TABLE 3

Parameters defining relative importance of active uptake and cellular binding in hepatic uptake of 16 drugs in rat hepatocytes in suspension

CompoundCLactive/PdiffKpuaKptotalfucell
Atorvastatin493 ± 651494 ± 6518781b0.056
Bosentan1.06 ± 0.562.06 ± 0.56150 ± 370.013
Cerivastatin13.1 ± 11.014.1 ± 11.0353b0.039
Clarithromycin5.05 ± 2.296.05 ± 2.29250 ± 220.024
Erythromycin1.00 ± 0.492.00 ± 0.4941 ± 90.05
Fexofenadine24.5 ± 19.425.5 ± 19.4245 ± 200.10
Nateglinide11.4 ± 5.412.4 ± 5.4250 ± 510.05
Olmesartan23.1 ± 27.524.1 ± 27.538 ± 100.62
Pitavastatin21.9 ± 29.222.9 ± 29.2800 ± 590.028
Pravastatin21.9 ± 8.222.9 ± 8.2149b0.15
Repaglinide6.94 ± 3.957.94 ± 3.95220 ± 430.036
Ritonavir7.94 ± 3.378.94 ± 3.37616c0.015
Rosuvastatin57.2 ± 11.958.2 ± 32.8125 ± 160.48
Saquinavir1.34 ± 1.062.34 ± 1.06306c0.0075
Telmisartan26.6 ± 16.127.6 ± 16.1680 ± 260.04
Valsartan7.69 ± 6.238.69 ± 6.2350 ± 360.17
  • a Calculated from CLuptake/Pdiff.

  • b Calculated using the regression equation logfucell = 0.9161 − 0.2567 logD7.4.

  • c From Parker and Houston (2008).