Volume 56, Issue 1
  • ISSN: 0002-9637
  • E-ISSN: 1476-1645



This study was designed to determine the pharmacokinetic parameters of a new pharmaceutical form of artemisinin (a natural substance extracted from the 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 pharmacokinetic studies. For artemisinin, the mean pharmacokinetic parameters were maximum drug concentration (C) = 0.36 µg/ml; peak time (t) = 100 min; appearance half-life (t) = 0.62 hr; distribution half-life (t) = 2.61 hr; decline half-life (t) = 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 pharmacokinetic parameters for dihydroartemisinin were appearance rate constant (K) = 2.11 hr;; elimination rate constant (K) = 1.18 hr; 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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