This study was designed to determine the pharmacokinetics parameters of a new pharmaceutical form of artemisinin (a natural substance extracted from the Artemisia annua L. plant) and of one of its derivatives, artesunate, a semisuccinate of 12-hydroxy-artemisinin. These two compounds are widely used in the treatment of malaria. The new oral forms of these two compounds, in 250-mg tablets, were used in two parallel pharmacokinetics studies. For artemisinin, the mean pharmacokinetics parameters were maximum drug concentration (C(max)) = 0.36 μg/ml; peak time (t(max)) = 100 min; appearance half-life (t(1/2 max)) = 0.62 hr; distribution half-life (t(1/2α)) = 2.61 hr; decline half-life (t(1/2β)) = 4.34 hr; and total area under the concentration-time curve (AUC) = 1.19 μg.hr/ml. For artesunate, its main metabolite, dihydroartemisinin, was measurable in the plasma. The mean pharmacokinetics parameters for dihydroartemisinin were appearance rate constant (K(a)) = 2.11 hr-1; elimination rate constant (K(e)) = 1.18 hr- 1; biotransformation half-life = 0.33 hr; elimination half-life = 0.65 hr; and AUC = 0.74 μg.hr/ml. Both pharmaceutical forms were well-tolerated and no undesirable side effects were observed in any of the subjects.
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