Transdermal delivery of hormones with low concentration of penetration enhancers
AssigneeBayer Intellectual Property GmbH
InventorsThomas Langguth, Stefan Bracht, Michael Dittgen, Petra Huber, Dirk Schenk
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AssigneeBayer Intellectual Property GmbH
InventorsThomas Langguth, Stefan Bracht, Michael Dittgen, Petra Huber, Dirk Schenk
Estimating the term…
The present invention relates to a patch comprising a drug-containing layer with low content of hormones, such as gestodene, and optionally an estrogen (e.g. ethinyl estradiol). 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.
A composition for transdermal delivery comprising a drug-containing layer wherein the drug-containing layer comprises Gestodene or an ester thereof and at least one pharmaceutically acceptable carrier which comprises one or more polyisobutylene polymer(s), wherein the drug-containing layer contains 25% to 99% by weight of the polyisobutylene polymer(s), wherein the drug-containing layer has a solubility for said Gestodene or an ester thereof of no more than 3% by weight of the drug-containing layer and the Gestodene or an ester thereof is completely dissolved in the layer, wherein the Gestodene or an ester thereof is in an amount ranging between 0.5 and 3% by weight of the drug-containing layer, wherein the drug-containing layer comprises less than 1.0% by weight of a skin penetration or permeation enhancer, wherein the drug-containing layer further comprises a tackifier selected from the group consisting of hydrocarbon resins, rosin resins and terpene resins, and wherein the one or more polyisobutylene polymer(s) include at least one polyisobutylene polymer with a high molecular weight of about 500,000 to 2,000,000 Da and at least one polyisobutylene polymer with a low molecular weight of about 20,000 to 100,000 Da.
Dependencies are inferred from the claim text.