Table 5.
Pharmacokinetic profile of MK-5172 in rat and doga
| Dosing method and species | Dose (mg/kg) | CLp (ml/min/kg) | V (liters/kg) | t1/2 (h) | AUC0-∞ (μM · h) | Cmax (μM) | C24h (μM) | Tmax (h) | %F | 24-h liver concn (μM) |
|---|---|---|---|---|---|---|---|---|---|---|
| i.v. | ||||||||||
| Rat | 2 | 28 ± 22 | 3.1 ± 2.6 | 1.4 ± 0.6 | 2.3 ± 1.6 | |||||
| Dog | 0.5 | 5 ± 2 | 0.7 ± 0.1 | 3.0 ± 0.8 | 2.0 ± 0.7 | |||||
| p.o. | ||||||||||
| Rat | 5 | 0.7 ± 0.3 | 0.3 ± 0.1 | < 0.005 | 4.0 ± 0.0 | 13 | 0.2 | |||
| Dog | 1 | 0.4 ± 0.3 | 0.1 ± 0.1 | 0.04 | 4.7 ± 1.2 | 12 ± 9 | 1.4 |
a
Values are means and standard deviations. i.v., intravenous; p.o., oral; CLp, plasma clearance; V, volume of distribution; t1/2, half-life; AUC0-∞, area under the concentration-time curve from 0 h to infinity; Cmax, maximum concentration of the drug; C24h, concentration of the drug at 24 h; Tmax, time to maximum concentration of the drug; %F, oral bioavailability.