Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Patent
1998-07-31
2000-09-05
Kishore, Gollamudi S.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
514725, 514844, 514859, 514937, 514938, A61K 700, A61K 9107
Patent
active
061139289
DESCRIPTION:
BRIEF SUMMARY
The present application is a U.S. National Application filed under 35 USC 371 of PCT/FR97/00196, filed Jan. 31, 1997 based upon French application Serial No. 96/01276 filed Feb. 2, 1996.
The present invention relates to dermocosmetic compositions containing retinal and to a process for improving their stability during storage.
Care products containing retinoids have become a center of interest in recent years. Retinoic acid, which is also known as vitamin A acid or tretinoin, is used in the treatment of acne, and there are many and varied products containing vitamin A acid.
More recently, other applications of retinoids have been revealed, such as actinic ageing. In effect, individuals who have been exposed to a great deal of sunlight during their childhood show the following characteristics in adulthood: craggy, wrinkled, yellow, saggy, rough, dry skin with hyperpigmentation, often with the appearance of various malignant growths. These phenomena are more pronounced in fair-skinned people, who burn often and do not tan.
U.S. Pat. No. 4,603,146 describes the treatment of skin damaged by exposure to the sun, using a preparation containing vitamin A acid in an emollient excipient. Subsequent to this, U.S. Pat. No. 4,877,805 disclosed that retinoids can be used to prevent and restore damage caused by sunlight on human skin.
It is also known that the use of certain retinoids, such as retinal (vitamin A aldehyde) (patents FR 94/03339 and FR 94/03970) and vitamin A esters (acetate and palmitate), are preferred to retinoic acid on account of their better skin tolerance. The reason for this is that retinal (vitamin A aldehyde), for example, occurs naturally in human metabolism: it is used in vision.
Patent FR 2,681,784 revealed the value of retinal and its precursors in the treatment of complaints such as rosacea or seborrhoeic dermatitis.
However, these are compounds with poor physicochemical stability; their formulation in a form which has good organoleptic qualities as well as good storage properties has not been satisfactorily solved to date.
For example, active retinal can be in 13-cis or 13-trans form, or in the form of mixtures thereof.
During storage, other forms tend to appear, such as 9-cis-retinal, 11-cis-retinal or condensation products of polymeric type, which are inactive.
U.S. Pat. No. 4,826,828 proposed the use of volatile silicones and ethanol for the preparation of compositions containing retinol; these preparations can be diluted before application by formation of a water/oil emulsion.
U.S. Pat. No. 4,720,353 describes water/oil emulsions stabilized with a specific organopolysiloxane.
However, these formulations do not give satisfactory storage results.
Patent application WO 93/00085 describes retinoid formulations in the form of a water/oil emulsion, stabilized with a complex system comprising a chelating agent and water-soluble and liposoluble antioxidants. EP 440,398 also relates to water/oil emulsions of retinoids.
These are formulations involving many parameters that are difficult to implement. In addition, water/oil emulsions are poorly suited to topical application, particularly in cosmetology.
Patent applications FR 94/03339 and FR 94/03970 proposed improved retinal formulations. For example, the stability of the oil/water emulsion is improved, in FR 94/03339, by using liposoluble antioxidants.
The Applicant has now found that the stability of retinal-based compositions in oil/water emulsion form can be optimized by the choice of constituents for the oily phase.
Hence, the subject of the present invention is a dermocosmetic composition containing retinal, characterized in that it is an oil-in-water emulsion and in that the constituents of the fatty phase have a peroxide number of less than or equal to about 5.
The chemical stabilization of retinal is defined by the persistent concentration of the latter in its original chemical form, this being after a defined storage duration and temperature.
The removal of any starting material having a peroxide number of greater than 5 makes it possib
REFERENCES:
patent: 5093360 (1992-03-01), Yu
patent: 5776986 (1998-07-01), Couval
European Pharmacopea translation of manography for lanolin and hydrated lanolin, eight (8) pages (1997).
Nogueira Laurent
Peyrot Nicole
Kishore Gollamudi S.
Pierre Fabre Dermo-Cosmetique
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