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Pharmacokinetics of artemisinin and artesunate after oral administration in healthy volunteers
Benakis, A.
Paris, M.
Loutan, L.
Plessas, C.T.
Plessas, S.T.
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.
(EN)
*Η εύρυθμη και αδιάλειπτη λειτουργία των διαδικτυακών διευθύνσεων των συλλογών (ψηφιακό αρχείο, καρτέλα τεκμηρίου στο αποθετήριο) είναι αποκλειστική ευθύνη των αντίστοιχων Φορέων περιεχομένου.
Pharmacokinetics of artemisinin and artesunate after oral administration in healthy volunteers
Pharmacokinetics of artemisinin and artesunate after oral administration in healthy volunteers
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