Objective: In previous work, Prifinium Bromide had been successfully formulated as oro-dispersible tablets. However, Prifinium Bromide, a quaternary ammonium compound, has a bitter taste; therefore, taste masking was necessary to produce acceptable oro-dispersible tablets and enhance patients' compliance.
Methods: In this work, several attempts had been made to mask the bitterness of this drug. β-cyclodextrin inclusion complexes, solid dispersions of the drug in ethyl cellulose and methyl cellulose as well as loading the drug on Eudragit E100 have all been used. The selected granules were used to prepare oro-dispersible tablets and were evaluated.
Results: Drug-Eudragit granules E3 prepared by mass extrusion method gave less than 10% of drug in simulated saliva fluid and almost complete release in simulated gastric fluid after 2 minutes. Therefore, it was used to prepare oro-dispersible tablets formulas. In vitro disintegration time of formula T2 was 45.5 ± 7.7 seconds showed a complete drug release of Prifinium Bromide in phosphate buffer (pH 6.8) and (94%) in SGF (pH 2.1).
Conclusion: Loading of Prifinium Bromide on Eudragit E100 using mass extrusion method was the best method to overcome the disagreeable taste of the drug. They gave the least amount of drug released in simulated saliva fluid and passed the quality control tests of tablets after formulation as oro-dispersible tablets. They also gave good taste when tested in vivo
