Synthesis, In Vitro Hydrolysis, Bioanalytical Method Development and Pharmacokinetic Study of an Amide Prodrug of Ibuprofen

Ibuprofen, one of the most widely used non-steroidal anti-inflammatory drug, is an aryl acetic acid derivative, which is an active ingredient in variety of oral formulations such as tablets, gel, pellets, and syrup dosage forms used worldwide. Gastric side effects of ibuprofen are attributed to the presence of free – COOH group and inhibition of endogenous prostaglandins. In recent years, considerable research has been directed at designing prodrugs of ibuprofen with reduced gastro-intestinal toxicity. Numerous ester and amide prodrugs of ibuprofen have been reported. With this background, the present work involves the synthesis, analytical method development, in-vitro hydrolysis, bioanalytical method development, and pharmacokinetics study of an amide prodrug of Ibuprofen coded as TRB-559.