Abstract

DEVELOPMENT OF ORAL DISINTEGRATING TABLET OF RIZATRIPTAN BENZOATE WITH INHIBITED BITTER TASTE

Sandeep Aher*, Dr. Salunkhe K. S., Dr. Chaudhari S. R.

Abstract

The purpose of this research was to mask the bitter taste of Rizatriptan benzoate (RB) and to formulate an oral disintegrating tablet (ODT) of the taste-masked drug. Taste masking was done by mass extrusion with aminoalkylmethacrylate copolymer, Eudragit EPO, in different ratios. The drug: polymer ratio was optimized based on bitterness score and RB -polymer interaction. Taste masking was evaluated by checking the in vitro release of RB in simulated salivary fluid (SSF) of pH 6.8 and by sensory evaluation in human volunteers. Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) were performed to identify the physicochemical interaction between RB and the polymer. For formulation of rapid- disintegrating tablets of RB, the batch that depicted optimum release of RB in SSF, was considered. ODTs of Rizatriptan Benzoate were prepared by using superdisintegrants namely, sodium starch glycolate, crospovidone and croscarmellose sodium using the direct compression method. The tablets were evaluated for hardness, friability, wetting time, in vitro disintegration time. The optimum formulation was selected and the tablets were evaluated for thickness, drug content, content uniformity and mouth feel, in vivo disintegration time, in vitro drug release at pH 1.2 and 6.8 and stability study. Eudragit EPO was able to mask the bitter taste of Rizatriptan benzoate effectively in 1:1 ratio by mass extrusion method. FTIR and DSC data revealed absence of RB-polymer interaction. ODTs containing crospovidone (5% w/w) depicted minimum disintegration time. Taste evaluation of ODT in human volunteers revealed considerable taste masking, with all 6 volunteers, reporting the taste of ODTs as good in comparison with RB. Thus, results conclusively demonstrated successful taste masking and rapid disintegration of the formulated tablets in the oral cavity withadequate dissolution. The research work suggests a rapid, simple and cost effective mass extrusion method for formulation of ODT of Rizatriptan benzoate.

Keywords: Taste masking Oral disintegrating tablet Rapid-disintegrating tablets Rizatriptan benzoate Eudragit EPO Superdisintegrants.