Formulação de grânulos para mascaramento de sabor amargo de fármacos hidrofílicos para o desenvolvimento de formas farmacêuticas sólidas orais de desintegração instantânea

Abstract

Palatability is one of the most critical attributes of orally disintegrating solid dosage forms. Therefore, the exploration of novel techniques to mask the aversive taste of drugs remains in continuous demand. This study focused on the development of effervescent granules for production of orally disintegrating solid dosage forms, specifically orally disintegrating tablets (ODTs), aiming to mask the bitter taste of dipyrone, a widely used drug. The strategy involved the selection of appropriate excipients and the development of effervescent granules as an intermediate step for ODT production, to reduce negative sensory impact. Eleven distinct formulations were prepared, each containing different combinations and proportions of excipients. The methodological process involved individualized weighing of components, standardized for 10 g formulations, with the exception of F1 (which followed quantities from the project reference article) and F8 (adapted due to the use of carnauba microparticles containing a smaller amount of dipyrone). The powders were pre-sieved through a 600 µm mesh to ensure uniformity, while the binders were weighed separately and incorporated using a mortar and pestle. After mixing, the granules were formed by sieving through a 1000 µm mesh, dried in an oven at 40 °C for approximately 3 hours, and stored in sealed bottles within a desiccator containing silica gel. Formulations F6, containing crospovidone and sodium starch glycolate, and F8, with carnauba microparticles, stood out due to superior processability and granule quality. In conclusion, from a pharmaceutic-technological perspective, the developed formulations demonstrated promising potential, with additional stages of physicochemical characterization and sensory evaluation required to verify the effectiveness of the taste-masking approach.