Table III.
Compound | BCS classa | P eff,int (jejunum) b (×10−4 cm/s) | P eff,int (ileum) b (×10−4 cm/s) | Observedc ileal CLabs (×10−4 cm3/s) | Predictedd ileal CL abs (×10−4 cm3/s) | ||||||
---|---|---|---|---|---|---|---|---|---|---|---|
M1 | M2 | M3 | M1 | M2 | M3 | M1 | M2 | M3 | |||
Hydrocortisone | 2 | 8.79 | 0.032 | 0.046 | 5.57 | 0.027 | 0.050 | 787 | 1242 | 928 | 724 |
Triamcinolone acetonide | 2 | 4.16 | 0.015 | 0.022 | 9.94 | 0.049 | 0.090 | 1405 | 588 | 439 | 343 |
Paracetamol | 1 | 4.79 | 0.018 | 0.025 | 7.17 | 0.036 | 0.065 | 2028 | 1356 | 1012 | 790 |
Salicylic acid | 1 | 2.67 | 0.011 | 0.014 | 4.12 | 0.024 | 0.037 | 3108 | 2010 | 1500 | 1171 |
Hydrochlorothiazide | 4 | 0.18 | 0.00079 | 0.0010 | 0.16 | 0.00089 | 0.0014 | 117 | 139 | 104 | 81 |
Atenonol | 3 | 0.38 | 0.0016 | 0.0020 | 0.27 | 0.0016 | 0.0025 | 206 | 283 | 211 | 165 |
Furosemide | 4 | 0.48 | 0.0021 | 0.0025 | 0.22 | 0.0013 | 0.0020 | 166 | 365 | 272 | 213 |
Cimetidine | 3 | 0.77 | 0.0033 | 0.0040 | 0.30 | 0.0017 | 0.0027 | 228 | 580 | 433 | 338 |
Talinonol | 4 | 0.31 | 0.0012 | 0.0016 | 0.37 | 0.0019 | 0.0034 | 106 | 88 | 66 | 52 |
Griseofulvine | 2 | 7.47 | 0.028 | 0.039 | 11.57 | 0.057 | 0.10 | 2181 | 1407 | 1051 | 820 |
Ranitidine | 3 | 1.74 | 0.0066 | 0.0091 | 1.41 | 0.0072 | 0.013 | 400 | 492 | 367 | 287 |
aBCS classification extracted from references (4,5)
bOpen perfusion regional permeability values were re-calculated from references (4,5,44–49) and the mSA values shown in Table I
cObserved regional absorption clearances were re-calculated from references (4,5,44–49) employing a parallel tube model (Eq. 7); the details for the calculations can be found in the Section 2 of the Supplementary Material
dPredicted values from Eq. 8, using jejunal P eff data derived by the open perfusion system and ileal mSA data from Table I