FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLET OF LOPERAMIDE

Purpose of present research work was to develop mouth dissolving tablets of loperamide using superdisintegrants. Mouth dissolving tablets of loperamide were prepared by direct-compression method after incorporating superdisintegrants Ac-Di-Sol, Sodium Starch Glycolate (SSG), and Crosspovidone in different concentrations. Effect of superdisintegrants on disintegration and dissolution behavior of tablet in O.1 N HCl, phosphate buffer (pH 6.8) was evaluated. To address poor solubility of loperamide, solid dispersion using solvent evaporation techniques was prepared using hydrophilic carrier PEG4000, PVP K-30, and Urea. Improvement in dissolution of drug was observed in solid dispersion as compared to pure drug. The 100% drug release was obtained from the solid dispersion (prepared by solvent evaporation method) of Loperamide: PEG4000 (1:6) in 10 minute. Formulations were evaluated for Weight variation, hardness, and thickness, friability, wetting time uniformity of dispersion, drug content, disintegration time and in vitro dissolution studies. The drug content of all the formulations was within the acceptable limits of the United States Pharmacopoeia XXVII. Optimized formulation showed good release profile with maximum drug being released at all-time intervals.  Optimized Formulation (F-8) containing crosspovidone showed > 90% drug release in 20 min and disintegration time of 17 sec.  From Stability point of view no appreciable change was observed in release profile and drug content after 3 month storage of tablet at 40±2º and 75±5% RH.