Inactivator depletion and recovery from hepatocyte incubation media Values are mean (S.D.), n = 3 incubations.
Concentration Range | Recovery from Mediuma | Percentage of Remaining in Incubationb | Percentage of Remaining in the Mediumc | |
|---|---|---|---|---|
| μM | ||||
| Amprenavir | 0.1 | 0.34 (0.03) | 63 (7) | 18 (4) |
| 0.5 | 0.36 (0.04) | 69 (9) | 26 (4) | |
| 1.0 | 0.36 (0.02) | 80 (11) | 80 (3) | |
| 5.0 | 0.41 (0.04) | 89 (9) | 97 (4) | |
| Diclofenac | 2.5 to 100 | 0.80 (0.01) | 29 (3) to 92 (6) | 27 (8) to 67 (8) |
| Diltiazem | 0.5 to 4 | 0.75 (0.01) | 95 (4) to 98 (5) | 85 (3) to 83 (4) |
| Erythromycin | 10 to 80 | 1.00 (0.04) | 93 (1) to 103 (8) | 105 (2) to 99 (2) |
| Raloxifene | 2.5 | 0.11 (0.02) | 27 (1) | 54 (3) |
| 5.0 | 0.09 (0.01) | 23 (1) | 51 (19) | |
| 10.0 | 0.11 (0.06) | 34 (4) | 61 (15) | |
| 20.0 | 0.11 (0.00) | 69 (5) | 70 (2) | |
| Troleandomycin | 0.75 to 6 | 0.99 (0.01) | 88 (5) to 94 (1) | 86 (3) to 91 (2) |
↵ a Calculated as the ratio of concentration in the medium to the concentration in hepatocyte suspension immediately after hepatocytes were spiked with inactivators (Iu/total inactivator concentration)
↵ b Percentage of inactivator concentration after 1-h preincubation (total concentration)
↵ c Percentage of inactivator concentration after 1-h preincubation (Iu)