Table 4. Full Pharmacokinetic Parameters of Compound 27 Compared to Compound 2 at a Dose of 10 mg/kg.
compd (route) | AUC0–lasta (μg·min/mL) | AUC0–∞b (μg·min/mL) | Cmaxc (μg/mL) | Tmaxd (h) | CLe (mL min–1 kg–1) | Vdf (L/kg) | t1/2g | Fh (%) |
---|---|---|---|---|---|---|---|---|
27 (iv) | 1540 | 1570 | 6.4 | 3.58 | t1/2α = 3.6 min | |||
t1/2β = 6.5 h | ||||||||
27 (po) | 552 | 582 | 2.7 | 0.5 | t1/2α = 2.4 h | 37 | ||
t1/2β = 6.6 h | ||||||||
2 (iv)i | 1180 | 1460 | 6.9 | 0.30 | t1/2α = 35.2 min | |||
t1/2β ≥ 20 h | ||||||||
2 (po)i | 408 | 738 | 1.3 | 1 | t1/2α = 1.9 h | 50 | ||
t1/2β > 20 h |
AUC0–last = area under the curve from 0 min to the last quantifiable time point.
AUC0–-∞ = area under the curve from 0 min extrapolated to infinity.
Cmax = maximum concentration.
Tmax = time at which maximum concentration is achieved.
CL = clearance.
Vd = volume of distribution.
t1/2α = half-life of distribution. t1/2β = half-life of elimination.
F = oral bioavailbility.
Data for compound 2 reproduced from Bouley et al. for comparison.