Comparative Study of Disintegrating Agents in Tiaramide Hydrochloride Tablets

Abstract

The water sorption properties of some commonly used disintegrants (i.e., starch, sodium starch glycolate, croscarmellose sodium, crospovidone and alginic acid) were studied to correlate the disintegration and physical mechanical properties of tiaramide hydrochloride tablets containing 5% of these disintegrants. With the exception of alginic acid, disintegration time of tablets decreased with the increase in water sorption properties of the disintegrants.When exposed to high humidity (100% RH at 35°C), tablets containing two high water-sorbing disintegrants, e.g., croscarmellose sodium and crospovidone, exhibited a marked decrease in hardness. When these tablets were dried after exposure to humidity, the hardness remained lower than the initial values. It is possible that high water affinity of the disintegrants disrupts the interparticulate bonds inside the tablets. However, such a decrease in interparticulate bond may not be observed if the disintegrant also acts as a binder in the presence of water. For example, the hardness of tablets containing another high water-sorbing disintegrant, sodium starch glycolate, increased when these tablets dried after exposure to high humidity. Unlike croscarmellose sodium and crospovidone, sodium starch glycolate also increased the disintegration time if tablets were previously exposed to high humidity. Studies of the moisture absorption and drying cycle may be very important in evaluating environmental effects of tablets containing high watersorbing disintegrants.