Bioequivalence of huperzine A substain-release tablets after multiple doses in healthy volunteers

Objective To evaluate the relative bioavailability of two kinds of huperzine A tablets and the bioequivalence 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 tablets were as follows: Cmin(ss)were(0.54±0.21) and(0.78±0.20) ng·mL-1,Cmax(ss)were(1.65±0.45)and(1.83±0.37) ng·mL-1;Css were(1.05±0.28) and(1.22±0.28) ng·mL-1;tmax were(3.50±1.90)and(1.10±0.40) h;AUC0-t(ss) were(30.70±8.20)and(35.10±8.93) ng·h·mL-1;AUC0-∞(ss) were(36.90±10.30)and(41.30±11.10) ng·h·mL-1;AUCss were(25.30±6.80)and(14.60±3.41) ng·h·mL-1,respectively.The relative bioavailability of test tablets as estimated byAUC0-t(ss) was(87.7±11.6)%.There was significant difference in tmax between two tablets.Conclusion The result shows that the two huperzine A tablets made in two different pharmacy are bioequivalent.Huperzine A substain-release tablets clearly have the characteristic of slow releasing properties.