Comparative pharmacokinetic study of oral and rectal formulations of artesunic acid in healthy volunteers.
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 Cmax and t1/2. As for dihydroartemisinin, differences were observed for t(max) and Cmax but not for AUC.


CONCLUSIONS
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.
Navaratnam
V
V
Centre for Drug Research, Universiti Sains Malaysia, Penang.
Mansor
S M
SM
Mordi
M N
MN
Akbar
A
A
Abdullah
M N
MN
D000284:Administration, Oral; D000285:Administration, Rectal; D000328:Adult; D000962:Antimalarials / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D037621:Artemisinins; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D006801:Humans; D008297:Male; D012717:Sesquiterpenes / Q000097:blood / Q000493:pharmacokinetics; D013386:Succinates / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D000962:Antimalarials; D037621:Artemisinins; D019086:Bridged Bicyclo Compounds, Heterocyclic; D012717:Sesquiterpenes; D013386:Succinates; C039060:artenimol; C111789:artesunic acid