Preparation of bitter taste-masking granules of lafutidine for orally disintegrating tablets using water-insoluble/soluble polymer combinations

Taste-masking granules were prepared by coating granules with a taste-masking layer prepared by combining the water-insoluble and -soluble polymers, ethylcellulose and hypromellose, respectively. These granules showed an immediate drug release property after a suitable lag time. We confirmed that the dissolution behavior depended on the polymer ratio in the taste-masking layer. The result showed that the dissolution lag time and rate of the taste-masking granules were shortened and enhanced, respectively by increasing the hypromellose content. Films with the same polymer ratio as the taste-masking layer were prepared, and their physical properties were measured to evaluate the relationship between the dissolution behavior and the film properties. The tensile strength of the films decreased with an increasing concentration of hypromellose. Furthermore, there was a relationship between the tensile strength of the films and dissolution rate of the taste-masking granules. The lag time was significantly shortened when the hypromellose blending ratio exceeded 20%, and this change was suggested to be associated with the water permeability of the film. These results indicate that the tensile strength and water permeability of the films were influenced by the polymer ratio, which also influenced the dissolution behavior of the taste-masking granule.

Schematic representation of taste-masking granule structure.Figure optionsDownload as PowerPoint slide