Evaluation of the Membrane Permeability (PAMPA and Skin) of Benzimidazoles with Potential Cannabinoid Activity and their Relation with the Biopharmaceutics Classification System (BCS)

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...

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Veröffentlicht in:AAPS PharmSciTech 2011-06, Vol.12 (2), p.573-578
Hauptverfasser: Alvarez-Figueroa, M. Javiera, Pessoa-Mahana, C. David, Palavecino-González, M. Elisa, Mella-Raipán, Jaime, Espinosa-Bustos, Cristián, Lagos-Muñoz, Manuel E.
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Sprache:eng
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Zusammenfassung: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
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-011-9622-1