Topical compositions for prostaglandin E.sub.1 delivery

Drug – bio-affecting and body treating compositions – Designated organic nonactive ingredient containing other... – Carboxylic acid ester

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514946, 514947, 514573, A61K 4714, A61K 4718, A61K 906

Patent

active

060462442

ABSTRACT:
A topical composition of a semi-solid consistency suitable is provided for transdermal application of prostaglandin E.sub.1. The composition comprises prostaglandin E.sub.1, a penetration enhancer, a polysaccharide gum, a lipophilic compound, and an acidic buffer system. The penetration enhancer is an alkyl-2-(N,N-disubstituted amino)-alkanoate ester, an (N,N-disubstituted amino)-alkanol alkanoate, or a mixture of these. The lipophilic compound may be an aliphatic C.sub.1 to C.sub.8 alcohol, an aliphatic C.sub.8 to C.sub.30 ester, or a mixture of these. The composition includes a buffer system capable of providing a buffered pH value for said composition in the range of about 3 to about 7.4.

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Uekama et al. Improved Transdermal delivery of Prostaglandin E1 Through Hairless Mouse Skin: Combined Use of Carboxymethyl-ethyl-beta-cyclodextrin and Penetration Enhancers.
Journal of Pharmaceutical Pharmacology. Feb. 1992. vol. 44, No. 2. pp. 119-121.
Adachi et al. Inhibitory Effect of Prostaglandin E1 on Laurate-Induced Peripheral Vascular Occlusive Sequelae in Rabbits: Optimized Topical Formulation with Beta-Cyclodextrin Derivative And Penetration Enhancer HPE-101. Journal of Pharmaceutical Pharmacology. Dec. 1992. vol. 44, No. 12. pp. 1033-1035.
Article, "Alkyl N,N-Disubstituted-Amino Acetates", Buyuktimkin, N., et al., pp. 91-102, appearing in "Percutaneous Penetration Enhancers," 1995 by CRC Press, Inc.

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