Summary of input parameters for telmisartan PBPK model
| Parameters | Values (CV) | Sources |
|---|---|---|
| LogD7.4 | 2.5 | In-house data |
| pKa | 3.8 | In-house data |
| Blood/plasma ratio (RB/P) | 0.78 | (Stangier et al., 2000a) |
| Erythrocyte/plasma ratio (RE/P) | 0.5 | (Stangier et al., 2000a) |
| Unbound fraction in plasma (fu, p) | 0.005 | (Stangier et al., 2000b) |
| Unbound fraction in human liver tissue (fu, liver) | 0.013 (16%) | In-house data |
| CLu, int, met (μl/min per milligram microsomal protein) | 1210 (32%) | In-house HLM with BSA data |
| CLu, int, act (μl/min per 106 cells) | 53 (53%) | This study |
| CLu, int, pass (μl/min per 106 cells) | 72 (43%) | This study |
| CLu, int, bile (μl/min per 106 cells) | 3 (84%) | This study |
| Unbound fraction of glucuronide in human liver tissue (fu, liver, glu) | 0.0073 (15%) | In-house data |
| CLu, int, bile, glu (μl/min per 106 cells) | 74 (16%) | This study |
BSA, bovine serum albumin.