1. Using a dual-drug resinate complex for taste masking: Box-Behnken modelling was used to optimize a resinate complex, to mask the taste of levocetirizine dihydrochloride and montelukast sodium in orally disintegrating tablets
- Author
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Mundlia, Jyoti, Marwaha, Rakesh Kumar, and Dureja, Harish
- Subjects
Properties ,Product development ,Oral drugs -- Product development ,Excipients -- Properties ,Oral medication -- Product development - Abstract
Organoleptic (i.e., sense-related) characteristics can have a significant impact on how closely patients adhere to any therapeutic regimen (1). Taste is one of the key factors that determine patient compliance [...], The goal of this project was to use complexation to develop a dual-drug resinate system, to mask the bitter taste of levocetirizine dihydrochloride and montelukast sodium. The maximum drug loading onto the resin, polacrilin potassium, USP (Tulsion 339) was found to be 1:3 drug-to-resin ratio. Box-Behnken design methods were used to study the effect of processing parameters such as swelling time ([X.sub.1]), stirring time ([X.sub.2]) and pH ([X.sub.3]), on cumulative percentage drug release. The cumulative percent drug release was found to be minimal at extreme pH values ([X.sub.3]) and at high values of swelling time (X) and low values of stirring time ([X.sub.1]). The maximum drug release was found at high values of stirring time, even at low values of swelling time. One-way analysis of variance (ANOVA) was applied to the cumulative percentage drug release to study the fitting and the significance of the model. Differential scanning calorimetry (DSC) and Fourier Transform Infrared (FTIR) analyses of the optimized formulation (F3) confirmed the drug complex formation suggesting that this model can be used to optimize dual drug release. Finally, the dual-drug resinate was formulated into orally disintegrating tablets (ODT), whose quality was found to be within pharmacopoeial limits. Drug release rate studies of the tablets in simulated gastric fluid and in phosphate buffer (pH 6.8) showed better results than the marketed formulation. Results suggest that dual-drug resinate can be a cost- effective and efficient method for masking unpleasant taste in dual drug formulations.
- Published
- 2015