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Am. J. Trop. Med. Hyg., 56(1), 1997, pp. 17-23
Copyright © 1997 by The American Society of Tropical Medicine and Hygiene

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Pharmacokinetics of Artemisinin and Artesunate after Oral Administration in Healthy Volunteers

Achille Benakis, Maria Paris, Louis Loutan, Charalambos T. Plessas AND Stavros T. Plessas
Laboratory of Drug Metabolism, Department of Pharmacology, University Medical Centre, Geneva, Switzerland; Travel and Migration Medicine Unit, Geneva University Hospital, Geneva, Switzerland; Laboratory of Physiology, Department of Nursing, University of Athens, Athens, Greece

This study was designed to determine the pharmacokinetic 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 pharmacokinetic studies. For artemisinin, the mean pharmacokinetic parameters were maximum drug concentration (Cmax) = 0.36 µg/ml; peak time (tmax) = 100 min; appearance half-life (t1/2 max) = 0.62 hr; distribution half-life (t1/2{alpha}) = 2.61 hr; decline half-life (t1/2ß) = 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 (Ka) = 2.11 hr;-1; elimination rate constant (Ke) = 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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Q. LI, L. H. XIE, A. HAEBERLE, J. ZHANG, and P. WEINA
THE EVALUATION OF RADIOLABELED ARTESUNATE ON TISSUE DISTRIBUTION IN RATS AND PROTEIN BINDING IN HUMANS
Am J Trop Med Hyg, November 1, 2006; 75(5): 817 - 826.
[Abstract] [Full Text] [PDF]


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Copyright © 1997 by the American Society of Tropical Medicine and Hygiene.