Taste Masking By Hot Melt Extrusion Without Loss Of Bioavailability For Pediatrics

ABSTRACT

Objective: The aim of present work was to develop a platform technology for the pediatric dosage form to mask the bitter taste of Furosemide (FUR) and prepare a flexible solid oral dosage form. Methods: Excipient compatibility study was carried out by using Fourier-transform infrared spectroscopy (FTIR). Taste masking was done by hot melt extrusion (HME) technology. Eudragit EPO and Soluplus were used as a taste masking and solubilizing polymers respectively. The prepared solid dispersion and tablets were evaluated for their physicochemical parameters such as hardness, friability, disintegration, in vitro drug release. Results: Experimental data revealed that physical integrity, brittleness of granules, conversion of a drug in amorphous form was improved by combining Eudragit EPO with Soluplus. Plasticizer helped to complete HME at 80 °C. Less than 10% drug release in pH 6.8 medium revealed that release would be extremely limited in the saliva and thus avoiding bitterness. Animal study data revealed that bioavailability has been increased by 30%. Differential scanning calorimetry (DSC) and x-ray diffraction (XRD) tests confirmed the existence of molecularly dispersed drug. Fourier-transform infrared spectroscopy (FTIR) confirmed the unchanged functional groups of FUR after HME processing. Conclusion: Proposed platform technology masked the bitter taste and enhanced the bioavailability of FUR in D P ratio of 12.