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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...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2023
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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. |
format | Online Article Text |
id | pubmed-10320128 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
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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