Patent ID: 6835392
Filing Date: 2004-12-28
Classification: A61K,Y10S

Abstract:
A method for enhancing the flux of a drug through a body surface, comprising administering the drug to a localized region of a human patient's body surface in combination with an effective permeation enhancing amount of permeation enhancer composition comprised of a hydroxide-releasing agent and a lipophilic co-enhancer, said lipophilic co-enhancer being selected from the group consisting of:(i) a compound having a molecular weight in the range of about 150 to 1000 and an aqueous solubility of less than about 1 wt %, and the structure (CH3â€”Lâ€”X)nR, wherein: n is 1 or 2; L is alkylene or alkenylene containing 1 to 3 double bonds, and from about 6 to about 22 carbon atoms; X is selected from the group consisting ofâ€”COOâ€”, â€”CH2Oâ€”, and â€”CH2Oâ€”(CO)â€”; and R is selected from the group consisting of H, lower alkyl, and lower alkyl substituted with one or two hydroxyl groups, with the proviso that if R is H, X is necessarily â€”CH2Oâ€”, and wherein when n is 2, R contains at least two carbon atoms; (ii) a lower alkyl ester of a C10-C18 fatty acid; and (iii) an esterified polyol selected from the group consisting of propylene glycol mono- or di-substituted with a C10-C18 fatty acid and glycerol mono- or di-substituted with a C10-C18 fatty acid; wherein the composition is effective to provide a pH in the range of approximately 8.0 to 13.0 at the localized region of the body surface, and the amount of hydroxide-releasing agent in the composition is the total of (a) the amount required to neutralize any acidic species in the composition plus (b) an amount equal to approximately 0.5 wt % to 25 wt % of the composition.