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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)

From: An investigation of the auto-induction of and gender-related variability in the pharmacokinetics of dihydroartemisinin in the rat

  AUC0-t(nmolhL-1) Cmax(nmolL-1) Tmax(h) MRT (h) CL/F (Lmin-1kg-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
  1. *: P < 0.05 (single dose compared with multiple dose); †: P < 0.05 (male rats compared with female rats).