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.


Article metrics loading...

The graphs shown below represent data from March 2017
Loading full text...

Full text loading...

This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error