TABLE 2

Kinetic parameters for the hepatic uptake of 16 drugs in rat hepatocytes in suspension

Values represent the mean ± S.D. of three to five experiments.

CompoundKmVmaxPdiffCLactiveCLactive/CLuptake
μMpmol/min/106 cellsμl/min/106 cells%
Atorvastatin4.03 ± 4.011340 ± 3205.35 ± 3.791500 ± 198098.5
Bosentan5.24 ± 1.56105 ± 8517.5 ± 4.418.7 ± 12.648.9
Cerivastatin5.17 ± 4.78804 ± 16823.7 ± 6.4285 ± 24786.7
Clarithromycin58.0 ± 47.92770 ± 247010.9 ± 4.150.7 ± 16.481.8
Erythromycin42.9 ± 13.9520 ± 35912.2 ± 4.411.4 ± 5.847.7
Fexofenadine7.41 ± 439885 ± 4746.75 ± 2.48167 ± 12694.3
Nateglinide4.83 ± 1.27834 ± 37316.6 ± 7.9179 ± 9690.7
Olmesartan53.0 ± 28.8514 ± 3260.863 ± 0.66410.6 ± 4.292.1
Pitavastatin6.30 ± 5.061070 ± 96018.8 ± 11.8197 ± 12187.9
Pravastatin30.5 ± 26.6789 ± 3851.67 ± 1.0231.7 ± 10.495.1
Repaglinide2.98 ± 1.28804 ± 34658.2 ± 44.2299 ± 12284.6
Ritonavir2.62 ± 1.842160 ± 1530118 ± 29873 ± 21687.5
Rosuvastatin6.05 ± 5.431250 ± 4007.08 ± 3.23418 ± 31997.7
Saquinavir51.7 ± 21.012,000 ± 7700191 ± 24239 ± 15252.1
Telmisartan3.85 ± 1.182220 ± 67028.1 ± 10.0630 ± 28694.5
Valsartan12.3 ± 13.0217 ± 2203.91 ± 2.3230.1 ± 32.479.4