EFFECT OF EFFERVESCENCE IN COMBINATION WITH SUPERDISINTEGRANTS IN THE FORMULATION OF PROPRANOLOL HCL ORAL DISINTEGRATING TABLETS

Abstract

ABSTRACTObjective: The current research work is intended to formulate propranolol HCl (PLH) as orally disintegrating tablet (ODT). It is also intending to checkthe superiority in a combination of superdisintegrants and effervescent mixture than the use of superdisintegrants alone by a direct compressiontechnique. To fasten the onset of action and thereby enhancing the bioavailability of PLH in comparison to its conventional tablets.Methods: Standard calibration curve of PLH was obtained in pH 6.8 phosphate buffer by spectrophotometric method, drug-excipient compatibilitystudies were carried by Fourier transform infrared (FT-IR) studies. All the formulations were evaluated for pre and postcompression studies.Accelerated stability studies were carried out up to 6 months for the optimized formulation, EF3.Results and Discussion: Superdisintegrants used in the study are compatible with PLH. Pre- and post-compression parameters were within theacceptable limits for all formulations. In vitro dissolution kinetic studies indicate the release of PLH from ODT increases as the concentration ofsuperdisintegrants as well as the ratio of citric acid: NaHCO3 of effervescent mixture increases. Formulations with an effervescent mixture are havingrapid disintegration and dissolution rate when compared to the formulations with superdisintegrants alone. The order of superdisintegrants inenhancing the dissolution rate of PLH is crospovidone (CPV) > croscarmellose sodium (CCS) > sodium starch glycolate (SSG). Formulation, EF3 (10%CPV and 1:3, citric acid: NaHCO3 ratio, respectively) had the highest dissolution efficiency at 10 minutes (DE10=82.74%); the first order dissolutionrate constant (K1=0.141/minutes) with a regression coefficient (r2=0.974) and lesser time for 90% of drug release (t90=4 minutes), was considered asthe optimal ODT in this study. Formulation EF3, passed the test for stability.Conclusion: Hence, an effective PLH ODT was formulated by the direct compression technique with disintegration by combination of superdisintegrantsand effervescent mixture, will fasten the onset of action and enhances the bioavailability of PLH in comparison to its conventional tablets.Keywords: Propranolol HCl, Orally disintegrating tablet, Sodium starch glycolate, Croscarmellose sodium, Crospovidone, Direct compression, In vitrodissolution studies.