Evaluation of the membrane permeability (PAMPA and skin) of benzimidazoles with potential cannabinoid activity and their relation with the Biopharmaceutics Classification System (BCS).
AAPS PharmSciTech
; 12(2): 573-8, 2011 Jun.
Article
en En
| MEDLINE
| ID: mdl-21538213
The permeability of five benzimidazole derivates with potential cannabinoid activity was determined in two models of membranes, parallel artificial membrane permeability assay (PAMPA) and skin, in order to study the relationship of the physicochemical properties of the molecules and characteristics of the membranes with the permeability defined by the Biopharmaceutics Classification System. It was established that the PAMPA intestinal absorption method is a good predictor for classifying these molecules as very permeable, independent of their thermodynamic solubility, if and only if these have a Log P(oct) value <3.0. In contrast, transdermal permeability is conditioned on the solubility of the molecule so that it can only serve as a model for classifying the permeability of molecules that possess high solubility (class I: high solubility, high permeability; class III: high solubility, low permeability).
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Absorción Cutánea
/
Bencimidazoles
/
Biofarmacia
/
Cannabinoides
/
Permeabilidad de la Membrana Celular
/
Absorción Intestinal
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Revista:
AAPS PharmSciTech
Asunto de la revista:
FARMACOLOGIA
Año:
2011
Tipo del documento:
Article
País de afiliación:
Chile
Pais de publicación:
Estados Unidos