Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Aldehyde doai
Patent
1996-09-20
1998-07-07
Cook, Rebecca
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Aldehyde doai
514970, A61K 3107
Patent
active
057769869
DESCRIPTION:
BRIEF SUMMARY
This is a 371 of PCT/FK95100250 filed Mar. 22, 1995.
The present invention relates to new dosage forms suitable for topical application and containing retinal.
Health-care products containing retinoids have become a focus of interest in recent years. Retinoic acid, also known by the name of vitamin A acid or tretinoin, is used in the treatment of acne, and compositions containing vitamin A acid are numerous and varied.
More recently, other applications of retinoids have been put forward, for instance light-induced aging. In effect, individuals who are exposed to large amounts of sunlight during their childhood display the following skin features in adulthood: wrinkled, furrowed, yellow, slack, rough, dry and blemished (hyperpigmentation) skin and various premalignant growths. These phenomena are more marked in fair-skinned individuals, who often burn in the sun and do not tan very much.
Before these skin manifestations appear clinically, serious adverse changes in the epidermis and dermis may be observed microscopically in young subjects who have received a large amount of exposure.
U.S. Pat. No. 4,603,146 describes the treatment of skin damaged by exposure to sunlight, using a preparation containing vitamin A acid in an emollient excipient. Later, in U.S. Pat. No. 4,877,805, it is taught that retinoids may be used to prevent and repair the damage caused by sunlight on human skin.
It is also known that the use of retinal (vitamin A aldehyde) is preferred to that of retinoic acid on account of its better skin tolerability. In effect, retinal (vitamin A aldehyde) occurs naturally in human metabolism: it is used, in particular, in treatments designed to improve vision.
However, retinal is a compound displaying poor physicochemical stability; its formulation in a form displaying good organoleptic qualities as well as good storage characteristics has not been achieved satisfactorily to date.
In the context of the present invention, the active retinal may be in 13-cis or 13-trans form or the form of all other mixtures of these isomers.
On storage, other forms tend to appear, such as 9-cis-retinal, 11-cis-retinal or condensation products of the polymer type, which are inactive.
U.S. Pat. No. 4,826,828 has proposed the use of volatile silicones and ethanol for the preparation of compositions containing retinol; these preparations may be diluted before application by formation of a water-in-oil emulsion.
U.S. Pat. No. 4,720,353 describes water-in-oil emulsions stabilized by a particular organopolysiloxane.
However, these formulations do not give satisfactory results on storage.
Application WO 93/00085 describes formulations of retinoids in the form of a water-in-oil emulsion, stabilized by a complex system comprising a chelating agent and water-soluble and fat-soluble antioxidant.
These formulations entail a large number of parameters which are difficult to implement. In addition, water-in-oil emulsions are poorly suited to topical application, especially in cosmetology.
Accordingly, the subject of the present invention is a dermocosmetological composition containing retinal, characterized in that it consists of an oil-in-water emulsion stabilized essentially by one or more fat-soluble antioxidants.
Oil-in-water emulsions according to the present invention possess good spreading capacities without a greasy feel. The specific stabilization system enables the phenomena of degradation over time which are observed with the conventional oil-in-water emulsions to be limited.
Antioxidants which are especially suitable for obtaining a stabilization system according to the invention may be chosen from the group comprising: butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), ascorbyl palmitate, alpha-tocopherol and its esters, citric acid, propyl gallate and/or mixtures thereof.
The alpha-tocopherol may be, in particular, in acetate form.
The retinal present in the composition is incorporated in the oily (internal) phase of the emulsion. The retinal will thus be better protected from aerial oxygen than if it were
REFERENCES:
patent: 5093360 (1992-03-01), Yu et al.
Clairand Valerie
Couval Emmanuelle
Firmino Nathalie
Jammes Henri
Peyrot Nicole
Cook Rebecca
Pierre Fabre Dermo-Cosmetique
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