European Journal of Clinical Pharmacology

, Volume 52, Issue 4, pp 307–310

Pharmacokinetics and bioavailability of oral and intramuscular artemether

  • J. Karbwang
  • K. Na-Bangchang
  • K. Congpuong
  • P. Molunto
  • A. Thanavibul
PHARMACOKINETICS AND DISPOSITION

DOI: 10.1007/s002280050295

Cite this article as:
Karbwang, J., Na-Bangchang, K., Congpuong, K. et al. E J Clin Pharmacol (1997) 52: 307. doi:10.1007/s002280050295

Abstract

Objective: The pharmacokinetics and bioavailability of artemether and dihydroartemisinin were investigated in eight Thai males following the administration of single oral and intramuscular doses of artemether (300 mg) in a randomized two-way cross-over study.

Results: Both oral and intramuscular artemether were well-tolerated. In most cases, artemether and dihydroartemisinin were detected in plasma after 30 min and declined to levels below the limit of detection within 18–24 h. Compared with intramuscular administration, oral administration of artemether resulted in a relatively rapid but incomplete absorption [Cmax: 474 vs 540 ng · ml−1; tmax: 2.0 vs 3.9 h; AUC: 2.17 vs 5.20 μg · h · ml−1]. Geographic means of lag-time and absorption half-life (t1/2a) of oral vs intramuscular artemether were 0.28 and 1.1 h vs 0.30 and 2 h, respectively. t1/2z was significantly shortened after the oral dose [2.8 vs 6.9 h]. Mean oral bioavailability relative to intramuscular administration was 43.2%. The ratio of the AUCs of artemether to dihydroartemisinin was significantly lower after the oral than after the intramuscular dose (geometric mean: 0.29 vs 0.60).

Key words Artemether Thai males; malaria dihydroartemisinin pharmacokinetics bioavailability 

Copyright information

© Springer-Verlag Berlin Heidelberg 1997

Authors and Affiliations

  • J. Karbwang
    • 1
  • K. Na-Bangchang
    • 1
  • K. Congpuong
    • 1
  • P. Molunto
    • 1
  • A. Thanavibul
    • 1
  1. 1.Clinical Pharmacology Unit, Department of Clinical Tropical Medicine, Mahidol University, 420/6 Rajvithi Road, Pyathai, Bangkok 10400, ThailandTH

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