DEVELOPMENT AND EVALUATION OF TASTE MASKED ORO-DISINTEGRATING TABLETS OF ITOPRIDE HCl USING DIFFERENT CO-PROCESSED EXCIPIENTS: PHARMACOKINETICS STUDY ON RABBITS

Abstract

Objective: This study aimed to mask the bitter taste of itopride HCl using the solid dispersion method by solvent evaporation technique and formulate an oral disintegrating tablet (ODT) by direct compression method using different co-processed excipients. Methods: Nine formulae of solid dispersion were prepared to mask the bitter taste of Itopride HCl using Eudragit EPO® and mannitol at different ratios after compatibility studies using infrared spectroscopy (IR). The prepared formulae were subjected to different physicochemical characterization, in vivo taste evaluation, and drug content. The best-selected formulae were used to formulate 10 different ODTs. The prepared tablets were evaluated through hardness, drug content, in vivo-in vitro disintegration, IR, wetting time, and finally, dissolution studies. The selected formula was subjected to a pharmacokinetic study compared to the brand. Results: F5, drug: Eudragit EPO® (1:2) and F8, Drug: Mannitol: Eudragit EPO® (1:1:2) formulae were selected as the best taste-masked formulae based on in vivo taste evaluation, which were used to formulate ten ODTs. The dissolution rate for the prepared ODTs was rapid if compared with the ordinary oral tablets. Statistical significance was obtained using one-way ANOVA among ODT formulae. The optimum tablet Prosolv SMCC 90® based formula (T10) had friability 0.15, wetting time 4±0.35 sec, in vitro dissolution 100.08±0.028% just after 2 min, where the in vitro disintegration time and in vivo disintegration time were 4±0.12 sec and 12±0.049 sec respectively. The relative bioavailability of ODT containing Prosolv SMCC 90®was increased significantly compared to the brand. Conclusion: The obtained results successfully confirmed the potential of the promising Prosolv SMCC 90® based formula (T10) to produce rapid onset action and in-time drug release instead of ordinary tablets containing itopride HCl and that provide by-passing the excessive degradation of drug by first-pass metabolism increasing the oral bioavailability from 60% of marketed drug Ganaton® to 88% for the prepared ODT (T10).