Table 1 The main pharmacokinetic parameters of dihydroartemisinin (DHA) and its phase I/II metabolites (M1 and DHA-G) after one-day and five-day oral administrations of DHA (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/kg) | |||
|---|---|---|---|---|---|---|---|
One-day | DHA | M | 1110.35 ± 724.56† | 2062.22 ± 1364.13† | 0.3 (0.2-0.5) | 0.6 ± 0.1 | 0.75 ± 0.45† |
F | 322.16± 159.67† | 562.71 ± 273.86† | 0.3 (0.2-0.5) | 0.6 ± 0.1 | 2.36 ± 1.40† | ||
M1 | M | 1202.13± 418.50† | 996.67 ± 244.81† | 0.4 (0.3-0.5)† | 1.0 ± 0.1† | 0.53 ± 0.14† | |
F | 191.46 ± 189.95† | 180.02 ± 158.28† | 0.5 (0.3-0.7)† | 0.7 ± 0.1† | 5.48 ± 3.98† | ||
DHA-G | M | 855.69 ± 789.17† | 1443.21 ± 1222.24† | 0.3 (0.2-0.5) | 0.6 ± 0.2† | 1.78 ± 1.98† | |
F | 58.16 ± 40.88† | 236.11 ± 232.63† | 0.2 (0.2-0.3) | 0.3 ± 0.1† | 10.43 ± 5.63*† | ||
Five-day | DHA | M | 1512.55 ± 950.76† | 2605.58 ± 1677.94† | 0.4 (0.2-0.7) | 0.8 ± 0.3 | 0.72 ± 0.82† |
F | 212.63 ± 202.33† | 378.05 ± 289.44† | 0.3 (0.2-0.3) | 0.6 ± 0.1 | 4.43 ± 2.83† | ||
M1 | M | 2034.92± 903.13† | 1102.67 ± 478.42† | 0.5 (0.3-0.7) | 1.3 ± 0.2† | 0.35 ± 0.19† | |
F | 157.11 ± 249.88† | 153.58 ± 229.01† | 0.6 (0.5-0.7) | 0.7 ± 0.1† | 8.77 ± 6.61† | ||
DHA-G | M | 907.28 ± 542.38† | 1155.90 ± 609.47† | 0.3 (0.2-0.7) | 1.0 ± 0.6† | 0.82 ± 0.39† | |
F | 19.33 ± 15.27† | 125.30 ± 58.48† | 0.2 (0.2-0.2) | 0.2 ± 0.1† | 20.49 ± 2.58† | ||