The pharmacokinetics of artemisinin after oral, intramuscular and rectal administration to volunteers

J Pharm Pharmacol. 1990 Nov;42(11):810-3. doi: 10.1111/j.2042-7158.1990.tb07030.x.

Abstract

The pharmacokinetics after oral, intramuscular and rectal administration of artemisinin, a new potent antimalarial drug, to healthy volunteers has been examined. The study was set-up as a four-way cross-over design with a wash-out period of one week between the test days. In ten volunteers artemisinin concentrations in serum were monitored using a reversed phase HPLC assay with UV detection after derivatization. After oral administration, artemisinin was rapidly but incompletely absorbed, the mean absorption time was 0.78 h and the bioavailability relative to the intramuscularly injected suspension in oil 32%. The mean residence time of the latter (10.6 h) was 3 times that of the oral formulation (3.4 h). This seems to enable a twice daily dosage regimen for the intramuscular oil injection, while the oral formulation necessitates a more frequent dosing interval. After intramuscular injection and rectal administration of an aqueous suspension, very low and variable artemisinin concentrations in serum were observed, probably indicating a poor and erratic absorption.

MeSH terms

  • Administration, Oral
  • Administration, Rectal
  • Adult
  • Antimalarials / administration & dosage
  • Antimalarials / blood
  • Antimalarials / pharmacokinetics*
  • Artemisinins*
  • Chromatography, High Pressure Liquid
  • Humans
  • Injections, Intramuscular
  • Male
  • Sesquiterpenes / administration & dosage
  • Sesquiterpenes / blood
  • Sesquiterpenes / pharmacokinetics*

Substances

  • Antimalarials
  • Artemisinins
  • Sesquiterpenes
  • artemisinine