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Tablet formulation development focusing on the functional behaviour of water uptake and swelling

Lenz, Jan, Bunjes, Heike, Kwade, Arno and Juhnke, Michael (2021) Tablet formulation development focusing on the functional behaviour of water uptake and swelling. International Journal of Pharmaceutics X, 3 (n/a). p. 100103. ISSN 2590-1567


The functional behaviour of tablets is strongly influenced by their manufacturing process and the choice of
excipients. Water uptake and swelling are prerequisites for tablet disintegration, dispersion and hence active
pharmaceutical ingredient (API) dissolution. High proportions of polymeric excipients in tablets, which are
typically used as API carriers in amorphous solid dispersions (ASDs), may be challenging due to the formation of
a gelling polymer network (GPN). In this study, systematic investigations into the formulation development of
tablets containing polymeric and other excipients are performed by water uptake and swelling analysis. The
impact of tablet composition and porosity as well as pH of the test medium are investigated. The pH affects the
analysis results for Eudragit L100–55 and Eudragit EPO. HPMC and Kollidon VA64 inhibit water uptake and
swelling of tablets due to the formation of a GPN. High tablet porosity, coarse particle size of the polymer and the
addition of fillers and disintegrants can reduce the negative impact of a GPN on tablet performance. The
application of lubricants slows down the analysed processes. Water uptake and swelling data are fitted to an
empirical model obtaining four characteristic parameters to facilitate the simple quantitative assessment of
varying tablet formulations and structural properties.

Item Type: Article
Date Deposited: 23 Nov 2021 00:45
Last Modified: 23 Nov 2021 00:45


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