European Journal of Clinical Pharmacology

, Volume 54, Issue 5, pp 411–414

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

Authors

  • V. Navaratnam
    • Centre for Drug Research, Universiti Sains Malaysia, 11800 Penang, Malaysia
  • S. M. Mansor
    • Centre for Drug Research, Universiti Sains Malaysia, 11800 Penang, Malaysia
  • M. N. Mordi
    • Centre for Drug Research, Universiti Sains Malaysia, 11800 Penang, Malaysia
  • A. Akbar
    • University Health Centre, Universiti Sains Malaysia, Penang, Malaysia
  • M. N. Abdullah
    • Cardiothoracic Department, General Hospital, Penang, Malaysia
PHARMACOKINETICS AND DISPOSITION

DOI: 10.1007/s002280050484

Cite this article as:
Navaratnam, V., Mansor, S., Mordi, M. et al. E J Clin Pharmacol (1998) 54: 411. doi:10.1007/s002280050484

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 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.

Key words Artesunic acidPharmacokineticsMalaria

Copyright information

© Springer-Verlag Berlin Heidelberg 1998