PREPARATION AND CHARACTERIZATION OF GLIBENCLAMIDE SERINE COMBINATION

ABRAHAM MIRANDA J; ZOPPI A; STERREN V; LONGHI MR

Rosario

Congreso; IV Reunión Internacional de Ciencias Farmacéuticas; 2016

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. The IR spectra of GLB:SERMAS showed the same characteristic vibrations of GLB and molecular interactions could not be detected. The SEM analyses showed differences in particle sizes and morphology also was confirmed sample homogeneity through EDS detector. All samples were crystalline because all of them presented a definite melting point. GLB:SERMAS achieved 37 ± 2% of GLB dissolved, while pure GLB only attained 1.1 ± 0.2% at the same analyses time. At last, f2 factors of GLB:SERMAS respect to GLB, GLBMAS and GLB:SERMP were lower than 50, indicating that there are significant differences between the mentioned profiles. It was concluded that the GLB and SER combination was obtained through an easy and fast method and offered an improved dissolution profile; therefore it is a good candidate for further studies aimed to increase GLB bioavailability.