Physical-chemical characterization of binary systems of albendazole desmotropes and glutamic acid or aspartic acid.

BONGIOANNI, AGUSTINA; GARNERO, CLAUDIA; MEZZANO, BELÉN; LONGHI, MARCELA RAQUEL

ON-LINE

Congreso; 6ta Reunión Internacional de Ciencias Farmacéuticas (RICiFa)-Edición Aniversario 10 años-; 2021

: Albendazole is a broad-spectrum anthelmintic widely used in the treatment of intestinal andsystemic parasitosis, which was included in the essential medicines list of the World HealthOrganization. However, it has an extremely low aqueous solubility. In additon, two desmotropes ofthe drug have been reported. In order to improve the biopharmaceutical properties of Albendazole,new binary systems of albendazole desmotropes and glutamic acid or aspartic acid were developedand investigated . Solid samples were prepared by kneading method and physical mixture to evaluate the interactions. It were characterized by powder X-ray diffraction, Fourier transform infrarred spectroscopy, scanning electron microscopy, thermal analysis and solubility studies. The structural characterization evidenced different interactions between both albendazole desmotropes and the amino-acids. Interestely, diffractograms showed that polymorphic transformation during the solids preparation did not occur. The saturation solubility studies showed a significantly solubilizing effect in water and simulated gastric fluid compared to free desmotropes, which could be attributed to several intermolecular H-bonds. In conclusion, the improving biopharmaceutical properties shows the amino-acids as promising candidates for the development of oral formulations for delivery of the albendazole.