Table 3.
Drugs | BCS Class | log P | Solubility ratio | Observed AUC Ratio | Observed Cmax Ratio | FE | Dose used in clinical data | Dose used flux study | Flux Fe (±SD; n=3) | Flux Fa (±SD; n=3) | Flux Ratios |
---|---|---|---|---|---|---|---|---|---|---|---|
(Fed/Fasted) | (Fed/Fasted) | (Fed/Fasted) | (mg) | (mg) | (Fed/Fasted) | ||||||
Amiodarone [27] (early)1 | II | 7.8 | 2.23 | 2.36 | 3.68 | positive | 600 | 200 | 0.073 ± 0.001 | 0.017± 0.003 | 4.25 |
Amiodarone (late)2 | II | 7.8 | 2.23 | 2.36 | 3.68 | positive | 600 | 200 | 1.277± 0.109 | 0.579 ± 0.095 | 2.21 |
Celecoxib [29] | II | 3.02 | 2.24 | 1.19 | 1.29 | positive | 200 | 50 | 0.632 ± 0.077 | 0.186 ± 0.021 | 3.4 |
Clopidogrel bisulfate [43] | II/IV | 4.2 | 3.85 | 1.02 | 0.79 | none | 75 | 75 | 2.168 ± 0.323 | 1.751 ± 0.540 | 1.24 |
Danazol [30] | II | 4.7 | 3.43 | 3.13 | 2.73 | positive | 100 | 100 | 0.352 ± 0.063 | 0.081 ± 0.016 | 4.35 |
Fluoxetine HCl [41] | I | 4.5 | 1.17 | 0.96 | 0.85 | none | 40 | 40 | 0.85 ± 0.01 | 1.77 ± 0.15 | 0.5 |
Furosemide [32] | IV | 2.56 | 0.23 | 1.18 | 0.67 | negative | 40 | 80 | 0.208 ± 0.036 | 0.018 ± 0.003 | 11.48 |
Griseofulvin [31] | II | 2.2 | 1.24 | 1.7 | 2.2 (4 h) 1.7 (8 h) |
positive | 1000 | 125 | 0.218 ± 0.009 | 0.205 ± 0.011 | 1.06 |
Isoniazid [37] | I | -0.52 | n/a | 0.88 | 0.49 | negative | 300 | 300 | 0.020 ± 0 | 0.020 ± 0 | 1.02/0.92 |
Nefazodone HCl [38] | II | 3.5 | 1.52 | 0.78 | 0.93 | negative | 200 | 50 | 1.077 ± 0.084 | 0.521 ± 0.179 | 2.07 |
Nefazodone HCl suspension | II | 3.5 | 1.52 | 0.78 | 0.93 | negative | 200 | 100 | 1.923 ± 0.547 | 2.610 ± 0.618 | 0.74 |
Nifedipine [44] | II | 3.17 | 3.2 | 1.02 | 0.74 | none | 10 | 25 | 0.235 ± 0.028 | 0.233 ± 0.073 | 1.01 |
Zidovudine [42] | III | 0.13 | n/a | 0.9 | 0.3 | negative | 100 | 200 | 0.034 ± 0.002 | 0.037 ± 0.007 | 0.92 |
1 “early” flux refers to the initial appearance rate in the acceptors. The early flux was calculated using the data in the first 2 hours of the experiment, selecting time interval for each media excluding lag time.
2 “late” flux corresponds to the appearance rate during the later time points in the acceptor. The late flux was calculated using the data in the 2.5-9 hours’ time interval, selecting the intervals guided by linearity of the concentration-time profiles in the receptor