Table III.
The 20 Model Drugs Suggested by the FDA for Use in Establishing Suitability of a Permeability Method Together with Predictability Using CLogf P and Log P vs Predictability Using Extent of Metabolism
Drug | Permeability Class | Predicted by CLogP and Log P | Predicted by Extent of Metabolisma |
---|---|---|---|
Antipyrine | High (Potential IS candidate) | No | Yes |
Caffeine | High | No | Yes |
Carbamazepine | High | Yes | Yes |
Fluvastatin | High | Yes | Yes |
Ketoprofen | High | Yes | Yes |
Metoprolol | High (Potential IS candidate) | Yes | Yes |
Naproxen | High | Yes | Yes |
Propranolol | High | Yes | Yes |
Theophylline | High | No | Yes |
Verapamil | High (Potential ES Candidate) | Yes | Yes |
Amoxicillin | Low | Yes | Yes |
Atenolol | Low | Yes | Yes |
Furosemide | Low | No | Yes |
Hydrochlorthiazide | Low | Yes | Yes |
Mannitol | Low (Potential IS candidate) | Yes | Yes |
α-Methyldopa | Low | Yes | Yes |
Polyethylene glycol (400) | Low | Yes | Yes |
Polyethylene glycol (1000) | Low | Yes | Yes |
Polyethylene glycol (4000) | Low (zero permeability marker) | Yes | Yes |
Ranitidine | Low | Yes | Yes |
Using 70% as the cutoff