Table 4. Pharmacokinetic Parameters for 13 and 19 Estimated in Blood in CD-1 Micea.
| area under curve AUC0-t (μg/h/mL) |
|||||||
|---|---|---|---|---|---|---|---|
| compd no. | clearance (mL/min/kg) | volume of distribution (L/kg) | half-lifeb (h) | maximum concn Cmaxc (μg/mL) | iv | po | oral bioavailability (% F) |
| 13d | 29.7 | 6.47 | 2.77 | 2.34 | 0.596 | 9.71 | 81 |
| 19e | 14.3 | 11.9 | 10.2 | 1.09 | 2.23 | 13.6 | 55 |
Dosing 2 mg/kg iv and 20 mg/kg po into CD-1 mice (n = 4 for both arms).
iv.
po.
iv vehicle 20% (v:v) encapsine in water, po vehicle 1% (w:v) methylcellulose in water.
iv vehicle 3% solutol, 7% PEG (v:v) in saline, po vehicle 1% (w:v) methylcellulose in water.