Table I.
Route | Compound | t (h) | AUCinf (μg h/L) | Volume of Distribution L/kg | Clearance (L h−1 kg−1) | % Dose Excreted | Bioavailability (%) | |
---|---|---|---|---|---|---|---|---|
Urine | Feces | |||||||
IV | Lee 562 | 1.30 ± 0.89 | 956 ± 442 | 28.9 ± 29.4 | 12.9 ± 7.6 | 0.001 ± 0.0003 | 0.001 ± 0.001 | |
Lee 878 | 2.63 ± 0.35 | 19,091 ± 1,724 | 2.00 ± 0.36 | 0.527 ± 0.05 | ND | ND | ||
Lee 952 | 7.34 ± 2.27 | 1,846 ± 82.2 | 58.0 ± 20.1 | 5.42 ± 0.24 | ND | ND | ||
Lee 1106 | 10.3 ± 1.41 | 22,423 ± 4,096 | 6.72 ± 1.10 | 0.456 ± 0.07 | 0.035 ± 0.01 | 0.14 ± 0.06 | ||
Oral | Lee 562 | 3.69 ± 0.86 | 1,519 ± 458 | 386 ± 187 | 71.6 ± 23.2 | 0.009 ± 0.02 | 0.023 ± 0.02 | 15.9 ± 4.8 |
Lee 878 | ND | 52,324 ± 14,834b | ND | 2.07 ± 0.71c | ND | ND | 27.4 ± 7.8c | |
Lee 952 | 3.39 ± 1.16a | 2,936 ± 1,119 | 192 ± 127 | 37.7 ± 12.5 | ND | ND | 15.9 ± 6.1 | |
Lee 1106 | 9.24 ± 1.71 | 10,230 ± 9,101 | 231 ± 174 | 16.0 ± 10.3 | 0.025 ± 0.02 | 11.8 ± 7.09 | 4.6 ± 4.1 |
ND Not determined
aNot reliable determined due to limited log-linear phase
bAUC0–48 h
cAUC0–48 h was used for calculation of clearance and oral bioavailability