Table 5.
Toxicokinetic parameters of hydroxychloroquine and artemisinin in rats after oral administration.
| Analyte | Gender | Doses (mg/kg) | C max (ng/mL) | AUC0−t (h × ng/mL) | Accumulation coefficient of Cmax | Accumulation coefficient of AUC | ||
|---|---|---|---|---|---|---|---|---|
| Day 1 | Day 14 | Day 1 | Day 14 | |||||
| Hydroxychloroquine | Female + male | 46 | 308.5 ± 87.7 | 346.0 ± 179.8 | 2859.0 ± 656.2 | 4274.9 ± 1083.2∗ | 1.1 | 1.5 |
| 219 | 616.7 ± 521.8 | 590.4 ± 169.6 | 4284.0 ± 916.1 | 7749.1 ± 1826.0∗ | 1.3 | 1.9 | ||
| 328 | 400.3 ± 155.8 | 631.5 ± 104.4∗ | 5408.3 ± 1463.5 | 9287.9 ± 1279.7∗ | 1.8 | 1.8 | ||
| 492 | 565.6 ± 301.6 | 826.0 ± 253.7∗ | 7086.1 ± 1718.3 | 11660.3 ± 2242.7∗ | 1.6 | 1.7 | ||
|
| ||||||||
| Artemisinin | Female | 46 | 154.8 ± 119.1 | 46.9 ± 24.3 | 161.6 ± 86.8 | 83.8 ± 37.6 | 0.4 | 0.6 |
| 219 | 319.3 ± 97.3 | 150.8 ± 218.6 | 369.3 ± 104.4 | 138.4 ± 89.2 | 0.5 | 0.4 | ||
| 328 | 341.5 ± 293.7 | 38.1 ± 17.3 | 451.9 ± 434.2 | 85.7 ± 26.0 | 0.3 | 0.6 | ||
| 492 | 270.8 ± 128.1 | 84.2 ± 48.8∗ | 379.3 ± 370.8 | 224.9 ± 110.1 | 0.3 | 0.8 | ||
| Male | 46 | 2.8 ± 2.4 | 7.1 ± 2.1 | 2.9 ± 2.4 | 15.1 ± 4.0 | 1.8 | 2.5 | |
| 219 | 12.7 ± 5.5 | 12.3 ± 4.5 | 10.1 ± 4.0 | 25.0 ± 11.6 | 1.1 | 2.9 | ||
| 328 | 10.9 ± 5.0 | 7.5 ± 4.9 | 21.2 ± 10.8 | 12.2 ± 9.3 | 0.8 | 0.7 | ||
| 492 | 39.3 ± 54.3 | 23.3 ± 22.9 | 37.7 ± 23.7 | 19.4 ± 11.0 | 2.3 | 0.6 | ||
∗ P ≤ 0.05 significant difference from day 1.