Importance

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Abstract

This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer being a carboxylic acid derivative or a salt thereof represented in one embodiment by the general formula ##STR1## wherein W represents oxygen, sulfur, or two hydrogen radicals; wherein Z represents oxygen, sulfur, or --CH.sub.2 --; wherein R represents alkyl optionally substituted with one to three double or triple bonds, --SR'', --OR'', --NHR'', --CH.sub.3, or COOR.sub.1, and wherein R.sub.1 represents hydrogen or lower alkyl; wherein R'' represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group; wherein R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, --(CH2).sub.y COOR.sub.1 and with y being between zero and 3, inclusive; and wherein R' represents hydrogen or --(CH2).sub.y COOR.sub.1 such that when R' is hydrogen, then W is two hydrogen radicals and R' is not hydrogen; and when R' is hydrogen, then R' is not hydrogen; and wherein m is between one and 5, preferably 2, 3, or 4, while n is between 1 and 24, preferably between 5 and 12, and x is zero or 1, inclusive. It has been found that both open and closed-chain embodiments of the penetration enhancer are sufficient to carry physiologically active agents through body membranes and into the bloodstream.

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First Claim