Importance

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Abstract

This invention relates to compounds and a method for their use in carrying physiologically active agents through body membranes such as skin and for retaining these agents in body tissues. More specifically, the invention relates to carboxylic acid derivatives and salts thereof, which compounds are useful in topically administering a physiologically active agent to a human or animal via a composition comprising the agent and an effective amount of a compound represented in one embodiment by the general formulae: ##STR1## wherein W represents oxygen, sulfur, or two hydrogen radicals; Z represents oxygen, sulfur, or --CH.sub.2 --; 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; R'' represents alkyl, alkylthioalkyl, alkoxyalkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group; R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy, --(CH.sub.2).sub.y COOR.sub.1 and with y being between zero and 3, inclusive; R'represents hydrogen or --(CH.sub.2).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 m is between one and 5, while n is between 1 and 24, and x is zero or 1, inclusive. The invention further relates to the penetration-enhancing agents themselves and the method of making such penetration-enhancing agents.

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First Claim