Table 7.
Human Microsomal Stability of 24b and 25b.
Compound | Human Liver Microsome |
||||
---|---|---|---|---|---|
R2 | T1/2 (min) | CLint(mic) (μL/min/mg) |
CLint(liver) (mL/min/kg) |
Remaining (T=60min) |
|
24b | 0.9412 | 80.1 | 17.3 | 15.6 | 55.8% |
25b | 0.9322 | 32.7 | 42.4 | 38.2 | 23.8% |
K-5a2 | 0.9973 | 2.4 | 577.3 | 519.6 | 0.8% |
25a | 0.992 | 1.6 | 847.3 | 762.5 | 0.2% |
Propafenone | 0.9846 | 5.2 | 265.9 | 239.3 | 0.1% |
R2 is the correlation coefficient of the linear regression for the determination of kinetic constant
CLint(mic) = 0.693/half-life/mg microsome protein per mL
CLint (liver) = CLint (mic)*mg microsomal protein/g liver weight*g liver weight/kg body weight
Liver weight: 20 g/kg for human.