Table 4. Preliminary Pharmacokinetic Parameters of 37 CD-1 Mouse Plasmaa.
|
37 |
||
|---|---|---|
| route of administration | IVb | POc |
| dose (mg/kg) | 0.5 | 2 |
| AUCinf [μM h] | 0.58 | 2.55 |
| Cmax [μM] | 0.58 | 0.58 |
| Tmax [h] | n/a | 1.00 |
| T1/2 [h] | 0.8 | 1.25 |
| Vdss [L/kg]d | 2.0 | n/a |
| MRT [h] | 1.01 | 3.01 |
| Cl [mL/min/kg] | 33.5 | n/a |
| F [%]e | 111% | |
Data presented as mean values. Three animals per arm, three animals per time point.
Dosed as a solution of the free base in 10% DMSO/90% 2-hydroxypropyl-beta-cyclodextrin (HPCD; 20% w/v).
Dosed as a solution of the free base in DMSO: methylcellulose (0.5% w/v).
Volume of distribution (Vd) calculated with the steady-state method.
Calculation for F [%] is calculated relative to IV and assumes clearance does not change from that calculated for IV. Thus, calculated values >100 can arise where compound adsorption and/or elimination is dramatically different following PO versus IV.