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AAPS PharmSciTech ; 12(2): 573-8, 2011 Jun.
Article in English | 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).


Subject(s)
Benzimidazoles/pharmacokinetics , Biopharmaceutics/methods , Cannabinoids/pharmacokinetics , Cell Membrane Permeability/physiology , Intestinal Absorption , Skin Absorption/physiology , Animals , Animals, Newborn , Benzimidazoles/classification , Benzimidazoles/standards , Biopharmaceutics/standards , Cannabinoids/classification , Cannabinoids/standards , Cell Membrane Permeability/drug effects , Drug Evaluation, Preclinical/methods , Drug Evaluation, Preclinical/standards , Intestinal Absorption/drug effects , Intestinal Absorption/physiology , Membranes, Artificial , Predictive Value of Tests , Skin Absorption/drug effects , Swine
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