Effect of superdisintegrants on dissolution of cationic drugs

Abstract

The effects of selected superdisintegrants on the dissolution behavior of several cationic drugs with varying water solubility were evaluated. All formulations were made with fixed disintegrant concentration and equal drug load using a model formulation. Tablets were made by direct compression and were compressed to equal hardness. Dissolution studies were carried out in dissolution media specified in the compendium (USP) or in media recommended by the U.S. Food and Drug Administration (FDA) for the respective actives. The effect of media pH on the dissolution of drugs was also evaluated. The use of crospovidone significantly improved the dissolution of the cationic drugs in the model formulation when compared with the other superdisintegrants studied. The compendial or the FDA recommended media, in most cases, was able to discriminate among the tablets containing different superdisintegrants. Crospovidone can be effectively used as a tablet disintegrant to improve the dissolution of either soluble or poorly soluble cationic drugs.