Depigmenting dermatological and/or cosmetic composition

Drug – bio-affecting and body treating compositions – Bleach for live hair or skin

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424 59, 4241951, A61K 742, A61K 748

Patent

active

058690310

DESCRIPTION:

BRIEF SUMMARY
This application claims priority under 35 USC 371 based upon PCT/FR96/00422 filed Mar. 21, 1996 and under 35 USC 119 based upon FR 95 03425 filed Mar. 23, 1995.
The present invention relates to novel dermocosmetic compositions which have depigmenting activity.
The color of the skin is due to several substances: haemoglobin in the blood vessels, carotenoids in the dermis and, especially, melanin in the epidermis.
This melanin is produced by melanocytes in the basal layer, under the action of tyrosinase, copper and oxygen.
Under the effect of exogenous or endogenous stimulations, changes in skin color may appear. These are dyschromias.
A change in the skin pigmentation may take place:
This may take place in the epidermis or in the dermis and may be due to a variation in the amount of melanin or in the number of melanocytes.
Hyperchromias are accumulations of melanin pigments, carotenoids or exogenous pigments.
The melanin in the skin is formed by a complex association of eumelanin and pheomelanin.
Their biosyntheses are common up to dopaquinone (double oxidation of tyrosine by tyrosinase, a cupro-proteinic enzyme). Their synthetic routes then diverge.
Brown eumelanin is an indole-5,6-quinone polymer, whereas pheomelanin, which is responsible for the red color, is a compound containing close to 10% sulfur and has a structure which is a polymer of cysteinyldopa.
Enzymes other than tyrosinase participate in the creation and control of melanins: 5,6-dihydroxyindole and controls melanogenesis in the absence of tyrosinase, cysteinyldopa, between the biosynthesis of eumelanin and pheomelanin.
It appears that the surrounding sulfur level is the determining factor of such an orientation.
The glutathione reductase activity and the level of reduced glutathione are higher in people with ginger pigmentation than in those with brown pigmentation. 5,6-dihydroxyindole-2-carboxylic acid and controls the proportion of carboxylated subunits in the melanin polymer.
Agents which depigment or whiten the complexion are chemical compounds that are capable of acting at the tissue, cellular or subcellular level.
They act on melanin itself or on the existence of melanocytes (melanocytotoxicity).
The general modes of action may be as follows: melanosomes in the keratinocytes.
Moreover, it is necessary to demonstrate and eliminate the factor which induces hyperpigmentation before treating it (U.V., perfume, oestroprogestative, and to recommend a maximum-type sun protection throughout the medical treatment).
The motivations which compel people to bleach their skin may be very diverse.
Direct lightening of the skin is desired in Black Africa, with traditional or chemical solutions which have considerable harmful side effects on the appearance and structure of the skin.
The pallor or whiteness of asiatic facial skin is obtained with molecules which act with the least possible toxicity (arbutin, kojic acid and ascorbic acid).
The treatment of hyperpigmentation marks in white people requires the use of diverse molecules, the main one of which, hydroquinone, is the subject of intense scrutiny and its maximum cosmetic dose is 2%.
There is thus a need for compositions which have pronounced depigmenting activity at moderate concentrations, and which are well tolerated by the skin.
Accordingly, the subject of the present invention is a dermatological and/or cosmetic composition, characterized in that it contains a depigmenting active extract obtained from mouse-ear hawkweed.
Mouse-ear hawkweed, Hieracium pilosella, belongs to the family of Compositae. It is a small herbaceous ground-covering plant 10 to 30 cm in height.
The leaves form a basal rosette, they are long, oval and whitish underneath and covered with a silky down on both sides.
The flower-bearing stem is upright, single and bears a capitulum with hermaphroditic flowers, all ligulated, pentadentate and pale yellow in color. There are many bracts, often carrying black glandular hairs.
The fruit is a finely ribbed achene with aigrettes.
Mouse-ear hawkweed flowers from May to September.
It

REFERENCES:
patent: 5085870 (1992-02-01), Seguin et al.
patent: 5559146 (1996-09-01), Sablon
patent: 5607692 (1997-03-01), Ribier et al.

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