Investigating the effect of supramolecular systems on biopharmaceutical properties of Albendazole desmotropes

C. GARNERO; A. BONGIOANNI; M. LONGHI

Rosario

Congreso; 4a Reunión Internacional de Ciencias Farmacéuticas (RiCIFA).; 2016

Universidad Nacional de Rosario

Albendazole (ABZ), a benzimidazole carbamate, is one of the most effective broad-spectrum anthelmintic agents with activity against human and animal parasites. ABZ belongs to biopharmaceutical classification system type II. Besides, two solids forms enantiotropically related have been reported and designated as ABZI and ABZII. Having in mind the improvement on the bioavailability of ABZ and the selection of a proper desmotrope for its pharmaceutical use, the aim of this study was to analyse the effect of supramolecular systems on solubility and dissolution behaviour of ABZI and ABZII.In order to investigate the influence of supramolecular systems on the biopharmaceutical properties of ABZ desmotropes, binary and ternary systems were studied. Among the available ligands capable of forming supramolecular systems that improve certain properties, were selected maltodextrin (MD) and glutamic acid (GLU). The solubility measurements of ABZ (I and II) and the systems ABZI:MD, ABZII:MD, ABZI:MD:GLU and ABZII:MD:GLU were performed in aqueous and simulated gastric fluid without enzymes, according to the method of Higuchi and Connors. Solid-state systems in equimolar ratio were prepared by kneading method and physical mixture. These were characterized by powder X-ray diffraction and scanning electron microscopy, and their dissolution behaviors were evaluated.