Table 1

Hepatobiliary disposition of APAP, AG, and AS in isolated single-pass perfused rat livers at steady-state

WistarTR
Excretion rate (pmol/min)
 Rbile_AG 174  ± 110.34  ± 0.021-150
 Rbile_AS 37  ± 211  ± 11-150
 RB/L_AG 175  ± 61428  ± 181-150
 RB/L_AS 909  ± 851039  ± 6
Biotransformation
 ER of APAP0.30  ± 0.020.30  ± 0.02
 AG %12.1  ± 3.314.3  ± 0.9
 AS %32.3  ± 2.135.2  ± 3.5
Concentration in liver (mM)
 Cliver_AG 0.613  ± 0.0660.415  ± 0.0281-150
 Cliver_AS 0.356  ± 0.0560.526  ± 0.1101-150
Clearance (μl/min)
 CLbile_AG 285  ± 371.67  ± 0.211-150
 CLbile_AS 106  ± 1216  ± 11-150
 CLB/L_AG 289  ± 1072110  ± 3591-150
 CLB/L_AS 1-b 2575  ± 2601510  ± 1301-150

Rbile_AG and Rbile_AS are biliary excretion rates for AG and AS, respectively; RB/L_AGand RB/L_AS are basolateral export rates for AG and AS, respectively; ER is the extraction ratio; AG% and AS% are the percentages of the dose recovered as AG and AS, respectively; Cliver_AG and Cliver_AS are the AG and AS concentrations at the end of perfusion. CLbile_AG, CLbile_AS, and CLB/L_AG are AG biliary clearance, AS biliary clearance, and AG basolateral clearance, respectively.1-a

  • 1-a  Mean ± S.D.,n = 3 for each group.

  • 1-b  Apparent as basolateral clearance.

  • 1-150P < 0.01, control vs. TR.