Table 1 Mean pharmacokinetic parameters of artesunate (AS) and its active metabolite dihydroartemisinin (DHA) after pharmacokinetic modelling by using compartment analysis with IV-infusion fitting for AS following single intravenous infusion (2 minutes) at single dose of 2.4 mg/kg in the adults with uncomplicated falciparum malaria in Kenya (n = 28)
PK parameters artesunate | CA IV-infusion (PK model 9) | CV (%) | PK parameters dihydroartemisinin | CA analysis (PK model 14) | CV (%) |
|---|---|---|---|---|---|
Cmax (ng/mL) | 28,558 ± 28,531 | 99.8 | Cmax (ng/mL) | 2,932 ± 850 | 28.9 |
Tmax (h) | 0.028 ± 0.015 | 54.6 | Tmax (h) | 0.18 ± 0.06 | 30.0 |
AUCinf (ng · h/mL) | 1,879 ± 1,190 | 63.4 | AUCinf (ng · h/mL) | 3,543 ± 989 | 27.9 |
t1/2 distribution (h) | 0.05 ± 0.01 | 15.2 | t1/2distribution (h) | 0.13 ± 0.05 | 38.5 |
t1/2 elimination (h) | 0.17 ± 0.08 | 47.4 | t1/2elimination (h) | 1.30 ± 0.34 | 26.5 |
CL (mL/h/kg) | 1,728 ± 983 | 56.9 | CL/F (mL/h/kg) | 731 ± 205 | 28.0 |
Vss (mL/kg) | 139 ± 124 | 89.2 | Vss/F (mL/kg) | 1,048 ± 250 | 23.8 |
MRT (h) | 0.07 ± 0.02 | 30.9 | MRT (h) | 1.61 ± 0.44 | 27.3 |
Ratio of AUCDHA/AS |  |  |  | 1.94 ± 1.16 | 59.8 |
Ratio of CmaxAS/DHA |  |  |  | 10.24 ± 7.61 | 74.3 |
Ratio of t1/2 DHA/AS |  |  |  | 7.65 ± 3.16 | 41.3 |