Papp coefficients across monolayers (HIECs and Caco-2 cells) and in the PAMPA for the 10 test compounds
Papp values represent the mean ± S.D. (n = 3).
| Compound | Faa | Papp | Major Route for Absorption or Transporter | MolecularWeight | LogPb | PSAb | ||
|---|---|---|---|---|---|---|---|---|
| HIECs | Caco-2 Cells | PAMPA | ||||||
| % | × 10−6 cm/s | Å2 | ||||||
| FD-4 | 0 | 0.56 ± 0.01 | 0.035 ± 0.009 | 0.0046 ± 0.0017 | Paracellular | 4000 | — | — |
| Vinblastine | 25 | 2.6 ± 0.1 | 0.57 ± 0.02 | 4.1 ± 0.8 | Transcellular/P-gp | 811.0 | 3.7 | 154.1 |
| Topotecan | 30 | 0.78 ± 0.14 | 0.35 ± 0.06 | 1.5 ± 0.1 | Transcellular/BCRP | 421.4 | 0.8 | 103.2 |
| Didanosine | 42 | 0.62 ± 0.12 | 0.11 ± 0.02 | 0.11 ± 0.01 | Nucleoside transporters | 236.2 | −1.2 | 88.7 |
| Atenolol | 50 | 0.68 ± 0.09 | 0.34 ± 0.05 | 0.022 ± 0.005 | Paracellular | 266.3 | 0.2 | 84.6 |
| Terbutaline | 62 | 0.70 ± 0.05 | 0.069 ± 0.006 | 0.014 ± 0.001 | Paracellular | 225.3 | 0.9 | 72.7 |
| Ribavirin | 85 | 4.1 ± 0.3 | 0.092 ± 0.003 | 0.030 ± 0.002 | Nucleoside transporters | 244.2 | −1.9 | 143.7 |
| Doxifluridine | 90 | 4.7 ± 0.6 | 0.20 ± 0.03 | 0.14 ± 0.03 | Nucleoside transporters | 246.2 | −1.4c | 99.1d |
| Pindolol | 90 | 7.9 ± 0.7 | 3.6 ± 0.3 | 2.2 ± 0.1 | Transcellular | 248.3 | 1.8 | 57.3 |
| Midazolam | 100 | 30 ± 3 | 170 ± 7 | 40 ± 4 | Transcellular | 325.8 | 3.1e | 30.2 |
LogP, partition coefficient; PSA, polar surface area.
↵a Fa values were obtained from published data (Yamashita et al., 2000; Sugano et al., 2002; Tavelin et al., 2003b; Dixit and Perelson, 2006; Skolnik et al., 2010; Varma et al., 2010; Lin et al., 2011; Sjöberg et al., 2013).
↵b Data obtained from www.drugbank.ca.
↵c Data obtained from the interview form of Furtulon capsules.
↵d Data obtained from http://pubchem.ncbi.nlm.nih.gov/.
↵e Data obtained from a reference (Rodgers and Rowland, 2006).