Single-dose pharmacokinetic proportionality study of PNU-288034 in rats
Indicated doses were administered to rats by oral gavage. Plasma was collected to 24 h after dose and analyzed by LC-MS/MS. Pharmacokinetic parameters were calculated from concentration-time curves as described under Materials and Methods.
| Dose | Cmax | Tmax | t1/2 | MRT | AUC0-∞ | Unchanged in Urine | F |
|---|---|---|---|---|---|---|---|
| mg/kg | μg/ml | h | h | h | μg × h/ml | % | % |
| 21.3 | 9.10 ± 2.0 | 0.5 ± 0.0 | 5.9 ± 1.4 | 2.63 ± 0.26 | 13.9 ± 0.8 | 73.2 ± 6.4 | 73.3 ± 9.3 |
| 30.6 | 10.9 ± 9.2 | 0.25 ± 0.00 | 9.6 ± 2.4 | 6.70 ± 4.5 | 24.1 ± 4.3 | 72.5 ± 0.8 | 88.0 ± 19 |
| 60 | 15.1 ± 1.6 | 0.75 ± 0.35 | 7.3 ± 3.4 | 3.78 ± 0.80 | 42.5 ± 3.9 | 63.9 ± 4.0 | 79.5 ± 6.0 |
| 107.9 | 20.7 ± 0.4 | 0.38 ± 0.18 | 5.9 ± 3.5 | 4.50 ± 1.1 | 55.8 ± 8.6 | 50.8 ± 2.4 | 53.2 ± 8.0 |