Pharmacokinetic comparison of two formulations of talniflumate 370mg tablets in healthy Korean volunteers .

Abstract

Talniflumate, a prodrug of niflumic acid, is a potent analgesic and anti-inflammatory drug that has been widely used for the treatment of rheumatoid diseases. The aim of this study was to compare the pharmacokinetics and to evaluate the bioequivalence of two formulations of talniflumate 370mg tablets (test formulation: Flumagen^® 370mg tablet; reference formulation: Somalgen^® 370mg tablet). A randomized, open-label, single dose, two-sequence, two-period crossover clinical study was conducted. After oral administration of the study drug in each period, blood samples were collected up to 15 hours post-dose. The plasma concentration of niflumic acid, a metabolite of talniflumate, was determined using HPLC-MS/MS. The pharmacokinetic parameters were estimated by non-compartmental method. The maximum plasma concentration (Cmax) and area under the concentration-time curve from zero to the time point with the last measurable concentration (AUClast) for the test formulation were 290.7±199µg/L and 1,154±643µg×h/L, respectively, and the corresponding values for the reference formulation were 286.8±193µg/L and 1,151±577µg×h/L, respectively. The geometric mean ratio and 90% confidence intervals (CI) of the test formulation to the reference formulation for the Cmax and -AUClast were 0.983 (0.829-1.166) and 0.979 (0.856-1.121), respectively. The pharmacokinetic profiles of the test and reference formulations were found not to be significantly different, meeting the Korean regulatory criteria for bioequivalence. .