Penetration enhancement with binary system of cell envelope...

A - Human Necessities – 61 – K

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A61K 47/10 (2006.01) A61K 47/12 (2006.01) A61K 47/14 (2006.01)

Patent

CA 1339073

Penetration-enhancing pharmaceutical compositions for topical transepidermal and percutaneous application are disclosed. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant contained in a novel penetration-enhancing vehicle comprising, (i) a cell-envelope disordering compound; and (ii) a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof. The weight ratio of cell-envelope disordering compound to lower alkanol is between about 50:1 to 1:50 and preferably between about 9:1 and 1:9. Preferred cell-envelope disordering compounds are oleic acid, oleyl alcohol, glycerol oleates, methyl oleate, methyl laurate and mixtures thereof. The novel penetration enhancer vehicles are non-irritating to the skin and enhance the penetration of a broad spectrum of pharmaceutical permeants including hydrophilic salts.

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