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A method for improving the properties of famotidine

According to crystal engineering, the pharmaceutical intermediate m-nitrobenzoic acid (MNBA), which contains a carboxylic acid group, was selected as a coformer (CCF) for drug cocrystallization with famotidine (FMT), and a new stable FMT salt cocrystal was synthesized. The salt cocrystals were chara...

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Detalles Bibliográficos
Autores principales: Zhao, Yongfeng, Fan, Ying, Zhang, Yan, Xu, Hong, Li, Min, Zhu, Yunjie, Yang, Zhao
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10320128/
https://www.ncbi.nlm.nih.gov/pubmed/37416673
http://dx.doi.org/10.1016/j.heliyon.2023.e17494
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author Zhao, Yongfeng
Fan, Ying
Zhang, Yan
Xu, Hong
Li, Min
Zhu, Yunjie
Yang, Zhao
author_facet Zhao, Yongfeng
Fan, Ying
Zhang, Yan
Xu, Hong
Li, Min
Zhu, Yunjie
Yang, Zhao
author_sort Zhao, Yongfeng
collection PubMed
description According to crystal engineering, the pharmaceutical intermediate m-nitrobenzoic acid (MNBA), which contains a carboxylic acid group, was selected as a coformer (CCF) for drug cocrystallization with famotidine (FMT), and a new stable FMT salt cocrystal was synthesized. The salt cocrystals were characterized by scanning electron microscopy, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy, powder X-ray diffraction and X-ray single crystal diffraction. A single crystal structure of FMT–MNBA (1:1) was successfully obtained, and then the solubility and permeability of the newly synthesized salt cocrystal were studied. The results showed that, compared with free FMT, the FMT from the FMT–MNBA cocrystal showed improved permeability. This study provides a synthetic method to improve the permeability of BCS III drugs, which will contribute to the development of low-permeability drugs.
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spelling pubmed-103201282023-07-06 A method for improving the properties of famotidine Zhao, Yongfeng Fan, Ying Zhang, Yan Xu, Hong Li, Min Zhu, Yunjie Yang, Zhao Heliyon Research Article According to crystal engineering, the pharmaceutical intermediate m-nitrobenzoic acid (MNBA), which contains a carboxylic acid group, was selected as a coformer (CCF) for drug cocrystallization with famotidine (FMT), and a new stable FMT salt cocrystal was synthesized. The salt cocrystals were characterized by scanning electron microscopy, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy, powder X-ray diffraction and X-ray single crystal diffraction. A single crystal structure of FMT–MNBA (1:1) was successfully obtained, and then the solubility and permeability of the newly synthesized salt cocrystal were studied. The results showed that, compared with free FMT, the FMT from the FMT–MNBA cocrystal showed improved permeability. This study provides a synthetic method to improve the permeability of BCS III drugs, which will contribute to the development of low-permeability drugs. Elsevier 2023-06-21 /pmc/articles/PMC10320128/ /pubmed/37416673 http://dx.doi.org/10.1016/j.heliyon.2023.e17494 Text en © 2023 Published by Elsevier Ltd. https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Research Article
Zhao, Yongfeng
Fan, Ying
Zhang, Yan
Xu, Hong
Li, Min
Zhu, Yunjie
Yang, Zhao
A method for improving the properties of famotidine
title A method for improving the properties of famotidine
title_full A method for improving the properties of famotidine
title_fullStr A method for improving the properties of famotidine
title_full_unstemmed A method for improving the properties of famotidine
title_short A method for improving the properties of famotidine
title_sort method for improving the properties of famotidine
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10320128/
https://www.ncbi.nlm.nih.gov/pubmed/37416673
http://dx.doi.org/10.1016/j.heliyon.2023.e17494
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