Table 3

CL and AUC profiles of E1S and E1 in PP and PV hepatocyte (n = 5) incubation systems

E1S μMAUC of E1SCLapp of E1S3-aAUC of E1
Cellular3-bExtracellular3-bExtracellular3-cCellular3-bExtracellular3-b
μM · min/106 cells ml/min/106cells μM · min/106 cells
AUC Embedded Image (0 → 30 min)AUC Embedded Image (0 → 30 min)AUC Embedded Image (0 → ∞)AUC Embedded Image (0 → 30 min)AUC Embedded Image (0 → 30 min)
PP
   174  ± 312.6  ± 0.93.0  ± 1.10.34  ± 0.1260  ± 270.71  ± 0.24
   5560  ± 14718  ± 3.320  ± 3.90.25  ± 0.05300  ± 1526.2  ± 1.7
  253,668  ± 1,123215  ± 27236  ± 300.106  ± 0.0142,052  ± 1,73857  ± 14
 12518,704  ± 7,1022,372  ± 3252,634  ± 3650.047  ± 0.0075,363  ± 2,272179  ± 79
PV
   161  ± 142.5  ± 1.42.7  ± 1.60.37  ± 0.2142  ± 290.35  ± 0.103-150
   5432  ± 16117  ± 8.219  ± 9.10.26  ± 0.12222  ± 1133.7  ± 0.943-150
  253,366  ± 1,340212  ± 75227  ± 810.11  ± 0.041,755  ± 1,20842  ± 15
 12518,908  ± 4,4892,363  ± 3222,586  ± 3640.048  ± 0.0075,166  ± 2,400174  ± 45
  • 3-150  Statistically different from periportal data (ANOVA,P < 0.05).

  • 3-a  CLapp = [dose/AUC Embedded Image (0 → ∞)].

  • 3-b  AUC of 0 to 30 min, estimated by trapezoidal method.

  • 3-c  AUC of 0 min to infinity; the AUC up to 30 min was estimated using trapezoidal method, and this was added to C30/ k (concentration at 30 min divided by the first order decay constant, k), assuming log-linear decline.