TABLE 2.
Pharmacokinetic parametera | Value for model at a dose (mg/kg) of: |
|||||||
---|---|---|---|---|---|---|---|---|
0.125 (thigh) | 0.25 (lung) | 0.5 (thigh) | 1 (lung) | 2 (thigh) | 4 (lung) | 8 (thigh) | 16 (lung) | |
Tmax (h) | 0.3 | 0.3 | 0.5 | 0.3 | 0.3 | 0.5 | 0.5 | 0.8 |
Cmax (ng/ml) | 175 | 319 | 650 | 1,470 | 2,460 | 4,400 | 5,820 | 12,600 |
Tlast (h) | 2 | 2 | 8 | 8 | 12 | 12 | 12 | 12 |
Clast (ng/ml) | 41.2 | 58.8 | 12.6 | 10.6 | 24.5 | 21.2 | 54.2 | 144 |
AUClast (h ng/ml) | 186 | 349 | 922 | 1,570 | 3,860 | 6,100 | 13,400 | 30,000 |
AUCINF (h ng/ml) | 234 | 403 | 946 | 1,580 | 3,920 | 6,210 | 13,500 | 30,400 |
CL/F (ml/h/kg) | 533 | 620 | 529 | 632 | 511 | 644 | 592 | 527 |
Vz/F (ml/kg) | 622 | 566 | 1,000 | 947 | 1,160 | 3,520 | 1,400 | 1,230 |
t1/2 (h) | 0.8 | 0.6 | 1.3 | 1 | 1.6 | 3.8 | 1.6 | 1.6 |
R2 | 0.997 | 0.992 | 0.918 | 0.919 | 0.86 | 0.986 | 0.954 | 0.916 |
Tlast, time of last quantifiable concentration; Clast, last quantifiable concentration; AUCINF, AUC to infinity; CL/F, apparent total clearance of drug after oral administration; Vz/F, apparent volume of distribution during terminal phase after oral administration; t1/2, half-life.