发明名称 A COMPOSITION FOR TRANSDERMAL DELIVERY OF HORMONES WITHOUT PENETRATION ENHANCERS AND ITS USE
摘要 The present invention relates to a composition for transdermal delivery comprising a drug-containing layer that comprises gestodene or an ester thereof and a carrier selected from the group consisting of polyisobutylenes, polybutenes, polyisoprenes, polystyrenes, styrene isoprene styrene block polymers, styrene butadiene styrene block polymers and mixtures thereof, wherein the drug-containing layer has a solubility for said gestodene of no more than 3% by weight of the drug-containing layer. The gestodene or an ester thereof is in an amount ranging between 0.5 and 3% by weight of the drug-containing layer. A patch comprising a drug-containing layer with low content of hormones, such as gestodene, and optionally an estrogen (e.g. ethinyl estradiol) is the most representative. Upon administering the patch to a woman, plasma levels of at least 1.0 ng/ml of gestodene is achieved at steady state conditions without the need of incorporating penetration enhancers or permeation enhancers in the drug-containing layer. Satisfactorily plasma levels of the hormones is also achieved throughout a period of at least 1 week, making the patch applicable for being used in female contraception with the concept of administering the patch ones weekly.
申请公布号 EA011160(B1) 申请公布日期 2009.02.27
申请号 EA20060001089 申请日期 2004.12.10
申请人 SCHERING AKTIENGESELLSCHAFT 发明人 BRACHT STEFAN;DITTGEN MICHAEL;HUBER PETRA;LANGGUTH THOMAS;SCHENK DIRK
分类号 A61K9/70;A61K31/56;A61K31/565;A61P15/18 主分类号 A61K9/70
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