| Compounds |
Human |
Mouse |
Rat |
Dog |
Monkey |
Microminipig |
| Caffeine |
|
|
|
|
|
|
| CLint (ml/min/mg protein) |
0.00788 ± 0.00012 |
0.00627± 0.00074 |
0.00312 ± 0.00034 |
0.00359 ± 0.00065 |
0.00398 ± 0.00012 |
0.00667 ± 0.00055 |
| CLint (ml/min/kg)a |
9.11± 0.14 |
24.7± 2.9 |
5.61± 0.61 |
5.16 ± 0.93 |
5.37 ± 0.16 |
5.19 ± 0.43 |
| Losartan |
|
|
|
|
|
|
| CLint (ml/min/mg protein) |
0.0379± 0.0062 |
0.0876± 0.0080 |
0.0149 ± 0.0020 |
0.0146 ± 0.0027 |
0.122 ± 0.007 |
0.0277 ± 0.0030 |
| CLint (ml/min/kg)a |
43.8± 7.2 |
345± 32 |
26.8 ± 3.5 |
21.1 ± 3.8 |
165 ± 9 |
21.6 ± 2.3 |
| Omeprazole |
|
|
|
|
|
|
| CLint (ml/min/mg protein) |
0.0354± 0.0042 |
0.0590± 0.0050 |
0.136 ± 0.008 |
0.0112 ± 0.0012 |
0.117 ± 0.006 |
0.0260 ± 0.0070 |
| CLint (ml/min/kg)a |
41.0± 4.9 |
232± 20 |
245 ± 15 |
16.2± 1.7 |
158 ± 8 |
20.2 ± 5.5 |
| Dextromethorphan |
|
|
|
|
|
|
| CLint (ml/min/mg protein) |
0.0327± 0.0066 |
0.167± 0.007 |
0.489 ± 0.001 |
0.0585± 0.007 |
0.669 ± 0.008 |
0.582 ± 0.011 |
| CLint (ml/min/kg)a |
37.8± 7.6 |
658± 27 |
880 ± 1 |
84.3 ± 9.8 |
903 ± 11 |
453 ± 8 |
| Midazolam |
|
|
|
|
|
|
| CLint (ml/min/mg protein) |
0.569± 0.018 |
0.460± 0.016 |
0.472 ± 0.028 |
0.528 ± 0.020 |
0.973 ± 0.058 |
0.246 ± 0.043 |
| CLint (ml/min/kg)a |
658± 21 |
1811± 62 |
850 ± 50 |
736 ± 70 |
1314 ± 78 |
192 ± 34 |
|
Each in vitro intrinsic clearance value represents mean ± SD for triplicate determinations.
aCalculated using standard values of 45 mg of microsomal protein/g liver [29] for all species and the following values for g liver/kg body weight: human, 25.7; mouse, 87.5;
rat, 40.0; dog, 32.0; monkey, 32.0 [30]; microminipig, 17.3.
CLint, in vitro intrinsic clearance value. |
| Table 6: In vitro intrinsic clearance values for caffeine, losartan, omeprazole, dextromethorphan, and midazolam in liver microsomes of various species. |
