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. 2022 Oct 7;10(4):299–314. doi: 10.5599/admet.1476

Table 3.

Physicochemical properties, food effect data and measured flux of the studied compounds

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