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Comparative pharmacokinetic study of oral and rectal formulations of artesunic acid in healthy volunteers

  • PHARMACOKINETICS AND DISPOSITION
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Abstract

Objective: A single cross-over, comparative pharmacokinetic study of oral and rectal formulations of 200 mg artesunic acid in 12 healthy Malaysian volunteers is reported.

Methods: Plasma concentrations of artesunic acid and dihydroartemisinin were determined simultaneously by HPLC 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 administration 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.

Conclusion: There appear to be pharmacokinetic differences between oral and rectal modes of administration. The significance of these findings should be explored in malaria patients before appropriate therapeutic regimens are devised.

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Received: 14 January 1997 / Accepted in revised form: 24 February 1998

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Navaratnam, V., Mansor, S., Mordi, M. et al. Comparative pharmacokinetic study of oral and rectal formulations of artesunic acid in healthy volunteers. E J Clin Pharmacol 54, 411–414 (1998). https://doi.org/10.1007/s002280050484

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  • DOI: https://doi.org/10.1007/s002280050484

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