NZ334080A - Process for enhancing skin permeation of a drug by mixing a drug containing composition with a permeation enhancer before applying the mixture - Google Patents

Abstract

This process comprises; a) preparing a first composition comprising the active compound and vehicle, wherein the active compound has long term storage stability in the vehicle. b) preparing a second composition comprising a permeation enhancer for the active compound, which when mixed with the active compound results in the instability of the active compound and the permeation enhancer. c) applying the first and second composition to the skin area, at the same time, successively or as a premixture of the first and second compositions. The first composition exhibits a first rate of skin permeation when applied to an area of skin that is inadequate for the active compound to produce its pharmacological effect. A second rate of skin permeation of the active compound is obtained by forming an active composition of the active compound and the permeation enhancer. This second rate of skin permeation is substantially higher than the first rate and allows the delivery of a therapeutically effective amount of the active compound. Examples of the active compound include phospholipase A2 inhibitors, steroidal and nonsteroidal antiinflammatories, protein Kinase C inhibitors, antibiotics, anti-bacterials, bronco-spasm relaxants, vasodilators, sex hormones, diuretics and anti-UV compounds. Examples of the permeation enhancer include water, alcohols, propylene glycols, fatty alcohols, fatty acids sulfoxides, surfactants and alkanones.