Pharmacokinetics and ex vivo anti-malarial activity of sera following a single oral dose of dihydroartemisinin in healthy Thai males.
The pharmacokinetics of dihydroartemisinin (DHA) was studied in eight healthy male Thai subjects after a single oral dose of 300 mg. Absorption of oral DHA was rapid, Cmax of 679 (307-1000) ng/ml was observed at 1.5 (1-2.5) hours after dosing [median (range)]. Plasma concentrations declined monoexponentially and at 12 hours after administration, the levels were below the detection limit (3 ng/ml). A large variation in the AUC (approximately) 50% was observed. The median (range) AUC was 2010 (636-4079) ng h/ml. The lag time and absorption half-life (t1/2a) were 0.169 (0.111-0.277) hours and 0.709 (0.367-1.118) hours respectively. t1/2z was 1.25 (0.79-1.89) hours Vz/f and CL/f were 5.9 (3.5-8.2) l/kg and 45.3 (28.6-122.8) ml/min/kg, respectively. The pattern of its ex vivo serum activity coincided with the plasma concentrations of DHA.
Na-Bangchang
K
K
Clinical Pharmacology Unit, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.
Congpoung
K
K
Ubalee
R
R
Thanavibul
A
A
Tan-anya
P
P
Karbwang
J
J
D000328:Adult; D000962:Antimalarials / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D037621:Artemisinins; D004334:Drug Administration Schedule; D006801:Humans; D008297:Male; D012016:Reference Values; D012717:Sesquiterpenes / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D013785:Thailand
D000962:Antimalarials; D037621:Artemisinins; D012717:Sesquiterpenes; C039060:artenimol