TABLE 1

Physicochemical and pharmacokinetic parameters of midazolam used for simulation

Parameters (U)
Mol. wt.325.77Vc (L/kg)0.326
logP3.25aK12 (1/h)1.57
fu,p (%)3.1a (2.32b)K21 (1/h)1.05
Blood/plasma conc. ratio0.55aV2 (L/kg)0.489
Peff (cm/s × 10−4)6.73aCYP3A_Km (μg/ml)0.896c
Solubility (mg/ml)0.082dCYP3A_Vmax, liver (mg/s)0.373c
CYP3A_Vmax, gut (mg/s)0.184e

  • ↵a Gertz et al. 2011.

  • ↵b The value was adjusted by GastroPlus for possible binding to plasma lipids.

  • ↵c Thummel et al. (1996), the values were converted using the unit converter in GastroPlus.

  • ↵d Andersin (1991), pH 6.39.

  • ↵e Vmax for intestinal CYP3A was adjusted to achieve the observed Fg (0.54).