Table 2

Pharmacokinetic parameters defining systemic disposition of SB-250231 in the monkey following intravenous, intraportal, and intraduodenal administration

ParameterIntravenousIntraportalIntraduodenal2-b
Portal SamplesSystemic Samples
Dose (mg/kg)1.39  ± 0.021.39  ± 0.022.68 ± 0.01
CL (ml/min/kg)12.9  ± 4.702-a
AUC (min · μg/ml)115  ± 4842.0  ± 28.1255, 2282-b 101, 96.02-b
DNAUC (min · kg/l)82.8  ± 34.130.5  ± 20.794.9, 85.02-b 37.6, 35.82-b
VdSS(l/kg)0.855  ± 0.825
MRT (min)58.7  ± 37.548.0  ± 12.374.5, 1452-b
t½ (min)60.9  ± 34.238.9  ± 4.565.6, 1562-b
Eh (%)35.0  ± 10.5
F (%)31.7, 70.22-b

Data are presented as mean ± S.D. of three monkeys, unless otherwise noted.

  • CL, clearance; MRT, mean residence time.

  • 2-a  —, parameter not determined for this route of administration.

  • 2-b  One monkey demonstrated sampling difficulties during the intraduodenal leg of the experiment; the data from that animal are excluded for this study leg.