Accuracy of prediction for in vivo changes in Clm,u, Clpo,u and Clpo for (S)-warfarin by coadministration of bucolome assessed as ratios of the respective Cl values in the presence to those in the absence of bucolome (expressed as %)
| Predicted from In Vitro Data Obtained from | Observed in Patients | ||
|---|---|---|---|
| Human liver microsomes | CYP2C9 | ||
| Clm,u(B)/Clm,u | 4.9a, 33.9b | 2.0a, 17.3b | 10.9 (1.8–23.2) |
| Clpo,u(B)/Clpo,u | 17.2a, 42.5b | 14.8a, 28.1b | 15.9 (8.1–28.2) |
| Clpo(B)/Clpo | 37.5a, 89.5b | 32.4a, 59.7b | 30.4 (15.6–53.7) |
Data were obtained with use of Iu that were calculated with 10a (an active transport factor) and 1b(no assumptive active transport of bucolome into the hepatocytes) as A in eq. 9. Data in parenthesis are the 95% confidence intervals for the respective ratios obtained from patients. Detailed description for the equations used for calculating the ratios for the respective clearance values is given in the text.