Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-04-25
1998-09-01
Cook, Rebecca
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3134
Patent
active
058011927
DESCRIPTION:
BRIEF SUMMARY
This is a 371 of PCT/lB96/00444 filed May 10, 1996.
The present invention relates essentially to the use of ascorbic acid, notably L-ascorbic acid or vitamin C, or of its isoascorbic acid isomer, called erythorbic acid, or salts or esters thereof, for promoting skin elastin synthesis. In the following part of the present description, the whole of these compounds is referred to under the generic name of <<ascorbic derivative >>for simplicity.
Vitamin C, or ascorbic acid, has been known for a long time for physiological activities such as an antiscorbutic, or an antioxidant such as described by DORVAULT, 23rd Edition, page 1893, edition Vigot, January 1995, or in the Merck Index 1989, 11th Edition, reference 855.
Furthermore, it is known from the article of C. L. Phillips et al. in J. Invest. Dermatol. 1994, 103, pages 228-232, that ascorbic acid favours the synthesis of collagen by fibroblasts of the human dermis, collagen contributing essentially to the resistance qualities of the skin against constraints which are applied thereto.
Furthermore, it is known from the article by Gregory C. Sephel et al. in J. Invest. Dermatol. 1986, 86, pages 279-285, that the production of elastin by the fibroblasts of aged donors diminishes. It is also known that the skin elasticity decreases significantly with age, as described by Takema et al. in British Journal of Dermatology 1994, 131 pages 641-648.
Within the context of the invention, it has been demonstrated in an unexpected way that these ascorbic derivatives enabled promoting the synthesis of elastin by the fibroblasts of the dermis, particularly the fibroblasts of the human dermis.
It shall be borne in mind now that in the dermis, the elastic fibres form a network which contributes to the elasticity of the skin and accordingly to its tone and firmness. Elastin is the major component of these fibres, and is initially synthesised by the fibroblasts in the form of a soluble polypeptide of 70 kDa which is tropoelastin. The formation of the microfibrils then takes place via intramolecular bonds, called desmosines, between the lysine residues of the polypeptide chains. These bonds confer a great insolubility to elastin.
Thus, an aim of the present invention is to solve the novel technical problem consisting of providing a solution which enables improving the skin elasticity in favouring the synthesis of elastin, according to one simply conceived solution which is easily usable on an industrial scale whilst still enabling a cosmetic or pharmaceutical, notably dermatological use.
Thus, according to a first aspect, the present invention relates to the use of ascorbic acid, particularly L-ascorbic acid or vitamin C, or of its erythorbic acid isomer, or salts or esters thereof, referred to under the generic name of ascorbic derivative, as cosmetic agent intended for promoting the synthesis of elastin by the fibroblasts of the dermis, with a view to improve particularly the skin elasticity, skin tone or to favour skin firmness.
According to a second aspect, the invention also relates to the use of ascorbic acid, in particular L-ascorbic acid or vitamin C, or of its erythorbic acid isomer, or salts or esters thereof, referred to under the generic name of ascorbic derivative, for the preparation of a pharmaceutical composition, notably dermatological composition, intended for promoting the synthesis of elastin by the fibroblasts of the dermis, with the view to improve particularly the skin elasticity, skin tone or to favour skin firmness.
Of course, the above-mentioned ascorbic derivative may be used both in a curative and in a preventative manner for correcting or preventing the loss of elasticity, tone or firmness of the skin, which is due notably to ageing or to the exposure to UV rays.
According to an advantageous embodiment, the above-mentioned ascorbic derivative is used topically at a concentration between 0.001% and 5% with respect to the total weight of a composition containing same in an appropriate excipient, vehicle or support, preferably cosmetically or
REFERENCES:
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Dumas et al., "In Vitro Biosynthesis of Type I and III Collagens by Human Dermal Fibroblasts from Donors of Increasing Age", Mechansims of Ageing and Development, vol. 73 (1994) pp. 179-187.
Dorvault, 23rd Edition, p. 1893, Edition Vigot, Jan. 1995.
Reference 855 Ascorbic Acid, Merck Index 1989, 11th Edition.
Phillips et al., "Effects of Ascorbic Acid on Proliferation and Collagen Synthesis in Relation to the Donor Age of Human Dermal Fibroblasts", Journal of Investigative Dermatology, vol. 103, No. 2, Aug. 1994, pp. 228-232.
Sephel et al., "Elastin Production in Human Skin Fibroblasts Cultures and Its Decline with Age", Journal of Investigative Dermatology, vol. 86, No. 3, Mar. 1986, pp. 279-285.
Takema et al., "Age-Related Changes in the Elastic Properties and Thickness of Human Facial Skin", British Journal of Dermatology, vol. 131, 1994, pp. 641-648. (Shisiedo) 1986.
Chemical Abstracts, vol. 72, nA 29295 1969.
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Bonte Frederic
Chaudagne Catherine
Dumas Marc
Meybeck Alain
Cook Rebecca
LVMH Recherche
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