Comparative pharmacokinetic study of oral and rectal formulations of artesunic acid in healthy volunteers
- Cite this article as:
- Navaratnam, V., Mansor, S., Mordi, M. et al. E J Clin Pharmacol (1998) 54: 411. doi:10.1007/s002280050484
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 tmax and AUC, with no changes for Cmax and t1/2. As for dihydroartemisinin, differences were observed for tmax and Cmax 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.