Uptake and metabolism kinetic parameters of telmisartan estimated in rat hepatocytes by using an extended two-compartment mechanistic model
Uptake kinetics was measured in freshly isolated rat hepatocytes plated for 2 h over 2 min or 90 min at nine concentrations (0.1–100 μM). Data represent mean of three experiments ± S.D.
| Extended Two-Compartment Model | ||
|---|---|---|
| 2 Min (n = 3) | 90 Min (n = 1) | |
| Km,u, μM | 5.96 ± 3.23 | 8.65 |
| Vmax, pmol/min/106 cells | 774 ± 208 | 482 |
| Pdiff,u, μl/min/106 cells | 41.6 ± 12.9 | 17.2 |
| fucell | 0.026 ± 0.019 | 0.002 |
| CLactive,u, μl/min/106 cells | 154 ± 68.8 | 55.7 |
| CLmet,gluc,u, μl/min/106 cells | 38.9 ± 38.8 | 37.5 |
| Maximal proportion of active transport, % | 78.7 ± 13.8 | 76.4 |