TABLE 3

Pharmacokinetic parameters of FEX following intravenous (1 mg/kg) or oral (5 mg/kg) administration of FEX with a concomitant oral dose of vehicle or KTZ (5, 20 mg/kg)

Each value represents the mean ± S.D. of four monkeys.



Intravenous (1 mg/kg FEX)

Oral (5 mg/kg FEX)

+Vehicle
+KTZ (20 mg/kg)
+Vehicle
+KTZ (5 mg/kg)
+KTZ (20 mg/kg)
Cmax (ng/ml) 269 ± 8 516 ± 218 350 ± 115
Tmax (h) 1.8 ± 0.5 2.3 ± 1.3 4.0 ± 2.8
t½ (h) 3.7 ± 0.2 4.1 ± 0.3 6.6 ± 1.0 5.1 ± 1.6 4.8 ± 2.4
CLtot (ml/h/kg) 385 ± 64 372 ± 75
Vdss (ml/kg) 302 ± 59 389 ± 102
AUCinf (h · ng/ml) 2469 ± 407 2592 ± 576 793 ± 97 1735 ± 337* 2077 ± 902
F (%) 6.6 ± 1.8 14.6 ± 5.1* 17.5 ± 9.9
Ratios (KTZ/Vehicle)
    Cmax 1.9 ± 0.8 1.3 ± 0.4
    AUCinf 2.2 ± 0.4 2.6 ± 1.1
    F



2.2 ± 0.4
2.6 ± 1.1
  • * p < 0.025, compared with the values in the monkeys coadministered with vehicle.