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

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 excipi...

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Autores principales: Jan Lenz, Jan Henrik Finke, Heike Bunjes, Arno Kwade, Michael Juhnke
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Lenguaje:EN
Publicado: Elsevier 2021
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spelling oai:doaj.org-article:29bba37f55714ef4ad67bfa2774cadac2021-11-06T04:35:51ZTablet formulation development focusing on the functional behaviour of water uptake and swelling2590-156710.1016/j.ijpx.2021.100103https://doaj.org/article/29bba37f55714ef4ad67bfa2774cadac2021-12-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S2590156721000323https://doaj.org/toc/2590-1567The 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.Jan LenzJan Henrik FinkeHeike BunjesArno KwadeMichael JuhnkeElsevierarticleWater uptakeSwellingTablet performancePharmaceutical polymersAmorphous solid dispersionsGellingPharmacy and materia medicaRS1-441ENInternational Journal of Pharmaceutics: X, Vol 3, Iss , Pp 100103- (2021)
institution DOAJ
collection DOAJ
language EN
topic Water uptake
Swelling
Tablet performance
Pharmaceutical polymers
Amorphous solid dispersions
Gelling
Pharmacy and materia medica
RS1-441
spellingShingle Water uptake
Swelling
Tablet performance
Pharmaceutical polymers
Amorphous solid dispersions
Gelling
Pharmacy and materia medica
RS1-441
Jan Lenz
Jan Henrik Finke
Heike Bunjes
Arno Kwade
Michael Juhnke
Tablet formulation development focusing on the functional behaviour of water uptake and swelling
description 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.
format article
author Jan Lenz
Jan Henrik Finke
Heike Bunjes
Arno Kwade
Michael Juhnke
author_facet Jan Lenz
Jan Henrik Finke
Heike Bunjes
Arno Kwade
Michael Juhnke
author_sort Jan Lenz
title Tablet formulation development focusing on the functional behaviour of water uptake and swelling
title_short Tablet formulation development focusing on the functional behaviour of water uptake and swelling
title_full Tablet formulation development focusing on the functional behaviour of water uptake and swelling
title_fullStr Tablet formulation development focusing on the functional behaviour of water uptake and swelling
title_full_unstemmed Tablet formulation development focusing on the functional behaviour of water uptake and swelling
title_sort tablet formulation development focusing on the functional behaviour of water uptake and swelling
publisher Elsevier
publishDate 2021
url https://doaj.org/article/29bba37f55714ef4ad67bfa2774cadac
work_keys_str_mv AT janlenz tabletformulationdevelopmentfocusingonthefunctionalbehaviourofwateruptakeandswelling
AT janhenrikfinke tabletformulationdevelopmentfocusingonthefunctionalbehaviourofwateruptakeandswelling
AT heikebunjes tabletformulationdevelopmentfocusingonthefunctionalbehaviourofwateruptakeandswelling
AT arnokwade tabletformulationdevelopmentfocusingonthefunctionalbehaviourofwateruptakeandswelling
AT michaeljuhnke tabletformulationdevelopmentfocusingonthefunctionalbehaviourofwateruptakeandswelling
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