Abstract: AIM: To evaluate the pharmacokinetics of Huperzine A sustained-release tablets after multiple doses in Chinese healthy volunteers. METHODS: In a randomized crossover trial, 24 healthy subjects received multiple oral doses of either Huperzine A sustained-release tablets or a common Huperzine A tablet for 7 days. The plasma concentrations were determined by LC/MS/MS. Pharmacokinetic parameters were obtained using DAS program. RESULTS: The major pharmacokinetic parameters of test and reference Huperzine A tables were as follows: C_{ss min} were (0.54±0.21) and (0.79±0.20)ng/mL,C_{ss max} were (1.65±0.45)and (1.83±0.37)ng/mL,C_ss were (1.05±0.28) and (1.22±0.28)ng/mL,t_max were (3.5±1.9) and (1.1±0.4) h,AUC_0-t(ss) were (31±8) and (35±9)ng·mL^-1·h,AUC_0-∞(ss) were (37±10)and (41±11)ng·mL^-1·h,AUC_ss were (25±7)and (15±3)ng·mL^-1·h,respectively. The relative bioavailability of test tablet as estimated by AUC_0-t(ss) was (88±12) %. There was significant difference in t_max between two tablets. CONCLUSION: The results show that the Huperzine A substain-release tablets clearly have the characteristic of slow releasing properties.

Key words: Huperzine A, Pharmacokinetics, LC/MS/MS