Binary Systems of Oxytetracycline hydrochloride polymorphs with N-acetylcysteine: improved solubility

BUENO, MARIA SOLEDAD; CAMACHO, NAHUEL; PALMA, SANTIAGO; LONGHI, MARCELA RAQUEL; GARNERO, CLAUDIA

Congreso; 6ta Reunión Internacional de Ciencias Farmacéuticas (RICiFA); 2021

Oxytetracycline hydrochloride (Oxy), an antibiotic of the tetracycline familiy, is a polymorphic drug unstable in solution that evidence erratic absortion in oral administration, which may be due to the presence of polymorphs. In recent years, the combination of active pharmaceutical ingredients with amino-acids has been studied in order to improve their unfavorable properties. The main objective of the study was to investigate the effect of N-acetylcysteine on the solubility of Oxypolimophs I, II and III. The binary systems, in 1:1 ratio,were obtained by kneading , spray drying (SD) and physical mixture. The solids werecharacterizated by serveral techniques, such as powder X-ray diffraction (PXRD) and Fourier transform-infrared spectroscopy.The saturation solubility was evaluated. Among the most important results, the complete amorphization of the systems obtained by SD was demonstrated by PXRD,while the solids obtained by KN remained in crystalline state. The binary SD systems significantly incremented the saturation solubility compared to free polymorphs, which could be attributed to the formation of co-amorphous solids.In conclusion, the results obtained revealed a potencial way for Oxy formulation with improved bioavailability.