Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Reexamination Certificate
2002-08-19
2004-06-22
Wang, Shenglun (Department: 1617)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
C424S069000, C514S556000, C514S726000, C514S733000
Reexamination Certificate
active
06753000
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Technical Field of the Invention
The present invention relates to novel cosmetic/dermatological compositions comprising at least one hydroxystilbene in intimate admixture with ascorbic acid, especially for skin-firming applications.
In particular, the novel compositions of this invention are well suited to stimulate the restructuring of the skin and/or mucous membranes by stimulating the proliferation of the dermal fibroblasts.
2. Description of the Prior Art
Human skin includes two compartments or constituents, i.e., a superficial compartment, the epidermis, and a deep compartment, the dermis.
Natural human skin is principally composed of three types of cell: the keratinocytes, which are the vast majority, the melanocytes and the Langerhans cells. Each of these cell types contributes, by virtue of its intrinsic functions, towards the essential role played in the body by the skin.
The dermis provides the epidermis with a soft support. It is also the epidermis' nourishing factor. It primarily includes fibroblasts and an extracellular matrix itself composed of different extracellular proteins, among which are, in particular, collagen, elastin and various glycoproteins. This assembly of extracellular components is synthesized by the fibroblasts. Leukocytes, mastocytes and tissue macrophages are also found in the dermis. Too, the dermis contains blood vessels and nerve fibers.
On account of their activity in the synthesis of the extracellular matrix proteins (proteoglycans, collagen fibers and other structural glycoproteins), the fibroblasts are the principal factors involved in the structural development of the dermis.
The collagen fibers provide the dermis with solidity. They are very strong, but are sensitive to certain enzymes generally referred to as collagenases. In the dermis, the collagen fibers comprise fibrils sealed together, thus forming more than ten different types of structure. The structure of the dermis is essentially due to the overlapping of the trapped collagen fibers. The collagen fibers contribute to the skin's tonicity. The collagen fibers are regularly renewed, but this renewal decreases with age, thus leading, especially, to a thinning of the dermis. This thinning of the dermis is also due to pathological causes such as, for example, the hypersecretion of corticoid hormones, certain diseases (Marfan's syndrome, Ehlers-Danlos syndrome) or vitamin deficiencies (scurvy). It is also accepted that extrinsic factors such as ultraviolet radiation, tobacco or certain treatments (retinoic acid and derivatives, glucocorticoids, vitamin D and derivatives, for example) also have an effect on the skin and on its collagen level.
Degradation of the collagen fibers results, notably, in the appearance of loose, wrinkled skin which individuals have always tried to combat, since skin which looks smooth and taut is obviously more preferred.
Moreover, during menopause, the principal changes relating to the dermis are a decrease in the level of collagen and in the thickness of the dermis. In menopausal women, this results in thinning of the skin. Women thus experience a sensation of “dry skin” or of skin which feels tight, and an increase in the level of surface wrinkles and fine lines developed. The skin feels rough to the touch. Lastly, the skin is less supple. It is demonstrated that women gradually lose their level of collagen yearly after menopause and that 30% of the overall level is lost in the first five years after menopause.
Thus, serious need continues to exist for alternative active agents that maintain the level of collagen in the skin and also maintain the smooth and taut appearance of the skin.
One approach for achieving this result entails stimulating the proliferation of the fibroblasts and, consequently, on account of the increase in the number of secretory cells in the dermis, also maintaining or even reinforcing/enhancing the synthesis of collagen.
SUMMARY OF THE INVENTION
It has now surprisingly and unexpectedly been determined that association of at least one hydroxystilbene with ascorbic acid or one of the analogs thereof presents the attribute of stimulating the proliferation of the dermal fibroblasts in proportions that are higher than those which would reasonably be expected by simple addition of the effects of each of these components taken separately.
DETAILED DESCRIPTION OF BEST MODE AND SPECIFIC/PREFERRED EMBODIMENTS OF THE INVENTION
More particularly according to the present invention, the subject hydroxystilbenes are compounds having the following structural formula (I):
in which n is an integer ranging from 0 to 4, inclusive, and m is an integer ranging from 0 to 5, inclusive.
These compounds can be in cis- or trans-configuration.
According to this invention, by the term “hydroxystilbene” are intended both the compounds of formula I and the hydroxyalkyl derivatives thereof.
The hydroxystilbenes are compounds that exist in the natural state in plants of the Spermatophyte class and particularly in vine. Such compounds as, for example, resveratrol are found in grapes and in wine.
In the prior art, the hydroxystilbenes are useful, inter alia, as depigmenting agents (JP-87192,040), as vasodilators (EP-96830,517), as antithrombin agents (JP-05016,413), for the treatment of various cardiovascular conditions (CA-2,187,990), as mutagenesis and carcinogenesis inhibitors (JP-06/24,967) or are described as antioxidants.
Among these compounds, resveratrol (or 3,5,4′-trihydroxystilbene) is particularly interesting for the activities described above, notably because it is a natural compound which is found in the skin of grapeseeds and in wine. In this regard, the review by Soleas et al. (
Clinical Biochemistry
, Vol. 30, No. 2, pp. 91-113 (1997)) well summarizes the state of the art regarding this compound and hydroxystilbenes.
Moreover, ascorbic acid (or vitamin C) is known to stimulate collagen synthesis by preventing, as a co-factor, the self-inactivation of the lysine and proline hydroxylase enzymes and by increasing the synthesis of procollagen mRNAs. Ascorbic acid (or vitamin C) is also known to stimulate the synthesis of elastin in the skin. In this regard, compare U.S. Pat. Nos. 5,801,192 and 4,983,382 and EP-0,717,983. See, also the article entitled “Pola to incorporate vitamin C in new cosmetics line for skin care” from the Japan Economic Journal of Jun. 5, 1984 (page 15). Thus, it has been described that ascorbic acid in cosmetic compositions is useful for treating wrinkles (
Fragrance Journal
, Vol. 8, No. 6(45) (1980) pp. 38-43, “Cosmetic and vitamin action and safety to dermatology”).
Thus, the present invention features compositions comprising, in a physiologically acceptable medium, at least one hydroxystilbene in immixture with ascorbic acid or with an analog thereof.
The subject compositions are particularly suited for stimulating the proliferation of dermal fibroblasts.
Exemplary hydroxystilbenes according to this invention are mono-, di-, tri-, tetra-, penta-, hexa-, hepta-, octa- and nonahydroxystilbenes, or, alternatively, hydroxyalkyl derivatives thereof.
According to the invention, the hydroxystilbenes can be used alone or as mixtures of any nature and can be of natural or synthetic origin.
The hydroxystilbenes according to the invention are preferably selected from among:
4′-hydroxystilbene,
2′,4′-dihydroxystilbene,
3′,4′-dihydroxystilbene,
4,4′-dihydroxystilbene,
2′,4′,4-trihydroxystilbene,
3′,4′,4-trihydroxystilbene,
2,4,4′-trihydroxystilbene,
3,4,4′-trihydroxystilbene,
3,4′,5-trihydroxystilbene,
2′, 3,4-trihydroxystilbene,
2,3′, 4-trihydroxystilbene,
2′,2,4′-trihydroxystilbene,
2,4,4′, 5-tetrahydroxystilbene,
2′,3,4′,5-tetrahydroxystilbene,
2,2′, 4,4′-tetrahydroxystilbene,
3,3′, 4′,5-tetrahydroxystilbene,
2,3′, 4,4′-tetrahydroxystilbene,
3,3′,4,4′-tetrahydroxystilbene,
3,3′,4′,5,5′-pentahydroxysti
Breton Lionel
Liviero Christel
Burns Doane Swecker & Mathis L.L.P.
L'Oreal
Wang Shenglun
LandOfFree
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