Formulation and evaluation of bitter taste-masked orally disintegrating tablets of high memantine hydrochloride loaded granules coated with polymer via layering technique

Abstract

Orally disintegrating tablets (ODTs) improve patient adherence as they can easily disintegrate in the presence of small amount of saliva. However, the bitter taste of the active pharmaceutical ingredient in ODTs reduces patient compliance. The present study aimed to formulate bitter taste-masked ODTs containing high-dose of memantine hydrochloride (MTN) to achieve a balance between bitterness suppression and dissolution rate or disintegration time and mechanical strength. The high MTN-loaded granules were prepared using a fluidized bed granulator. Taste-masking granules coated with the selected polymer were prepared using the layering technique. Three ODTs, composed of granules coated with different polymers, were prepared. The ODT prepared using granules coated with enteric polymers showed the fastest collapse time (>20 s). Dissolution rates of ODTs composed of enteric polymers were reduced by 5 min compared with ODTs composed of non-coated or coated with water-insoluble polymer granules. X-ray computed tomography analysis revealed that low density distribution of ODTs with enteric polymer granules may result in faster disintegration time. Although ODT prepared using enteric polymers had the fastest collapse time, its change in membrane potential caused by adsorption (CPA), corresponding to aftertaste, was the lowest among formulations. This CPA value was lower than the bitterness threshold.