Preparation and characterization of glibenclamide serine combination

V. STERREN; M. LONGHI; A. ZOPPI; J. ABRAHAM-MIRANDA

Rosario

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

Universidad Nacional de Rosario

Glibenclamide (GLB) is an oral hypoglycemic agent indicated for treatment of type II diabetes. Its poor water solubility causes a limited and variable bioavailability. The present investigation was aimed to develop and characterize GLB and serine (SER) combination to improve drug dissolution characteristics. The combination of GLB and SER (GLB:SERMAS) was prepared by solvent assisted milling (MAS), in 1:1 molar ratio with addition of water. The same method was applied to raw drug like process control (GLBMAS). Also was obtained a physical mixture of both compounds (GLB:SERMP). All the samples were analyzed by infrared spectroscopic (IR), electron microscopy studies (SEM), and hot-stage microscopy. In addition, rate dissolution studies were realized through palette method in 500 ml of phosphate buffer (pH 7.4) at 37.0 ± 0.5 ºC and 50 rpm. Finally, was calculated the similarity factor f2 to compare the dissolution curves.