Table 4

Pharmacokinetic parameters for midazolam and 1′-hydroxymidazolam after single intravenous administration of midazolam (0.25 mg/kg) in wild-type and Tg-CYP3A4 mice

ParametersWild-TypeTg-CYP3A4Tg-CYP3A4/Wild-Type
Midazolam
C max(nmol/l)593 ± 113857 ± 3351.45
 AUC0–180 min(nmol · min/l)6460 ± 6018256 ± 8421.28
 AUC0–∞(nmol · min/l)6530 ± 758390 ± 8221.28
V ss(liter)2.00 ± 0.301.80 ± 0.300.90
 CLiv(l/min)0.120 ± 0.000.10 ± 0.000.83
 MRT (min)17.0 ± 4.7019.2 ± 1.701.13
T 1/2(min)14.3 ± 2.6020.8 ± 3.401.45
1′-OH-Midazolam
C max(nmol/l)135 ± 28.9185 ± 49.61.37
 AUC0–180 min(nmol · min/l)4750 ± 3679140 ± 16301.92

Values represent the mean ± S.D from three mice.