Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1996-10-30
1998-08-25
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514178, 552617, 552625, 560138, A61K 3156, C07J 100, C07C 6900
Patent
active
057983488
ABSTRACT:
The pharmaceutical and/or cosmetic compositions for treatment of obesity and/or overweight contain an effective amount of a fatty-acid monoester of an estrogen and a fatty acid wherein the estrogen is estrone, diethylstilbestrol, estriol, estradiol or ethinyl estradiol and the fatty acid is oleic, linoleic, linolenic, stearic, palmitic, palmitoleic or arachidonic acids. The fatty-acid monoesters mimic the function of estrone monooleate, as a signal that informs the brain of the size of fat tissue mass. In preferred pharmaceutical and/or cosmetic compositions for intravenous injection the monoester is incorporated in a lipidic suspension, prepared from lipoproteins or from liposome components, such as soy oil and egg phospholipids. When administered to rats with a 15% of total adipose tissue, they produce weight reduction of about 10%, by a new and unexpected mechanism. They are useful for the treatment of obesity and/or overweight in mammals, with the advantages of high efficacy and low toxicity. New substantially pure fatty-acid monoesters including estrone monooleate and diethylstilbestrol monooleate are also described.
REFERENCES:
Zhang, Positional Cloning . . . , Dec. 1994, p. 425.
Vazquez-Alcantara, Long-Acting, Estrogenic . . . , J. steroid, 1989.
Clear, M. The Antiobesity Effect . . . , Hormel Institute, 1991
D. Sanchis, et al, Oleoyl-estrone . . . , Int. Journal of Obesity, 1996.
Henley III Raymond
Laboratorios S.A.L.V.A.T., S.A.
Striker Michael J.
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