Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator

Continuous manufacturing is becoming the new technological standard in the pharmaceutical industry. In this work, a twin-screw processor was employed for the continuous production of liquisolid tablets containing either simethicone or a combination of simethicone with loperamide hydrochloride. Both...

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Main Authors: Daniel Zakowiecki, Margarethe Richter, Ceren Yuece, Annika Voelp, Maximilian Ries, Markos Papaioannou, Peter Edinger, Tobias Hess, Krystyna Mojsiewicz-Pieńkowska, Krzysztof Cal
Format: Article
Language:English
Published: MDPI AG 2023-04-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/15/4/1265
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author Daniel Zakowiecki
Margarethe Richter
Ceren Yuece
Annika Voelp
Maximilian Ries
Markos Papaioannou
Peter Edinger
Tobias Hess
Krystyna Mojsiewicz-Pieńkowska
Krzysztof Cal
author_facet Daniel Zakowiecki
Margarethe Richter
Ceren Yuece
Annika Voelp
Maximilian Ries
Markos Papaioannou
Peter Edinger
Tobias Hess
Krystyna Mojsiewicz-Pieńkowska
Krzysztof Cal
author_sort Daniel Zakowiecki
collection DOAJ
description Continuous manufacturing is becoming the new technological standard in the pharmaceutical industry. In this work, a twin-screw processor was employed for the continuous production of liquisolid tablets containing either simethicone or a combination of simethicone with loperamide hydrochloride. Both active ingredients present major technological challenges, as simethicone is a liquid, oily substance, and loperamide hydrochloride was used in a very small amount (0.27% <i>w</i>/<i>w</i>). Despite these difficulties, the use of porous tribasic calcium phosphate as a carrier and the adjustment of the settings of the twin-screw processor enabled the optimization of the characteristics of the liquid-loaded powders and made it possible to efficiently produce liquisolid tablets with advantages in physical and functional properties. The application of chemical imaging by means of Raman spectroscopy allowed for the visualization of differences in the distribution of individual components of the formulations. This proved to be a very effective tool for identifying the optimum technology to produce a drug product.
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spelling doaj.art-1a54c7a6b4334e1a98b533798ab3fc012023-11-17T20:55:03ZengMDPI AGPharmaceutics1999-49232023-04-01154126510.3390/pharmaceutics15041265Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw GranulatorDaniel Zakowiecki0Margarethe Richter1Ceren Yuece2Annika Voelp3Maximilian Ries4Markos Papaioannou5Peter Edinger6Tobias Hess7Krystyna Mojsiewicz-Pieńkowska8Krzysztof Cal9Chemische Fabrik Budenheim KG, Rheinstrasse 27, 55257 Budenheim, GermanyThermo Electron (Karlsruhe) GmbH, Pfannkuchstrasse 10-12, 76185 Karlsruhe, GermanyThermo Electron (Karlsruhe) GmbH, Pfannkuchstrasse 10-12, 76185 Karlsruhe, GermanyThermo Electron (Karlsruhe) GmbH, Pfannkuchstrasse 10-12, 76185 Karlsruhe, GermanyThermo Fisher Scientific GmbH, Im Steingrund 4-6, 63303 Dreieich, GermanyChemische Fabrik Budenheim KG, Rheinstrasse 27, 55257 Budenheim, GermanyChemische Fabrik Budenheim KG, Rheinstrasse 27, 55257 Budenheim, GermanyChemische Fabrik Budenheim KG, Rheinstrasse 27, 55257 Budenheim, GermanyDepartment of Physical Chemistry, Faculty of Pharmacy, Medical University of Gdansk, al. Gen. J. Hallera 107, 80-416 Gdansk, PolandDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Gdansk, al. Gen. J. Hallera 107, 80-416 Gdansk, PolandContinuous manufacturing is becoming the new technological standard in the pharmaceutical industry. In this work, a twin-screw processor was employed for the continuous production of liquisolid tablets containing either simethicone or a combination of simethicone with loperamide hydrochloride. Both active ingredients present major technological challenges, as simethicone is a liquid, oily substance, and loperamide hydrochloride was used in a very small amount (0.27% <i>w</i>/<i>w</i>). Despite these difficulties, the use of porous tribasic calcium phosphate as a carrier and the adjustment of the settings of the twin-screw processor enabled the optimization of the characteristics of the liquid-loaded powders and made it possible to efficiently produce liquisolid tablets with advantages in physical and functional properties. The application of chemical imaging by means of Raman spectroscopy allowed for the visualization of differences in the distribution of individual components of the formulations. This proved to be a very effective tool for identifying the optimum technology to produce a drug product.https://www.mdpi.com/1999-4923/15/4/1265continuous manufacturingliquisolid tabletssimethiconeloperamide hydrochloridetwin-screw granulatortribasic calcium phosphate
spellingShingle Daniel Zakowiecki
Margarethe Richter
Ceren Yuece
Annika Voelp
Maximilian Ries
Markos Papaioannou
Peter Edinger
Tobias Hess
Krystyna Mojsiewicz-Pieńkowska
Krzysztof Cal
Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator
Pharmaceutics
continuous manufacturing
liquisolid tablets
simethicone
loperamide hydrochloride
twin-screw granulator
tribasic calcium phosphate
title Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator
title_full Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator
title_fullStr Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator
title_full_unstemmed Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator
title_short Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator
title_sort towards the continuous manufacturing of liquisolid tablets containing simethicone and loperamide hydrochloride with the use of a twin screw granulator
topic continuous manufacturing
liquisolid tablets
simethicone
loperamide hydrochloride
twin-screw granulator
tribasic calcium phosphate
url https://www.mdpi.com/1999-4923/15/4/1265
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