TABLE 5

Pharmacokinetic parameters of MDZ after oral administration (1 mg/kg) of MDZ in the absence and presence of AZM

Each value, with the exception of Tmax, represents the geometric mean (geometric coefficient of variation) of four monkeys. The Tmax values represent the median (minimum, maximum) of four monkeys.

Day −7Day 1Day 3Day 4Day 9
C max (ng/ml)20 (0.31)38** (0.17)45** (0.22)31* (0.41)16 (0.19)
T max (h)1.5 (1.0, 2.0)1.5 (0.5, 2.0)1.0 (0.5, 3.0)1.0 (0.5, 2.0)1.0 (1.0, 2.0)
CL/F(ml/h/kg)19,512 (0.24)12,505 (0.37)10,641* (0.50)15,251 (0.54)26,953 (0.28)
AUC(h · ng/ml)51 (0.24)80 (0.37)94* (0.50)66 (0.54)37 (0.28)
Ratios to control (day −7)
C max 2.02.31.60.8
CL/F0.70.60.81.4
AUC1.62.01.40.7
  • * p < 0.05 and

  • ** p < 0.001 compared with control values obtained on day −7.