Comparison and Evaluation of Bitter Taste Masked Levocetrizine diHCl Using β-Cyclodextrin and Kyron T-114

The purpose of this study was to evaluate the possibility of taste masking of Levocetirizinedihydrochloride (L-CTZ) by means of inclusion complexation and ion exchange resin. Initially anattempt was given to mask the bitter taste of the drug by inclusion complexation with β-Cyclodextrinusing kneading method. But from gustatory evaluation, it was found that β-Cyclodextrin was not provengood for effective taste masking. So, another attempt was given to mask bitter taste of LevocetrizinediHCl by Kyron T-114 (weak cation exchange resin). It is a water-insoluble, high molecular weight,cross linked polymer of methacrylic acid. Kyron T-114 is inexpensive and this method is simple, rapidand cost-effective method for taste masking. Ion exchange resin complex was prepared by the batchtechnique and various parameters viz. resin activation, drug: resin ratio, pH, temperature, swelling timeand stirring time were optimized to successfully formulate the tasteless Drug Resin Complex (DRC).Maximum drug loading was obtained when the resin was activated by acid treatment, with 1:3 drug:resin ratio, soaked in water for 90 min. and stirred with the drug for 240 minutes, pH maintained 5.5 andtemperature maintained 30 C. Complexation was confirmed by FT-IR and DSC study. The drug resincomplex was evaluated for taste in-vitro and in-vivo evaluation. The volunteers rated the complexes astasteless and agreeable. Drug release from DRC in salivary pH was insufficient to impart bitter taste.Complete drug release was observed at gastric 0.1 N HCl (pH 1.2). Formulation of drug resin complexwas confirmed by FT-IR and DSC studies.