PHARMACOKINETICS OF TALNIFLUMATE, A PRODRUG OF NIFLUMIC ACID, FOLLOWING ORAL-ADMINISTRATION TO MAN

Plasma profile of niflumic acid following oral administration of talni flumate tablets (Somalgen) was compared to that of niflumic acid table ts in man. Plasma niflumic acid was assayed by HPLC method. Plasma nif lumic acid profile from the talniflumate tablets was similar to that f rom the niflumic acid tablets resulting in no differences in AUC, C-ma x, t(max), and MRT. It demonstrates that talniflumate is a prodrug of niflumic acid, and undergoes extensive first-pass biotransformation to niflumic acid. However, plasma niflumic acid concentration at 30 min after talniflumate dosing was significantly (p <0.05) higher than that of niflumic acid dosing. The more potent analgesic activity of talnif lumate than niflumic acid might be related to this higher plasma drug concentration at the earlier phase. Considering that talniflumate is l ess irritant to gastrointestinal mucosa than niflumic acid, talnifluma te seems to be advantageous over niflumic acid in therms of activity a nd side effects.