Transdermal delivery of estradiol and process for manufacturing

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...

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424449, A61F 1300

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active

057051852

ABSTRACT:
The present invention relates to a transdermal delivery device for estradiol where the metabolic degradation of estradiol to estrone during permeation is inhibited by another substance in the transdermal delivery device. The transdermal device also includes a compound for enhancing the rate of estradiol permeation. The transdermal delivery device containing the inhibitor and enhancer can also be used to simultaneously deliver both estradiol and a progestin at therapeutic rates.

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Cooper, E.R., "Increased Skin Permeability for Lipophilic Molecules," Journal Pharmaceutical Sciences, 73(8):1153-1156, (1984).
Idson, B., "Dermatological Emulsions," Cosmetics & Toiletries, Creams and Lotions, 95:59-62 (Mar. 1980).
Mollgaard et al., "Vehicle Effect On Topical Drug Delivery" II. Concurrent skin transport of drugs and vehicle components, Acta Pharm. Suec. 20:443-450 (1983).
Biological Abstracts, vol. 88, nr. 1, 1989, abstract nr 9062, Philadephia, PA, US; goodman et al.: "Action of penetration enhancers on skin as assessed by the permeation of model drug 5-fluorouracil and estradiol", & J. Invest. Darmatol. 91(4): 323-327, 1988.
Proceed. Intern. Symp. Control. Rel.Bioact. Mater. 14 (1987) pp. 101-102.

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