Table 2 The main pharmacokinetic parameters of artesunate (ARS) and its phase I/II metabolites (dihydroartemisinin: DHA, M1 and DHA-G) after one-day and five-day oral administrations of ARS (10 mg/kg) to male (M) and female (F) rats (mean ± s.d)
AUC0-t(nmol⋅h⋅L-1) | Cmax(nmol⋅L-1) | Tmax(h) | MRT (h) | CL/F (L⋅min-1⋅kg-1) | |||
|---|---|---|---|---|---|---|---|
One-day | ARS | M | 169.45 ± 52.77 | 657.30 ± 201.19 | 0.1 (0.1-0.2) | 0.3 ± 0.1 | 2.78 ± 0.85 |
F | 149.86 ± 52.36 | 677.70 ± 296.28 | 0.1 (0.1-0.2) | 0.2 ± 0.04 | 3.15 ± 0.92 | ||
DHA | M | 1470.64 ± 695.34 | 2139.18 ± 737.53 | 0.2 (0.2-0.3) | 0.6 ± 0.1* | 0.34 ± 0.13 | |
F | 1357.65 ± 564.25 | 2867.33 ± 982.21 | 0.3 (0.2-0.5) | 0.6 ± 0.1 | 0.38 ± 0.18 | ||
M1 | M | 208.79 ± 140.96 | 197.74 ± 135.08 | 0.5 (0.3-0.7)† | 0.8 ± 0.2 | 2.74 ± 1.36 | |
F | 280.05 ± 202.13 | 195.61 ± 89.26 | 0.8 (0.5-1.0)*† | 1.0 ± 0.2 | 2.55 ± 1.94 | ||
DHA-G | M | 568.52 ± 442.13 | 925.92 ± 708.54 | 0.2 (0.2-0.3) | 0.6 ± 0.2* | 1.08 ± 0.54 | |
F | 395.43 ± 129.49 | 964.72 ± 293.54 | 0.2 (0.2-0.5) | 0.4 ± 0.1 | 1.21 ± 0.43 | ||
Five-day | ARS | M | 188.03 ± 107.53 | 864.21 ± 444.42 | 0.1 (0.1-0.2) | 0.2 ± 0.03 | 3.08 ± 1.78 |
F | 179.43 ± 111.88 | 861.62 ± 580.92 | 0.1 (0.1-0.2) | 0.2 ± 0.05 | 3.47 ± 2.07 | ||
DHA | M | 1171.60 ± 613.77 | 2531.74 ± 1177.65 | 0.2 (0.2-0.3) | 0.4 ± 0.1* | 0.50 ± 0.32 | |
F | 893.01 ± 468.66 | 2008.96 ± 925.29 | 0.3 (0.1-0.3) | 0.4 ± 0.1 | 0.61 ± 0.32 | ||
M1 | M | 203.02 ± 226.62 | 219.10 ± 195.25 | 0.4 (0.3-0.5) | 0.6 ± 0.2† | 9.50 ± 12.08 | |
F | 282.03 ± 170.42 | 216.74 ± 100.50 | 0.5 (0.3-0.7)* | 0.9 ± 0.2† | 2.11 ± 1.31 | ||
DHA-G | M | 1105.48 ± 986.09 | 2396.47 ± 1827.67 | 0.2 (0.2-0.3) | 0.4 ± 0.1* | 0.82 ± 0.72 | |
F | 406.74 ± 135.55 | 1025.37 ± 484.94 | 0.2 (0.1-0.3) | 0.4 ± 0.2 | 1.20 ± 0.48 | ||