Table 2. Mean values for the pharmacokinetic parameters of active metabolite (dl-NBP) following intravenous administration of dl-PHPB and dl-NBP in Beagle dogs and SD rats (n=6, 3/sex).
Beagle dogs |
SD rats |
||||||||
---|---|---|---|---|---|---|---|---|---|
dl-PHPB | dl-NBP | dl-PHPB | dl-NBP | ||||||
2 mg/kg | 4 mg/kg | 8 mg/kg | 6.2 mg/kg | 5 mg/kg | 10 mg/kg | 20 mg/kg | 15.6 mg/kg | ||
A | μg/mL | 28.05 | 10.05 | 25.37 | 16.27 | 15.74 | 29.59 | 47.33 | 44.73 |
α | min−1 | 1.05 | 0.22 | 0.15 | 0.11 | 0.34 | 0.16 | 0.16 | 0.20 |
B | μg/mL | 0.80 | 4.64 | 1.02 | 3.63 | 4.47 | 1.54 | 1.47 | 1.89 |
β | min−1 | 0.07 | 0.06 | 0.02 | 0.05 | 0.06 | 0.02 | 0.02 | 0.02 |
V(c) | L/kg | 0.69 | 1.36 | 0.76 | 1.05 | 0.62 | 0.80 | 1.03 | 1.05 |
t(1/2)α | min | 0.66 | 3.19 | 4.75 | 6.34 | 2.04 | 4.31 | 4.33 | 3.52 |
t(1/2)β | min | 10.49 | 11.39 | 31.29 | 14.44 | 11.96 | 33.40 | 44.76 | 43.95 |
K21 | min−1 | 0.09 | 0.11 | 0.03 | 0.06 | 0.12 | 0.03 | 0.02 | 0.02 |
K10 | min−1 | 0.75 | 0.12 | 0.12 | 0.09 | 0.16 | 0.12 | 0.13 | 0.13 |
K12 | min−1 | 0.28 | 0.05 | 0.02 | 0.01 | 0.11 | 0.03 | 0.03 | 0.06 |
AUC | μg·min·mL−1 | 38.67 | 122.50 | 219.59 | 224.41 | 123.48 | 258.28 | 390.79 | 347.30 |
CL | L·kg−1·min−1 | 0.52 | 0.17 | 0.09 | 0.08 | 0.10 | 0.10 | 0.13 | 0.15 |