Kinetic parameters for in vitro biliary excretion of unlabeled compounds in SCRH Data are taken from Fig. 3. All compounds were tested at 1 μM except for pravastatin at 10 μM. Intrinsic uptake clearance (CLuptake, int), intrinsic biliary clearance (CLbile, int), and BEI of test compounds were calculated from eqs. 1, 2, and 3, respectively, as described under Materials and Methods. CLbile, int and BEI were determined at 10 min. Each value represents the mean ± S.E.M. (n = 6).
CLuptake,int | CLbile,int | BEI | |||||
|---|---|---|---|---|---|---|---|
| μl/min/mg protein | ml/min/kg | μl/min/mg Protein | ml/min/kg | % | |||
| Pravastatin | 8.11 ± 0.69 | 64.9 ± 5.5 | 1.08 ± 0.48 | 8.7 ± 3.8 | 27.1 ± 11.7 | ||
| Rosuvastatin | 62.49 ± 11.03 | 499.9 ± 88.2 | 15.56 ± 5.79 | 124.5 ± 46.3 | 39.5 ± 11.1 | ||
| Valsartan | 17.85 ± 0.98 | 142.8 ± 7.8 | 3.50 ± 1.98 | 28.0 ± 15.9 | 15.5 ± 11.2 | ||
| Cefmetazole | 1.50 ± 0.06 | 12.0 ± 0.5 | 0.005 ± 0.019 | 0.04 ± 0.16 | 0.1 ± 4.5 | ||
| Cefoperazone | 0.39 ± 0.02 | 3.1 ± 0.1 | 0.07 ± 0.01 | 0.5 ± 0.1 | 30.8 ± 5.7 | ||
| Taurocholic acid | N.C. | N.C. | 6.37 ± 0.81 | 50.9 ± 6.5 | 76.8 ± 2.3 | ||
N.C., not calculated