| abstract |
Compounds and their method of use to transport physiologically active agents through membranes of the body, such as the skin, and to retain these agents in body tissues. More specifically, carboxylic acid derivatives and their salts useful for the topical administration of a physiologically active agent to a human or an animal by means of a composition containing the agent and an effective amount of a represented compound , in one embodiment, by the formulas (I), in which W represents oxygen, sulfur or two hydrogen radicals; Z represents oxygen, sulfur or -CH2-; R represents alkyl optionally substituted with one to three double or triple bonds, -SR '' ', -OR' '', -NHR '' ', -CH3 or COOR1, where R1 represents hydrogen or lower alkyl; R '' 'represents alkyl, alkylthioalkyl, alkoxy, alkyl, substituted aminoalkyl, optionally substituted with a phenyl, benzoyl or heterocyclic group; R 'represents hydrogen, alkyl, alkoxyl, acyloxyl, alkylthio, hydroxyl, - (CH2) yCOOR1, including between 0 and 3; R '' represents hydrogen or - (CH2) yCOOR1, so that when R '' is hydrogen, W represents two hydrogen radicals and R 'is not hydrogen; and when R 'is hydrogen, R' 'is not hydrogen; m is between 1 and 5, preferably equal to 2, 3 or 4, while n is between 1 and 24, preferably between 5 and 12, and x is equal to zero or one. It has been discovered that these penetration promoting agents transport physiologically active agents through membranes of the body and retain them in body tissues. The invention further relates to these penetration promoters themselves and their preparation process. |