GRANFILLER-D™ Water Absorption Behavior and Disintegration Mechanism

In the formulation design of conventional orally disintegrating tablets (ODTs) by direct compression, disintegratablity often reduces when active pharmaceutical ingredient (API) content is high. Since API tends to block the gap between particles in tablets, which is considered to be the main water absorption pathway, water is prevented from reaching disintegrants. In contrast, GRANFILLER-D (GNF), Daicel’s co-processed excipient (CPE) for ODTs, shows excellent disintegration performance even in case of high-dose APIs. It was suggested that GNF seems to have another water absorption pathway besides the gap between particles. Here we make a hypothesis that GNF particles themselves have a water conducting function. In this study, we observed its water absorption behavior in disintegrating tablets and verified this hypothesis while making a comparison with other CPEs for ODT.

We analyzed the initial state of disintegration and water absorption behavior of tablets by using X-ray. In case of tablet with GNF, water absorption was proceeded more smoothly and homogeneously than other samples. GNF was also found that fine disintegration proceeded directly at a primary particle level rather than at a granulated aggregate level. From these results, it can be assumed that tablet with GNF has a fine water pathway besides gaps between particles.

Next, the relation between porosity and disintegration time of ODTs with various CPEs was investigated by M. Kokott, et al. Tablet with GNF maintains short disintegration time being less than 30 seconds over a wide range of porosity. Therefore, the disintegration of tablet with GNF is hardly affected by the porosity.

These results showed that GNF particles themselves seem to function as a water absorption pathway besides the gap in tablets. We assume that this is the reason why GNF shows excellent disintegration even with high API content or high tableting pressures. GNF is a versatile excipient that shows high performance even in complex formulations and it has been adapted to several marketed products.

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