Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
1999-10-12
2002-02-19
Dudash, Diana (Department: 1619)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S725000, C424S062000, C424S741000, C424S773000, C514S557000, C514S844000, C514S159000, C514S947000
Reexamination Certificate
active
06348204
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a cosmetic or dermatological composition containing, in combination, at least one extract of mulberry or an active substance isolated from such an extract, at least one extract of skullcap or an active substance isolated from such an extract, and at least one salicylic acid derivative. The present invention also relates to the use of the composition by topical application to the skin of the face and/or the body, with the objective of whitening or depigmenting the skin, of depigmenting head hair and/or other hair, or of treating skin pigmentation marks.
2. Description of the Background
The color of human skin depends on many different factors and, in particular, on the seasons of the year, race and sex, and it is mainly determined by the concentration and nature of the melanin produced by the melanocytes. In addition, at different periods in their lives, certain individuals develop darker and/or more colored marks on the skin, and more especially on the hands, which imparts heterogeneity to the skin. These marks also result from a large concentration of melanin in the keratinocytes located at the surface of the skin.
Similarly, the color of head hair and other hair results from melanin; when the head hair or other hairs are dark, certain people wish to have them lightened in color. This is particularly advantageous for hair which is less visible when light than when dark.
The mechanism of pigmentation of skin, head hair and other hair, that is to say the formation of melanin, is particularly complex and schematically involves the following main steps:
Tyrosine→Dopa→Dopaquinone→Dopachrome→Melanin
Tyrosinase is the essential enzyme involved in the above reaction sequence. In particular, tyrosinase catalyses the reaction for the conversion of tyrosine into dopa (dihydroxyphenylalanine) by virtue of its hydroxylase activity, and the reaction for the conversion of dopa into dopaquinone by virtue of its oxidase activity. Tyrosinase only acts when it is in the mature form, under the action of certain biological factors.
Tyrosinase is recognized as being depigmenting if it acts directly on the vitality of the epidermal melanocytes in which melanogenesis takes place and/or if it interferes with one of the steps in the biosynthesis of melanin, either by inhibiting one of the enzymes involved in melanogenesis or by becoming intercalated as a structural analogue of one of the chemical compounds in the synthetic chain of melanin, which chain can then become blocked and ensure the depigmentation.
The substances most commonly used as depigmenting agents particularly are hydroquinone and its derivatives, in particular its ethers such as hydroquinone monomethyl ether and monoethyl ether. Although these compounds have a certain efficacy, they are, unfortunately, not free of side effects because of the toxicity they entail, which can make them intricate, or even dangerous, to use. This toxicity arises from the fact that the compounds intervene in fundamental mechanisms of melanogenesis, killing cells which then risks disturbing the biological environment of the cells and which consequently obliges the skin to eliminate them by producing toxins.
Thus, hydroquinone is a compound which is particularly irritant and cytotoxic to melanocytes, and the total or partial substitution of this compound has been envisaged by those of skill in the art.
Substances have thus been sought which do not have any involvement in the melanogenesis mechanism, but which act upstream on tyrosinase by preventing its activation and are thus considerably less toxic.
The use of inoffensive topical depigmenting substances which are of good efficacy is most particularly desired in order to treat regional hyperpigmentations mediated by melanocyte hyperactivity such as idiopathic melasmas, which occur during pregnancy (“pregnancy mask” or chloasma) or in oestro-progestative contraception, localized hyperpigmentations mediated by hyperactivity and proliferation of benign melanocytes such as senile pigmentary marks known as actinic lentigo, accidental hyperpigmentations or depigmentations resulting from photosensitization and post-lesional cicatrization, as well as certain leucodermias such as vitiligo. For the latter it is possible for the cicatrization to result in a scar, giving the skin a whiter look, and leukodermias, failing the ability to repigment the injured skin. Depigmentation of the areas of residual normal skin is effected to give the skin an overall uniform white shade.
Thus, various whitening agents for human skin, head hair and/or other hair have been proposed which do not have the drawbacks of known compounds, i.e. which are non-irritant, non-toxic and/or non-allergenic to the skin and which are stable in a composition.
For example, patent EP-A-0,747,043 describes the use of alkyl salicylic acid derivatives as inhibitors of tyrosinase activity in a whitening or depigmenting composition. U.S. Pat. No. 5,580,549 also describes the use of alkyl and alkoxy salicylic acid derivatives at high concentrations or in combination with other depigmenting agents, for treating dyschromia.
Depigmenting cosmetic compositions comprising, as active principles, compounds which inhibit the activity of tyrosinase, obtained from extracts of bark, of the exudates or of the roots of mulberry, or sohakuhi, are also known as disclosed in
C.A. Essential Oils, Cosmetics,
vol. 88, 1978, page 227, abstract 88:65874z or JP-A-50 135,236. EP-A-0,296,923 also discloses a composition with depigmenting activity comprising an extract of mulberry, or an active substance isolated from such an extract.
For its part, JP 06-107,532 relates to a cosmetic composition which prevents and treats pigmentation marks by inhibiting melanogenesis, which composition contains from 0.001 to 20% by weight of one or more extracts, including an extract of the root of Scutellaria baicalensis (skullcap) and an extract of mulberry bark, and 0.001 to 30% by weight of a UV absorbing agent and/or an agent for scattering UV rays.
A need continues to exist for a depigmenting or whitening composition which is more effective than the compositions mentioned above, while at the same time is well tolerated.
SUMMARY OF THE INVENTION
Accordingly, one object of the present invention is to provide a composition for cosmetic or dermatological use for the depigmentation or whitening of the human skin or hair which is better tolerated by the skin and hair and which is more effective than art known compositions.
Briefly, this object and other object of the present invention as hereinafter will become more readily apparent can be attained by a cosmetic and/or dermatological composition containing, in combination, at least one extract of mulberry or an active substance isolated from an extract, at least one extract of skullcap or an active substance isolated from an extract, and at least one salicylic acid compound of formula (I) or a salt thereof:
wherein R is hydrogen or a saturated or unsaturated, linear, branched or cyclic aliphatic, alkoxy, ester or ketoxy chain containing from 2 to 22 carbon atoms and optionally substituted with at least one substituent selected from the group consisting of halogen, trifluoromethyl and hydroxyl in free form or esterified with an acid containing from 1 to 6 carbon atoms or with a carboxyl group which is free or esterified with a lower alcohol containing from 1 to 6 carbon atoms; and R′ is a hydroxyl group or an ester function of the formula:
wherein R
1
is a saturated or unsaturated C
1-18
-aliphatic group.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
In the salicylic acid formula above, substituent R preferably contains at least 4 carbon atoms. Preferred such groups are saturated linear alkyl or alkoxy radicals containing from 4 to 11 carbon atoms.
Advantageously, the salicylic acid derivative is selected from salicylic acid, 5-n-octanoylsalicylic acid, 5-n-decanoylsalicylic acid and 5-n-dodecanoyl-salicylic acid, particularly 5-n-oc
Dudash Diana
L'Oreal
Ostrup Clinton
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