Accuracy of clearance predictions from liver microsomal in vitro T1/2 values including and excluding values for blood binding and microsome binding
Average Fold Error (predicted CLblood/actual CLblood) | ||||
---|---|---|---|---|
Basic compounds only (n = 12) | Neutral compounds only (n = 8) | Acidic compounds only (n = 9) | All compounds (n = 29) | |
Well-stirred model | ||||
No binding considered (eq. 1) | 1.37 | 1.99 | 5.05 | 2.28 |
Including fu(blood) (eq. 2) | 5.17 | 3.90 | 3.91 | 4.39 |
Including fu(blood) and fu(mic) (eq.3) | 1.86 | 2.55 | 2.83 | 2.31 |
Parallel-tube model | ||||
No binding considered (eq. 4) | 1.31 | 1.99 | 5.35 | 2.28 |
Including fu(blood) (eq.5) | 4.75 | 3.90 | 3.79 | 4.20 |
Including fu(blood)and fu(mic) (eq. 6) | 1.60 | 2.53 | 2.74 | 2.14 |