composition is to be used to protect the skin against damage by an increased ozone concentration in the atmosphere and against secondary reactions thereto. The composition contains at least one oxidoreductase and at least one proteinase inhibitor, whereby the weight ratio of the oxidoreductase to the proteinase inhibitor is preferably between 20: 1 and 1: 20, preferably between 10: 1 and 1: 10 and in particular, between 6: 1 and 1: 6.

Description

Composition for cosmetic and dermatological care of the skin

The present invention relates to a composition for cosmetic and dermatological care of the skin, this composition containing at least one oxidoreductase and at least one proteinase inhibitor. The compositions according to the invention can be present, for example, as a cream, lotion, emulsion, gel, powder, plaster or in another suitable form.

The task of the skin as an organ enveloping the organism consists in sealing and mediating functions against the environment. Various biochemical and bio-physical systems serve to maintain the integrity of this exposed organ. For example, an immune system protects the skin from damage caused by pathogenic microorganisms, the melanin-forming system regulates pigmentation and protects the skin from radiation damage, a lipid system produces lipid micelles that contain the transdermal water loss, and regulated keratin synthesis provides the mechanically resistant horny layer. The systems mentioned are based on complex chemical processes, the course of which is kept in motion by enzymes and regulated by enzyme inhibitors. Even a slight inhibition or disinhibition of these biochemical systems manifests itself in noticeable changes in the skin. The visible and tangible condition of the skin is, however, a yardstick for beauty, health and youth; Preserving it is a general goal of nourishing cosmetics.

The human skin usually reacts to exogenous, ie external stress factors such as UV radiation, ozone or other harmful substances present in the air (environmental pollution) with slight or severe irritation. nen. In particular, the skin is damaged by the released in irritation reactions of oxygen radicals and non-spe ^¬-specific proteases. For example, this can have a negative effect on the appearance or the elasticity or the barrier functions of the skin. In inflammatory processes and immune reactions, excess mobilized body proteinases, such as tryptases, elastases, collagenases and cathepsins, can attack the skin and in particular its structural proteins such as collagen and elastin.

EP 0 532 465 discloses the use of selected protein fractions obtained from legume seeds as a proteinase inhibitor for the cosmetic and dermatological care of the skin and for the treatment of inflammatory skin diseases.

It has now surprisingly been found that a combination of an oxidoreductase together with a proteinase inhibitor is excellent for the cosmetic and dermatological care of the skin and for the treatment of inflammatory skin diseases and in particular for protection against damage to the skin by pollutants in the atmosphere, such as ozone and nitrogen oxides , Dust particles etc., as well as UV rays and detergents, is suitable, the protection against the damage caused by ozone being in the foreground. The combination of a biotechnologically produced, purified oxidoreductase with a proteinase inhibitor, preferably a proteinase inhibitor obtained from legume seeds and containing selected protein fractions, is particularly suitable. Human keratinocytes, which were exposed to atmospheric ozone in an in vivo study, showed increased survivability. Clinical studies on subjects with skin irritated or inflamed and dry as a result of detergents and UV radiation, showed a considerable improvement in skin irritation when the composition according to the invention was applied. Similarly, in vivo studies by measuring skin elasticity showed significant improvements in skin elasticity and resistance.

The present invention is defined in the claims. In particular, the present invention relates to a composition which is suitable for the cosmetic and dermatological care of the skin, in particular for protecting the skin against damage caused by an increased ozone concentration in the atmosphere and its subsequent reactions, characterized in that this composition comprises at least one oxidoreductase and contains at least one proteinase inhibitor.

The present invention also relates to the use of a composition which contains at least one oxidoreductase and at least one proteinase inhibitor for the cosmetic and dermatological care of the skin and for the treatment of inflammatory skin reactions, in particular for protection against damage to the skin by pollutants in the atmosphere (ozone , Nitrogen oxides, dust particles etc.), UV rays and detergents.

The invention further relates to a preparation which is preferably a cream, lotion, emulsion, a gel, powder, plaster or another suitable cosmetic form of application which contains a composition according to the invention.

The weight ratio of the oxidoreductase to the proteinase inhibitor is generally preferably in the range from 20: 1 to 1:20, preferably in the range from 10: 1 to 1:10 and in particular from 6: 1 to 1: 6. For dermatological and cosmetic use, the substances according to the invention are expediently used in a skin-friendly vehicle, for example as a cream, lotion, gel, face mask, powder or plaster. The acid value is preferably in the pH range from 5.5 to 9. With the exception of the plasters, the finished preparations generally contain 0.001 to 1% by weight, preferably 0.01 to 0.5% by weight, preferably 0.05 to 0.5% by weight , the composition according to the invention as dry matter, calculated on the total weight (100% by weight) of the finished product. However, the preparations can also contain larger amounts, for example up to about 2.5% by weight, preferably 0.001 to 2.2% by weight, calculated on the total weight of the finished product. The upper limit is not critical. However, plasters for transdermal application of a preparation according to the invention can contain up to 10% by weight, preferably up to 5% by weight, of the composition according to the invention (always calculated as dry matter) calculated on the total weight (100% by weight) of the patch -Finished preparation included. The composition preferably contains the proteinase inhibitor in an amount of at least 0.005% by weight, preferably at least 0.01% by weight, calculated on the total weight of the composition. In order to facilitate the formulation of liquid or semi-solid preparations, in a first step, well-dosed, stable active ingredient concentrates which contain the combination according to the invention of at least one oxidoreductase and at least one proteinase inhibitor, with an active ingredient content as dry substance of 0.01 to 10 wt. %, preferably from 0.1% by weight to 5% by weight, can be prepared by dissolving the combination of active substances according to the invention in water and with the addition of a water-soluble preservative, such as, for example, methyl p-oxybenzoate, to prevent microbial growth Growth and one polyhydric alcohol, such as ethylene glycol or propylene glycol, to stabilize the active ingredient.

The oxidoreductases used according to the invention are able to intercept or neutralize free oxygen radicals. Oxidoreductases are preferably produced biotechnologically. This production is known per se and, for example, in Appl. Microbiol. Biotechnol. (1987) 26, pp. 531-536. Oxidoreductases are, for example, lactoperoxidase, glutathione oxidase, glutathione reductase, glutathione peroxidase, superoxide dismutase, thiol oxidase, peroxidase, thioredoxin reductase, cytochrome c reductase, cytochrome oxidase. Lactoperoxidase, glutathione peroxidase and superoxide dismutase are preferred.

The proteinase inhibitor to be used according to the invention is capable of rendering non-specific proteinases ineffective. The proteinase inhibitor to be used according to the invention is preferably a protein fraction containing at least one protein which a) was isolated from legume seeds, and b) at least one band in polyacrylamide gel electrophoresis with sodium dodecyl sulfate, c) molecular weights in the range from 3,000 to 30 minutes. 000 g / mol, d) a total nitrogen content of 14% to 20% and

Amino nitrogen from 1% to 2% based on the protein content, e) solubility in water and aqueous electrolyte solutions and insolubility in ethanol and acetone, f) strong precipitation in aqueous solution after the addition of

Trichloroacetic acid, sulfosalicylic acid, picric acid or

Benzethonium chloride, and g) inhibition of proteinases. Such preferred proteinase inhibitors are described, for example, in EP 0 532 465. Proteins or proteinase inhibitors to be used according to the invention are preferably produced from legume seeds, for example from bean species, such as, for example, Phaseolus angularis, Phaseolus lunatus, Phaseolus aureus, Phaseolus vulgaris, Phaseolus coccineus, Phaseolus limensis, from pea species such as, for example, La thyrus odora tus, from soybeans Glycine max and Glvcine hispida, from peanut Arachis hypogaea and from seeds of tropical legumes of the genera Cajanus, Dolichus, Vigna and Vi cia. Protein fractions which have been produced from legume seeds soya or lima beans are preferred.

The composition according to the invention is preferably used in day creams, after-sun creams, in products for the treatment of dry, poorly elastic skin, for skin which is sensitive to harmful substances of the environment, such as, for example, ozone, or also for the regenerative treatment of tired, aging or stressed skin, used.

The composition according to the invention is preferably produced on an aqueous basis and can contain further additives such as solvents, preservatives, buffers, antioxidants and / or dyes. Such additives are known per se and are listed, for example, in the CTFA Dictionary. Preferred solvents are, for example, polyglycols or polyalcohols, preferably glycerol. Preferred preservatives are, for example, phenoxyethanol, methylparaben, propylparaben, ethylparaben or butylparaben, such as are commercially available, for example, as a mixture under the brand name Phenonip®. Other additives are known to the person skilled in the art. The composition according to the invention can also be combined with active ingredients, such as sunscreens, moisturizers, skin-revitalizing active ingredients, barrier agents and / or self-tanners. Such active ingredients are known per se. Sunscreens include octyl methoxycinnamate, butyl methoxydibenzoylmethane, benzophenone, titanium dioxide, zinc oxide, and related compounds. Humectants are, for example, glycosammoglycans, hyaluronic acid and other polysaccharides, proteins and protein hydrolysates such as collagen, elastm, wheat protein hydrolysates and similar compounds, urea, glycols and polyglycols. Skin revitalizing active ingredients include vitamins, alpha-hydroxy acids, amino acids and related compounds. Barriers are, for example, ceramides, free fatty acids, sterols, triglycerides. Self-tanning agents are, for example, dihydroxyacetone or erythrulose.

The methods for testing inflamed skin and the corresponding healing processes are known per se. The following application examples explain the invention.

example 1

Table 1

* made from soybeans

Preparation of a make-up lotion: a) The additives of the substances listed in Table 1 under A) are heated in a mixer to 70 ° C. and mixed well. The substances listed in Table 1 above under B) are then mixed in a mixer at a temperature of 75 ° C. b) The mixture of components B) is then slowly added to mixture A with stirring at 70 ° C. and, after the addition has ended, cooled to 50 ° C., homogenized and then cooled to 30 ° C. Then the dye is added and stirred cold. You get a make-up lotion with a very good effect.

Example 2 Table 2

* made from soybeans

Production of a protective and regenerative lipstick:

a) The wax premix specified in Table 2, No. 1 is melted at 80 ° C. Components 2 to 5 are ground separately in a ball mill to form a homogeneous suspension with an average particle size of 10-30 μm. This suspension is added to the melted wax premix and homogenized. Components 6 and 7 are then added in succession.

b) Now component 8 is melted at 80 ° C. The compounds 9 to 13 are heated to 80 ° C. and added to the molten component 8, so that an emulsion of the components listed under B) is obtained.

c) The emulsion of components B) is stirred into the mixture prepared in paragraph a) at 80 ° C., stirred well, poured into molds (lipstick molds) and allowed to cool. The lipstick produced in this way protects the lips against harmful environmental influences such as ozone, nitrogen oxides, UV rays etc. and detergents.

Example 3 Table 3

* obtained from lima beans

Preparation of an emulsion-like douche gel for cleaning and care of the skin: a) The compounds A) are mixed well. Connection 7 is released in connection 6. The solution obtained is stirred into the mixture of compounds A).

b) The compounds of phase C) are dissolved one after the other in compound 8. The solution obtained is stirred into the mixture obtained in section a).

c) The compounds of phase D) are stirred into the mixture obtained in section b) and the pH in the gel obtained is adjusted to 5.2. Example 4 Table 4

* Made from lima beans Production of a protective day cream:

a) The components of phase A) are mixed and heated to 70 ° C. while mixing. The components of phase B) are heated to 75 ° C.

b) The resulting mixture of phase B) is added to the mixture of phase A) obtained with stirring. The mixture is then cooled to 50 ° C., homogenized and further cooled to 30 ° C.

c) The compound 16 of phase C) is now added and mixed well. You get a day cream with good protection against environmental influences. Example 5 Table 5

* made from soybeans

Preparation of a regenerative gel: a) Components 2 to 6 of phase A) are dissolved in water. Components 7 and 8 of phase B) are added to thicken and neutralize the mixture obtained, a gel being obtained.

b) The compounds 9 and 10 are stirred into the gel obtained. Then component 12 is dissolved in component 11 and phase D is stirred into the gel. A clear, firm gel is obtained which is suitable for the intensive treatment of tired or slightly damaged skin.

Claims

claims

1. Composition which is suitable for the cosmetic and dermatological care of the skin, in particular for protecting the skin against its damage by an increased ozone concentration in the atmosphere and its subsequent reactions, characterized in that this composition has at least one oxidoreductase and at least one proteinase inhibitor contains, wherein the weight ratio of the oxidoreductase to the proteinase inhibitor is preferably 20: 1 to 1:20, preferably 10: 1 to 1:10 and in particular 6: 1 to 1: 6.

2. Composition according to claim 1, characterized in that it contains the proteinase inhibitor in an amount of at least 0.005% by weight, preferably at least 0.01% by weight, calculated on the total weight of the composition.

3. Composition according to claim 1 or 2, characterized in that it contains a biotechnologically produced purified oxidoreductase.

4. Composition according to one of claims 1-3, characterized in that the proteinase inhibitor is a protein fraction containing at least one protein which a) has been isolated from legume seeds, and b) at least one band in polyacrylamide gel electrophoresis with sodium dodecyl sulfate, c ) Molecular masses in the range from 3,000 to 30,000 g / mol, d) a total nitrogen content of 14% to 20% and amino nitrogen of 1% to 2% based on the protein content, e) solubility in water and aqueous electrolyte solutions and Insolubility in ethanol and acetone, f) strong precipitation in aqueous solution after addition of trichloroacetic acid, sulfosalicyl acid, picric acid or benzethonium chloride, and g) inhibition of proteinases.

5. Composition according to any one of claims 1-4, characterized in that the proteinase inhibitor

Legume seeds was produced, preferably from soybeans or lima beans.

6. Preparation for dermatological and cosmetic use, which has a composition according to one of the

Contains claims 1-5, characterized in that it is a cream, lotion, a gel, a face mask, a powder or a plaster.

7. Preparation according to claim 6, characterized in that its acid value is in the pH range from 5.5 to 9.

8. Preparation according to one of claims 1-7 in the form of a cream, lotion, gel, face mask or powder, characterized in that it is 0.001 to 2.2% by weight, preferably 0.001 to 1% by weight, preferably 0.01 to 0.5 wt .-%, preferably 0.05 to 0.5 wt .-%, of the composition according to any one of claims 1-5 as a dry substance, calculated on the total weight (100 wt .-%) of the finished preparation.

9. plaster for transdermal application of a composition according to any one of claims 1-5, characterized in that this up to 10 wt .-% of a composition according to one of claims 1-6, calculated as dry matter and based on the total weight (100 % By weight) of the finished plaster preparation.

10. Day cream, after-sun cream, products for the treatment of dry and less elastic skin, for skin which is sensitive to harmful substances of the environment, in particular to ozone, characterized in that it has a composition according to any one of claims 1- 5 contains.

11. Preparation according to one of claims 1-10, characterized in that it further contains a sunscreen, humectant, skin-revitalizing active ingredients, barrier agents and / or self-tanners.

12. Use of a composition according to any one of claims 1-11 for the cosmetic and dermatological care of the skin and for the treatment of inflammatory skin reactions, in particular for protection against damage caused by pollutants in the atmosphere, such as ozone, nitrogen oxides, dust particles, etc., UV rays and Detergents.