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Terahertz Spectroscopy for Non-Destructive Solid-State Investigation of Norfloxacin in Paper Tablets after Wet Granulation

(1) Background: Amorphous drug systems are an intensively studied approach to overcome the insufficient bioavailability of poorly soluble drugs. Here, paper tablets were studied, which were made from cellulose-based paper matrices loaded with norfloxacin. Moreover, wet granulation was introduced as...

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Autores principales: Heidrich, Lara, Abdelkader, Ayat, Ornik, Jan, Castro-Camus, Enrique, Keck, Cornelia M., Koch, Martin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10386691/
https://www.ncbi.nlm.nih.gov/pubmed/37513973
http://dx.doi.org/10.3390/pharmaceutics15071786
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author Heidrich, Lara
Abdelkader, Ayat
Ornik, Jan
Castro-Camus, Enrique
Keck, Cornelia M.
Koch, Martin
author_facet Heidrich, Lara
Abdelkader, Ayat
Ornik, Jan
Castro-Camus, Enrique
Keck, Cornelia M.
Koch, Martin
author_sort Heidrich, Lara
collection PubMed
description (1) Background: Amorphous drug systems are an intensively studied approach to overcome the insufficient bioavailability of poorly soluble drugs. Here, paper tablets were studied, which were made from cellulose-based paper matrices loaded with norfloxacin. Moreover, wet granulation was introduced as an additional processing step for improving the flowability of the solids, which is necessary when considering production on an industrial scale. (2) Methods: The possible impact of the wet granulation on the crystallinity of norfloxacin was studied by examining granulated and non-granulated samples. Crystallinity investigations were performed using X-ray powder diffraction (XRD) and terahertz time-domain spectroscopy (THz TDS). (3) Results: THz TDS allowed for a more straightforward crystallinity assessment than XRD. Moreover, using THz TDS, it was possible to detect minor changes in the crystallinity of the API after the granulation, whereas this was not possible with the XRD analysis. (4) Conclusions: THz TDS results indicate a partial crystallization of norfloxacin due to the wet granulation. Depending on the formulation, THz TDS can serve as a beneficial and advantageous tool to determine the crystallinity of an API.
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spelling pubmed-103866912023-07-30 Terahertz Spectroscopy for Non-Destructive Solid-State Investigation of Norfloxacin in Paper Tablets after Wet Granulation Heidrich, Lara Abdelkader, Ayat Ornik, Jan Castro-Camus, Enrique Keck, Cornelia M. Koch, Martin Pharmaceutics Article (1) Background: Amorphous drug systems are an intensively studied approach to overcome the insufficient bioavailability of poorly soluble drugs. Here, paper tablets were studied, which were made from cellulose-based paper matrices loaded with norfloxacin. Moreover, wet granulation was introduced as an additional processing step for improving the flowability of the solids, which is necessary when considering production on an industrial scale. (2) Methods: The possible impact of the wet granulation on the crystallinity of norfloxacin was studied by examining granulated and non-granulated samples. Crystallinity investigations were performed using X-ray powder diffraction (XRD) and terahertz time-domain spectroscopy (THz TDS). (3) Results: THz TDS allowed for a more straightforward crystallinity assessment than XRD. Moreover, using THz TDS, it was possible to detect minor changes in the crystallinity of the API after the granulation, whereas this was not possible with the XRD analysis. (4) Conclusions: THz TDS results indicate a partial crystallization of norfloxacin due to the wet granulation. Depending on the formulation, THz TDS can serve as a beneficial and advantageous tool to determine the crystallinity of an API. MDPI 2023-06-21 /pmc/articles/PMC10386691/ /pubmed/37513973 http://dx.doi.org/10.3390/pharmaceutics15071786 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Heidrich, Lara
Abdelkader, Ayat
Ornik, Jan
Castro-Camus, Enrique
Keck, Cornelia M.
Koch, Martin
Terahertz Spectroscopy for Non-Destructive Solid-State Investigation of Norfloxacin in Paper Tablets after Wet Granulation
title Terahertz Spectroscopy for Non-Destructive Solid-State Investigation of Norfloxacin in Paper Tablets after Wet Granulation
title_full Terahertz Spectroscopy for Non-Destructive Solid-State Investigation of Norfloxacin in Paper Tablets after Wet Granulation
title_fullStr Terahertz Spectroscopy for Non-Destructive Solid-State Investigation of Norfloxacin in Paper Tablets after Wet Granulation
title_full_unstemmed Terahertz Spectroscopy for Non-Destructive Solid-State Investigation of Norfloxacin in Paper Tablets after Wet Granulation
title_short Terahertz Spectroscopy for Non-Destructive Solid-State Investigation of Norfloxacin in Paper Tablets after Wet Granulation
title_sort terahertz spectroscopy for non-destructive solid-state investigation of norfloxacin in paper tablets after wet granulation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10386691/
https://www.ncbi.nlm.nih.gov/pubmed/37513973
http://dx.doi.org/10.3390/pharmaceutics15071786
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