论文部分内容阅读
Aim To investigate the pharmacokinetics of the antimalarial artemisinin in rats after single and multiple oral doses. Methods Six male Wistar rats were orally given a single dose of artemisinin 40 mg·kg-1(Group 1). Another six rats were orally given artemisinin at the same dose once daily for 5 consecutive days(Group 2). Artemisinin plasma concentrations，after single dose or after 5 consecutive doses，were determined by high performance liquid chromatography-tandem mass spectrometry(LC/MS/MS). Results The artemisinin pharmacokinetic parameters of Group 1 were compared with that of Group 2. The areas under the plasma concentration-time curve(AUC0-8)decreased from 126.53 h·ng·mL-1 of Group 1 to 39.91 h·ng·mL-1 of Group 2(p<0.05)，and oral clearance(CL/F)increased dramatically from 375.54 L·h-1 to 1365.84 L·h-1(p<0.05). However，the half-life(t1/2)did not change significantly(p>0.05). Conclusions The optimized LC/MS/MS method was successfully applied to the pharmacokinetic study of artemisinin in rats after single and multiple oral doses. The results suggested that artemisinin exhibits time-dependent pharmacokinetics.