Table 1.
The permeability means values of 7 reference chemicals in GIT PAMPA.
| Compound | CAS No. | Test conc. | BCS class1 | pKa | Uncharged pH range | pH | Permeability (10−6 cm/s) (Mean±S.D.) | |
|---|---|---|---|---|---|---|---|---|
|
| ||||||||
| Expected from supplier2 | Measured in this lab3 | |||||||
| Ketoprofen | 22071-15-4 | 50 μM | 2 | 4.1 | <4.1 | 5.0 | 41.2±5.0 | 61.5±15.9 |
| 6.2 | 15.8±2.0 | 15.4±1.9 | ||||||
| 7.4 | 1.7±0.5 | 1.3±0.1 | ||||||
|
| ||||||||
| Verapamil HCl | 152-11-4 | 50 μM | 1 | 9.1 | >9.1 | 5.0 | 47.5±5.0 | 60.4±15.8 |
| 6.2 | 60.5±10.0 | 66.5±21.8 | ||||||
| 7.4 | 61.3±10.0 | 67.0±28.7 | ||||||
|
| ||||||||
| Carbamazepine | 298-46-4 | 50 μM | 2 | 1.4 | >1.4 | 5.0 | 41.8±5.0 | 44.1±7.0 |
| 6.2 | 36.6±5.0 | 42.9±6.3 | ||||||
| 7.4 | 42.9±5.0 | 40.9±7.7 | ||||||
|
| ||||||||
| Propranolol | 318-98-9 | 50 μM | 1 | 9.5 | >9.5 | 5.0 | 44.2±6.5 | 49.9±11.0 |
| 6.2 | 66.7±10.3 | 80.8±25.1 | ||||||
| 7.4 | 63.9±10.1 | 83.1±30.1 | ||||||
|
| ||||||||
| Metoprolol Tartrate | 56392-17-7 | 50 μM | 1 | 9.6 | >9.6 | 5.0 | 4.9±0.5 | 4.1±0.2 |
| 6.2 | 19.1±3.0 | 29.1±4.0 | ||||||
| 7.4 | 45.7±5.0 | 59.0±21.6 | ||||||
|
| ||||||||
| Antipyrine | 60-80-0 | 250 μM | 1 | 1.4 | >1.4 | 5.0 | 2.9±0.3 | 2.0±0.2 |
| 6.2 | 2.8±0.3 | 2.0±0.2 | ||||||
| 7.4 | 2.4±0.2 | 1.9±0.1 | ||||||
|
| ||||||||
| Ranitidine | 66357-59-3 | 50 μM | 3 | 2.0, 8.3 | >8.3 | 5.0 | <0.1 | 0.1±0.1 |
| 6.2 | <0.1 | 0.0±0.0 | ||||||
| 7.4 | 0.1±0.5 | 0.3±0.1 | ||||||
1
BCS represents biopharmaceutics classification system that classifies the drugs/chemicals on the basis of their solubility and permeability.
2
The expected permeability values of reference chemicals were provided by the supplier of PAMPA.
3
The measured permeability values in this study were generated from three different experiments.