Table 7. Pharmacokinetic Parameters in Male C57/BL6 Mouse Blooda.
| route of administration | i.v. | oral | i.v. | oral | i.v. | oral |
|---|---|---|---|---|---|---|
| 12 | 47 | 40 | ||||
| dose (mg/kg) | 2 | 20 | 2 | 20 | 2 | 20 |
| apparent t1/2 (h) | 3.1 | 4 | 5.6 | 4.4 | 4.0 | 6.1 |
| CLtotal (mL/min/kg) | 2.7 | 80.9 | 0.4 | |||
| CLint (mL/min/kg) | 476 | >4000 | 34 | |||
| Vd (L/kg) | 0.7 | 37.4 | 0.1 | |||
| Cmax (μM) | 29.1 | 65.6 | 2.4 | 2.9 | 33.1 | 104.5 |
| Tmax (h) | 0.5 | 0.5 | 1.0 | |||
| AUC0–∞ (min·μM) | 2928 | 12004 | 91 | 313 | 15373 | 65417 |
| oral bioavailability F (%) | 41 | 33 | 44 | |||
a
i.v.: intravenous; t1/2: elimination half-life; CLtotal: total blood clearance; CLint: intrinsic clearance; Vd: volume of distribution during elimination phase; Cmax, maximum (peak) plasma concentration following oral administration; and AUC: area under the curve.