Transdermal compositions with enhanced skin penetration properties
AssigneeJenapharm GmbH & Co. KG
InventorsMichael Dittgen, Sabine Fricke, Christoph Volkel, Kathrin Ahrens, Hagen Gerecke, Kai Kopke
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Abstract
The invention relates to a transdermal therapeutic system for application to the skin and/or mucosa consisting of at least one active substance in the form of a solid dispersion in combination with at least one destructuring agent and/or at least one structuring agent in a common matrix.
Claims35
Transdermal therapeutic system for application to the skin and/or mucosa consisting of at least one active substance in the form of a solid dispersion in combination with at least one destructuring agent and/or at least one structuring agent in a common matrix.
Transdermal therapeutic system according to any of the preceding claims, characterized in that the ratio between destructuring agent and structuring agent is from 10:1 to 1:10.
Transdermal therapeutic system according to any of the preceding claims, characterized in that the active substance is selected from hormones, immunomodulators, immunosuppressants, antibiotics, cytostatics, diuretics, gastrointestinal agents, cardiovascular agents and neuropharmaceuticals or mixtures thereof.
Composition for transdermal administration comprising in an amount of at least more than 10% by weight and less than 90% by weight a penetration-enhancing agent of the following formula 1 4
- where R1 and R2 are identical or different and are selected from the group of C1- to C6-alkyl radicals, in particular the optionally branched, saturated C1- to C4-alkyl radicals,
- R3 is selected from the group consisting of hydroxy-(C1- to C6-)alkyl radicals, in particular hydroxy-(C1-to C4-) alkyl radicals,
- and at least one pharmaceutical active substance or its pharmaceutically acceptable salt and
- another lipophilic penetration-enhancing agent.
Composition for transdermal administration comprising a penetration-enhancing agent of the following formula 1 5
- where R1 and R2 are identical or different and are selected from the group of C1to-C6-alkyl radicals, in particular the optionally branched, saturated C1- to C4-alkyl radicals,
- R3 is selected from the group consisting of hydroxy-(C1- to C6-)alkyl radicals, in particular hydroxy-(C1-to C4-)alkyl radicals,
- and at least one pharmaceutical active substance or its pharmaceutically acceptable salt and
- another lipophilic penetration-enhancing agent, excepting oleic acid, whose lipophilicity measured by determining the water absorption capacity is in the region of 0 to 1.4% by weight, preferably in the region of 0.001 to 0.330% by weight or in the region of 0.340 to 1.400% by weight.
Dependencies are inferred from the claim text.