Table 3.
Tg-CYP2D6 | Wild-type | ||||||||
---|---|---|---|---|---|---|---|---|---|
Parameters | Units | i.v. 5 mg/kg | i.v. 15 mg/kg | i.p. 5 mg/kg | i.p. 15 mg/kg | i.v. 5 mg/kg | i.v. 15 mg/kg | i.p. 5 mg/kg | i.p. 15 mg/kg |
AUC0→∞ | min·μmol/L | 134 ± 19 | 544 ± 10 | 94.3 ± 9.5 | 359 ± 15 | 233 ± 34* | 682 ± 114 | 175 ± 28** | 662 ± 39*** |
CL | mL/min/kg | 176 ± 27 | 128 ± 2 | - | - | 102 ± 16* | 104 ± 16 | - | - |
Vss | L/kg | 4.41 ± 0.08 | 5.14 ± 0.46 | - | - | 5.74 ± 1.02 | 6.23 ± 0.57 | - | - |
Tmax | min | - | - | 6.67 ± 2.89 | 8.33 ± 5.77 | - | - | 5.83 ± 3.82 | 15.0 ± 5.0 |
Cmax | μmol/L | - | - | 3.82 ± 1.04 | 11.0 ± 1.0 | - | - | 3.02 ± 0.25 | 11.5 ± 1.3 |
t1/2 | min | 18.0 ± 2.9 | 36.5 ± 3.3 | 17.8 ± 2.7 | 19.1 ± 3.5 | 41.9 ± 11.7* | 43.1 ± 9.6 | 32.3 ± 10.7 | 35.5 ± 5.1* |
F | % | - | - | 68.6 ± 16.6 | 60.0 ± 2.4 | - | - | 73.7 ± 20.5 | 98.2 ± 10.1 |
p<0.05,
p<0.01,
p<0.001 compared with the corresponding values in Tg-CYP2D6 mice receiving the same treatment.