Pharmacokinetics and Bioequivalence of Fudosteine in Healthy Chinese Volunteers Under Fasting and Fed Conditions: A 4-Way Replicate Crossover Study.

ABSTRACT

The bioequivalence of a generic fudosteine tablet vs a brand-named fudosteine tablet under fasting and fed conditions was evaluated in this study. This randomized, open-label, single-dose, 4-way replicate, crossover, bioequivalence study included 64 healthy Chinese subjects (fasting cohort, n = 32; fed cohort, n = 32) who were assigned to receive a single 200-mg dose of generic or brand-named fudosteine. Blood samples were collected before dosing and up to 24 hours after dosing. The plasma concentrations of fudosteine were analyzed by high-performance liquid chromatography-tandem mass spectrometry. Safety was monitored. There were no significant differences in maximum plasma concentration (Cmax ), area under the plasma concentration-time curve (AUC) from time 0 to time t (AUC0-t ), or AUC from time 0 to infinity (AUC0-∞ ) between the test and reference formulations. However, food showed a significant effect on Cmax , AUC0-t , and AUC0-∞ for both generic and brand-named fudosteine. The 90%CIs of the test/reference ratios of Cmax , AUC0-t, and AUC0-∞ were within the range of 80% to 125% under both fasting and fed conditions. No serious adverse events were reported. The bioequivalence between generic and brand-named fudosteine under fasting and fed conditions was demonstrated. Both of them had good tolerance for healthy Chinese volunteers. In addition, food delayed the absorption of fudosteine, so taking this medicine before meals might be an optimized option.