Multiple dose pharmacokinetics of artemisinin in rats by high performance liquid chromatography-tandem mass spectrometry

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-∞) decreased from 126.53 h·ng·mL -1 of Group 1 to 39.91 h·ng·mL -1 of Group 2 (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.