Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice
Patent
1996-03-13
1998-03-24
Venkat, Jyothsan
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Cosmetic, antiperspirant, dentifrice
514460, 514859, 514944, 514969, A61K 748
Patent
active
057309922
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention is generally in the field of compositions for topical application onto the skin intended to improve the skin's condition. The present invention provides method and compositions useful for improving various skin conditions, in particular acne.
BACKGROUND OF THE INVENTION
Acne is a chronic inflammatory disorder of the pilosebaceous follicles, particularly in the face and neck region, occurring most commonly in adolescence between the ages of about 14 to about 19. Acne involves increased sebum secretion, hyperkeratinization in the infrainfundibulum of the follicular duct, increased microbial colonization and inflammation (Strauss, J. S., J. Dermatol. Treat., 1:3-6 (1989)). Various methods for the treatment of acne and other sebaceous glands' inflammation have been proposed, ranging from special diets, prevention of contact of the skin by known acneignic agents (e.g., low grade cosmetics), use of endocrine preparations containing progesterone or estrogen, and others, most of which have not proved to be effective. Additionally, it has also been proposed to use antiseptic, antibacterial and wide-spectrum antibiotic compounds in both topical and systemic application.
All hitherto used anti-acne agents were effective in suppressing the development of microbial population, keratinization and comedo formation in the sebaceous glands. However, only few of the anti-acne agents hitherto used were effective in the reduction of the sebum excretion rate (Gollnick, H., J. Dermatol. Treat. 1:S23-S28 (1990) and none of the agents was useful in affecting lipid biosynthesis in the pilosebaceous unit.
Isoprenoid groups such as cholesterol, squalene and cholesteryl-esters are synthesized via the mevalonate pathway (Goldstein, J. L., Brown, M. S., Nature, 34B, 425 (1990)), wherein the end-product is cholesterol. One of the key enzymes which regulate the production of mevalonate, the precursor of the above isoprenoid groups, is the 3-hydroxy-3-methylglutary coenzyme A (HMG-CoA) reductase. Inhibitors of this enzyme inhibit the synthesis of cholesterol and are thus used as antihypercholesterolemic medicaments for the treatment of arteriosclerosis, hyperlipemia and related diseases. An example of such an inhibitor is Lovastatin (Merck Index 5460, U.S. Pat. No. 4,231,938). Pharmaceutical compositions comprising this inhibitor of HMC-CoA reductase are given orally or parenterally to patients suffering from arteriosclerosis or hyperlipemia.
SUMMARY OF THE INVENTION
In accordance with the invention it has surprisingly been found that acne can be treated by the use of a topically applied inhibitor of cholesterol synthesis. In accordance with the invention use is thus made with an inhibitor of cholesterol synthesis to treat various skin disorders.
In accordance with the present invention there is thus provided a composition for topical skin application comprising a carrier and, as an active ingredient, an effective amount of an inhibitor of cholesterol synthesis.
The composition of the invention may be a pharmaceutical or cosmetic composition.
The pharmaceutical composition of the invention may be used for various indications including acne vulgaris, psoriasis, scalp dandruff and saborea.
The present invention further concerns the use of inhibitors of cholesterol synthesis, for example inhibitors of the HMG-CoA reductase, for the preparation of topical pharmaceutical compositions for the treatment, alleviation or prevention of skin disorders.
Also provided by the invention is a method for improvement of skin condition comprising topically applying onto the skin a composition comprising a carrier and, as an active ingredient, an effective amount of an inhibitor of cholesterol synthesis.. A particular application of the method is the treatment, alleviation or prevention of acne.
The term "effective amount" should be understood as meaning an amount of an active ingredient needed to achieve a desired therapeutic or pharmaceutical effect. For example, in a pharmaceutical composition of the inv
REFERENCES:
patent: 4231938 (1980-11-01), Monaghan et al.
J.S. Strauss, "The Pathogenesis of Acne: How Might Azelaic Acid Act?", Journal of Dermatological Treatment (1989) I, 3-6.
H. Gollnick, "The New Therapeutic Agent: Azelaic Acid in Acne Treatment", Journal of Dermatological Treatment (1990) 1 (Suppl 3): S23-S28.
Goldstein, Joseph L. and Brown, Michael S., "Regulation of the Mevalonate Pathway", Nature, vol. 343, 1 Feb. 1990, 425-430.
The Merck Index, An Encyclopedia of Chemicals, Drugs and Biologicals, 11th Edition, 1989.
Brenner Sara
Savion Naphtali
Ramot University Authority for Applied Research and Industrial
Venkat Jyothsan
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