PHARMACOLOGICAL STUDIES OF AMWANNICH BASE PRODRUGS OF IBUPROFEN

摘要

The final efficacy and safety of N-Mannich base prodrugs of amides of ibuprofen, IBMB-M and IBMB-P, were confirmed by performing pharmacological studies on animals. The antiinflammatory activity of the prodrugs was evaluated by rat paw edema method. The results confirmed that both the prodrugs have sufficient antiinflammatory activity. The gastrointestinal toxicity was evaluated on fasted rat model and these studies confirmed that both the prodrugs had remarkably reduced gastrointestinal ulceration. Finally, acute toxicity studies were performed on rats by administering the prodrugs at the dose level equivalent to LD_50 of ibuprofen and higher doses. The LD_50 of both the prodrugs was much higher than the LD_50 of ibuprofen, which confirmed the safety of the prodrugs.