COMPARATIVE PHARMACOKINETIC STUDY OF ORAL AND RECTAL FORMULATIONS OF ARTESUNIC ACID IN HEALTHY-VOLUNTEERS

Objective: A single cross-over, comparative pharmacokinetic study of o ral and rectal formulations of 200 mg artesunic acid in 12 healthy Mal aysian volunteers is reported. Methods: Plasma concentrations of artes unic acid and dihydroartemisinin were determined simultaneously by HPL C with electrochemical detection. The test drug was well tolerated and no undesirable adverse effects were observed. Results: Comparison of pharmacokinetic parameters of artesunic acid after oral and rectal adm inistration showed statistically significant differences in t(max) and AUC, with no changes for C-max and t(1/2). As for dihydroartemisinin, differences were observed for t(max) and C-max but not for AUC. Concl usion: There appear to be pharmacokinetic differences between oral and rectal modes of administration. The significance of these findings sh ould be explored in malaria patients before appropriate therapeutic re gimens are devised.