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
in En
| MEDLINE
| ID: mdl-21538213
ABSTRACT
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).
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Skin Absorption
/
Benzimidazoles
/
Biopharmaceutics
/
Cannabinoids
/
Cell Membrane Permeability
/
Intestinal Absorption
Type of study:
Prognostic_studies
Limits:
Animals
Language:
En
Journal:
AAPS PharmSciTech
Journal subject:
FARMACOLOGIA
Year:
2011
Type:
Article
Affiliation country:
Chile