Table 5.
Species | Dose (mg/kg) | Route | Tmax (h) | AUC0→t (ng h/mL) | CLP (L/h/kg)a | CLB (L/h/kg)b | VssP (L/kg)a | VssB (L/kg)b | T1/2 (h) | F |
---|---|---|---|---|---|---|---|---|---|---|
Mouse | 10 | IV | 0.25 | 6,636 | 1.50 | 1.78 | 1.51 | 1.79 | 0.80 | |
50 | PO | 17,004 | 4.29 | 51 | ||||||
Rat | 2 | IV | 1.00 | 1,877±242 | 1.06±0.14 | 0.83±0.11 | 1.75±0.29 | 1.38±0.23 | 1.30±0.30 | |
10 | PO | 6,406±1,556 | 4.81±0.90 | 68±17 | ||||||
Dog | 2 | IV | 2.00 | 1,007±18 | 1.87±0.07 | 2.23±0.08 | 4.65±0.13 | 5.54±0.15 | 2.33±0.67 | |
50 | PO | 5,178±3,923 | 6.71±5.44 | 21±16 | ||||||
Monkey | 2 | IV | 6 | 2,031±326 | 0.49±0.09 | – | 3.57±0.71 | – | 6.82±0.90 | |
5 | PO | 2,578±1,615 | 4.56±0.50 | 25±15 |
Notes:
CLP and VssP were derived from analysis of the plasma concentration–time data.
CLB (L/h/kg) and VssB (L/kg) were calculated using the plasma parameter and blood/plasma values from in vitro studies.
Abbreviations: h, hour; IV, intravenous; CL, clearance.