PRODRUG ANHYDRIDES OF ASPRIN, INDOMETHACIN AND IBUPROFEN, THEIR PREPARATION, COMPOSITIONS, AND ANTI-INFLAMMATORY METHOD OF USE

摘要

Compositions degrading by hydrolysis to release a bioactive compound having carboxylic acid moieties, which are organic acid anhydrides having the following formula: Formula 1: IMAGE wherein R' is a residue of a therapeutic bioactive compound, for example, a non-steroidal anti-inflammatory agent; a penicillin or cephalosporin antibiotic; or bioactive compounds for non-therapeutic use, for example, herbicides, insecticides, fungicides, antimicrobials, pesticides, pheromones, and fertilizers; m is an integer of between 1 and 3; and R is a carrier. The resulting mixed anhydrides are characterized by having between one and three drug molecules attached to a single carrier molecule. The prodrugs are highly susceptibility to hydrolytic degradation in a predictable and controlled fashion, have variable solubilities in water and lipids, with increased biomembrane transport, elicit a bio-affecting/pharmacological response, and are less irritating to topical and gastric or intestinal mucosal membranes.