Publication: The pharmacokinetics of oral dihydroartemisinin and artesunate in healthy Thai volunteers
Issued Date
2004-09-01
Resource Type
ISSN
01251562
Other identifier(s)
2-s2.0-20844440700
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Mahidol University
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SCOPUS
Bibliographic Citation
Southeast Asian Journal of Tropical Medicine and Public Health. Vol.35, No.3 (2004), 575-582
Suggested Citation
K. Na-Bangchang, S. Krudsood, U. Silachamroon, P. Molunto, O. Tasanor, K. Chalermrut, N. Tangpukdee, O. Matangkasombut, S. Kano, S. Looareesuwan The pharmacokinetics of oral dihydroartemisinin and artesunate in healthy Thai volunteers. Southeast Asian Journal of Tropical Medicine and Public Health. Vol.35, No.3 (2004), 575-582. Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/21563
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Title
The pharmacokinetics of oral dihydroartemisinin and artesunate in healthy Thai volunteers
Abstract
The pharmacokinetics of oral dihydroartemisinin (DHA) following the dose of 2 and 4 mg/ kg body weight dihydroartemisinin (Twisinin™, T-2 Program, Thailand) and 4 mg/kg body weight oral artesunate (AS; Guilin Pharmaceutical Works, Guangxi, China) were investigated in 20 healthy Thai volunteers (10 males, 10 females). All formulations were generally well tolerated. Oral DHA was rapidly absorbed from gastrointestinal tract with marked inter-individual variation. The pharmacokinetics of DHA following the two dose levels were similar and linearity in its kinetics was observed. Based on the model-independent pharmacokinetic analysis, median (95% CI) values for C max of 181 (120-306) and 360 (181-658) ng/ml were achieved at 1.5 hours following 2 and 4 mg/kg body weight dose, respectively. The corresponding values for AUC0-∞, t1/2z, CL/f and Vz/f were 377 (199-1,128) vs 907 (324-2,289) ng.h/ml, 0.96 (0.70-1.81) vs 1.2 (0.75-1.44) hours, 7.7 (4.3-12.3) vs 6.6 (3.1-10.1) 1/kg, and 90.5 (28.6-178.2) vs 6.6 (3.1-10.1) ml/min/kg, respectively (2 vs 4 mg/kg dose). Oral AS was rapidly biotransformed to DHA, which was detectable in plasma as early as 15 minutes of AS dosing. Following 4 mg/kg dose, median (95% CI) value for C max of 519 (236-284) ng/ml was achieved at 0.7 (0.25-1.5) hours. AUC0-∞, and t1/2z were 657 (362-2,079) ng.h/ml, 0.74 (0.34-1.42) hours, respectively. Cmax of DHA following oral AS were significantly higher, but total systemic exposure was greater following oral DHA at the same dose level (4 mg/kg body weight). There was no significant sex difference in pharmacokinetics of DHA.