Abstract: AIM: To study the pharmacokinetics and bioequivalence of nicergoline tablets in healthy volunteers. METHODS: A single oral dose (20 mg test or reference formulation)was given to 20 healthy volunteers according to an open randomized crossover design.10α-methoxy-9, 10-dihydrolysergol(MDL) is a majormetabolite of nicergoline, the concentration of MDL in plasma was determined by LC-MS.The pharmacokinetics parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS program. RESULTS: The main pharmacokinetic parameters of nicergoline tablets were as follows:t_max were (3.3±0.9) and (3.2±0.7) h, t_1/2 were (12.9±4.0) and(12.8±2.4) h, C_max were (23±6) and (22±6) μg/L;AUC_0-t were (291±51) and(282±44) μg·L^-1·h;AUC_0-∞ were (316±50) and (299±46) μg·L^-1·h.The relative bioavailability of two formulations was (104±17)%. CONCLUSION: The two nicergoline formulations are bioequivalent.

Key words: nicergoline, 10α-methoxy-9,10-dihydrolysergol, relative bioavailability, bioequivalence, LC-MS