Determination of huperzine A in human serum by LC-MS/MS and its application to relative bioavailability

Objective:To develop a LC /MS/MS method for determining the concentration of huperzine A in human serum and to investigate the pharmacokinetics and bioequivalence of two tablets in Chinese healthy volunteers.Methods:LC/MS/MS was used to determine the concentration in the selected-reaction monitoring model after the samples were extracted with ethyl acetate.Target ions were at m/z 243.2→210.9 for huperzine A and m/z 229.9→212.9 for the internal standard.Twenty volunteers were randomly divided into two groups(test and reference) in a double cross-over design.Pharmacokinetic parameters were calculated with DAS 2.0 program.Results:The calibration curve was linear over the range of 0.08～8ng·mL-1.The main pharmacokinetic parameters of huperzine tablets were as follows:Cmax(2.596±0.914) and(2.675±0.848)ng·mL-1,Tmax(1.125±0.329) and(1.113±0.358)h,AUC0~72 h(31.275±6.889) and(30.476±7.051)ng·h·mL-1.Conclusion:The method was convenient,sensitive and specific.The statistical analysis showed that the test and reference preparation were bioequivalent.