Table 3.
Metabolic and solution stabilities.
Compound | The plasma stability | The microsome stability | The solution stability | |||
---|---|---|---|---|---|---|
The intact ± SEM at 120 (min%) | t1/2 (min) | Clint (μL/min /mg protein) | The intact ± SEM at 120 min (%) | |||
pH = 5.0 | pH = 7.4 | pH = 9.4 | ||||
4 | 98.2 ± 6.3 | 14.4 | 96.2 | 92.7 ± 3.1 | 97.3 ± 1.1 | 89.1 ± 2.1 |
13 | 91.5 ± 2.5 | 25.3 | 54.8 | 85.9 ± 0.8 | 87.9 ± 3.4 | 89.3 ± 1.3 |
15 | 84.5 ± 10.2 | 57.3 | 24.2 | 87.1 ± 0.9 | 88.3 ± 1.9 | 84.3 ± 1.8 |
Diltiazem | 49.0 ± 10.6 | -- | -- | 94.7 ± 1.4 | 99.0 ± 5.7 | 69.8 ± 2.6 |
Propranolol | -- | 3.6 | 390 | -- | -- | -- |