Unbound fractions of tolbutamide and gemfibrozil in incubation buffers containing human liver microsomes and different concentrations of Hsa and Hlc
| Matrix | Tolbutamide2-a | Gemfibrozil2-a |
|---|---|---|
| Buffer control | 1.0 | 0.98 |
| Microsomes (0.1 mg/ml) | 1.0 | 0.97 |
| Hsa (mg/ml) | ||
| 0.5 | 0.82 | 0.69 |
| 1 | 0.67 | 0.28 |
| 2 | 0.55 | 0.15 |
| 5 | 0.36 | 0.07 |
| Hlc (mg/ml) | ||
| 0.5 | 0.94 | 0.96 |
| 1 | 0.93 | 0.97 |
| 2 | 0.92 | 0.88 |
| 5 | 0.85 | 0.82 |
| Hsa (5 mg/ml) + Hlc (0.5 mg/ml) | 0.38 | 0.08 |
↵2-a Data are expressed as unbound fractions (mean of duplicate determinations) determined at a spiked drug concentration of 50 μM.