Table 3. Permeability Coefficient and Fraction Absorption of N-sulfonylhydrazone Prototypes (1–3) and Quality Control Standards Determined by the PAMPA-GIT Assayc.
| compounds | literature fraction absorption (%)a | experimental permeability (10–6 cm/s) | experimental fraction absorption (%)b | classificationb |
|---|---|---|---|---|
| acyclovir | 21 | 0.1 | 8.62 | low |
| atenolol | 52 | 0.1 | 15.81 | low |
| ceftriaxone | 1 | 0.3 | 23.70 | intermediate |
| coumarin | 100 | 27.9 | 100.00 | high |
| diclofenac | 100 | 14 | 100.00 | high |
| hydrocortisone | 91 | 6.7 | 100.00 | high |
| norfloxacin | 35 | 0.8 | 51.39 | intermediate |
| ranitidine | 55 | 0.4 | 49.75 | intermediate |
| sulfasalazine | 12 | 0.1 | 8.62 | low |
| verapamil | 98 | 7.3 | 99.86 | high |
| LASSBio-1771 (1) | 18.2 | 100.00 | high | |
| LASSBio-1772 (2) | 13.1 | 100.00 | high | |
| LASSBio-1773 (3) | 23.2 | 100.00 | high | |
| LASSBio-1774 (4) | NA | NA | NA |
a
Zhu et al.29
b
Fraction absorption classification: High, 70–100% Fa; Intermediate, 30–69% Fa; and Low, 0–29% Fa.
c
NA = nonanalyzed. Compound 4 could not be evaluated by PAMPA-GIT since it was not soluble in the solution PBS pH 6.6–10 mM: DMSO (95:5).