Table 1 Comparison of main pharmacokinetic parameters of [14C] dihydroartemisinin (DHA) in plasma and blood, as well as unchanged DHA in plasma at 3 mg/kg, in rats following a single intravenous dose
14C-Dihydroartemisinin 3 mg/20 μCi/kg | Unchanged DHA 3 mg/kg | ||
|---|---|---|---|
Parameters | Plasma Three-compartment | Blood Three-compartment | Plasma Two-compartment |
Cmax (ng/ml) | 3446 ± 396 | 3105 ± 430 | 1999 ± 507 |
Tmax (hr) | 0.02 | 0.02 | 0.02 |
AUCinf. (ng*h/ml) | 21014 ± 2718 | 52690 ± 4971 | 933.2 ± 125.4 |
t1/2 – alpha (hr) | 0.21 ± 0.05 | 0.18 ± 0.02 | 0.25 ± 0.04 |
t1/2 – beta (hr) | 15.49 ± 1.64 | 19.68 ± 3.88 | 1.03 ± 0.19 |
t1/2 – gamma (hr) | 75.57 ± 7.34 | 122.13 ± 8.73 | - |
CL (ml/hr/kg) | 144.63 ± 18.17 | 43.58 ± 30.70 | 3350.02 ± 423.37 |
Vss (ml/kg) | 8216 ± 828 | 10792 ± 3771 | 1658 ± 540 |
MRT (hr) | 57.00 ± 2.84 | 148.57 ± 90.24 | 0.49 ± 0.12 |
Cmax at first peak (ng/ml) | 3446 ± 396 (0.02 h) | 3105 ± 430 (0.02 h) | 1999 ± 507 (0.02 h) |
at second peak (ng/ml) | 2373 ± 195 (0.19 h) | 1557 ± 955 (0.94 h) | 1638 ± 468 (0.38 h) |
at third peak (ng/ml) | 863 ± 537 (1.70 h) | 978 ± 164 (2.00 h) | - |
at fourth peak (ng/ml) | 584 ± 65.5 (6.00 h) | 833 ± 99 (6.00) | - |