TABLE 5.
Route of administration | Dose (mg/kg) | CLobs (ml/min/kg) | t1/2 (h) | Tmax (h) | Cmax (ng/ml) | AUClast (ng · h/ml) | AUCinf (ng · h/ml) | AUCextrap (%) | Vss,obs (liters/kg) | F (%) | 24-h liver concn/plasma concn ratio |
---|---|---|---|---|---|---|---|---|---|---|---|
i.v. | 2 | 31 | 1.1 | NA | 930 | 1,120 | 1,122 | 0 | 2 | <LLOQ | |
p.o. | 10 | 3.4 | 0.33 | 490 | 1,994 | 2,238 | 10 | 40 | <LLOQ | ||
p.o. | 30 | 3.2 | 1.67 | 1,028 | 5,832 | 6,174 | 5 | 37 | <LLOQ | ||
p.o. | 100 | 5.9 | 0.50 | 2,709 | 23,024 | 25,232 | 8 | 45 | 2.9 |
Values are means (n = 3 per group). CLobs, observed clearance; t1/2, half-life; Tmax, time to maximum concentration; Cmax, maximum concentration; AUClast, area under the concentration-time curve at 1 h after the last dose; AUCinf, area under the concentration-time curve from 0 h to infinity; AUCextrap, extrapolated area under the concentration-time curve; Vss,obs, observed volume of distribution at steady state; F, bioavailability; NA, not applicable; LLOQ, lower limit of quantitation.