TABLE 3.
Uptake kinetic parameters of rosuvastatin estimated in three human hepatocyte donors using a mechanistic two-compartment model
Uptake kinetics was measured in cryopreserved human hepatocytes plated for 6 h over 2 min at seven concentrations (0.1–300 μM).
Donor | Km, u | Vmax | Pdiff, u | fumed | CLactive, u |
---|---|---|---|---|---|
μM | pmol · min−1 · 106 cells−1 | μl · min−1 · 106 cells−1 | μl · min−1 · 106 cells−1 | ||
HU4122 | 11.2 | 104 | 0.391 | 0.80 | 9.21 |
HU4199 | 9.80 | 16.6 | 0.148 | 1 | 1.69 |
HU8089 | 12.0 | 16.3 | 0.243 | 0.96 | 1.35 |
Mean ± S.D. | 11.0 ± 1.1 | 45.5 ± 50.3 | 0.261 ± 0.123 | 0.93 ± 0.13 | 4.09 ± 4.44 |