Table 2. In Vitro Determination of the Metabolic Stability after Incubation with Mouse and Human Liver Microsomesa.
| compd | human
liver microsomes (HLM) |
mouse
liver microsomes (MLM) |
||
|---|---|---|---|---|
| μL/min/mg protein | min | μL/min/mg protein | min | |
| Cli ± SD | t1/2 ± SD | Cli ± SD | t1/2 ± SD | |
| 15 | 35.9 ± 0.2 | 38.7 ± 0.2 | 461.1 ± 45.5 | 3.0 ± 0.3 |
| 7-ECb | 231.3 ± 37.5 | 6.1 ± 1.0 | 710.8 ± 1.2 | 2.0 ± 0.1 |
| Pro.c | 45.9 ± 2.7 | 30.2 ± 1.8 | 235.1 ± 24.0 | 5.9 ± 0.6 |
a
Results are expressed as the mean ± SD, n = 2.
b
7-EC, ethoxycoumarin.
c
Pro., propranolol. The standard compounds 7-EC and Prop. showed metabolic stability in agreement with the literature and internal validation data.