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Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid

[Image: see text] BBC is a drug with a variety of activities but poor solubility. Cocrystal technology is an effective method to improve the solubility and stability of this type of compound. In this work, the cocrystal of BBC with fumaric acid was obtained at a stoichiometric ratio of 2:1. Studies...

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Autores principales: Yang, Dezhi, Cao, Junzi, Jiao, Lingtai, Yang, Shiying, Zhang, Li, Lu, Yang, Du, Guanhua
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7161028/
https://www.ncbi.nlm.nih.gov/pubmed/32309739
http://dx.doi.org/10.1021/acsomega.0c00692
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author Yang, Dezhi
Cao, Junzi
Jiao, Lingtai
Yang, Shiying
Zhang, Li
Lu, Yang
Du, Guanhua
author_facet Yang, Dezhi
Cao, Junzi
Jiao, Lingtai
Yang, Shiying
Zhang, Li
Lu, Yang
Du, Guanhua
author_sort Yang, Dezhi
collection PubMed
description [Image: see text] BBC is a drug with a variety of activities but poor solubility. Cocrystal technology is an effective method to improve the solubility and stability of this type of compound. In this work, the cocrystal of BBC with fumaric acid was obtained at a stoichiometric ratio of 2:1. Studies on stabilities and solubilities were carried out using BBC dihydrate and tetrahydrate as reference materials. Results showed that this new cocrystal did not only significantly improve the dissolution rate of BBC but also highly improved the stability in high humidity and temperature. Given that the cocrystals formed by BBC as the host molecule were few, different techniques were applied for characterization and structural analyses. Moreover, theoretical calculations were performed on weak interactions, such as hydrogen bonding and π–π stacking interactions, which provided the research data for the study of this kind of cocrystal.
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spelling pubmed-71610282020-04-17 Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid Yang, Dezhi Cao, Junzi Jiao, Lingtai Yang, Shiying Zhang, Li Lu, Yang Du, Guanhua ACS Omega [Image: see text] BBC is a drug with a variety of activities but poor solubility. Cocrystal technology is an effective method to improve the solubility and stability of this type of compound. In this work, the cocrystal of BBC with fumaric acid was obtained at a stoichiometric ratio of 2:1. Studies on stabilities and solubilities were carried out using BBC dihydrate and tetrahydrate as reference materials. Results showed that this new cocrystal did not only significantly improve the dissolution rate of BBC but also highly improved the stability in high humidity and temperature. Given that the cocrystals formed by BBC as the host molecule were few, different techniques were applied for characterization and structural analyses. Moreover, theoretical calculations were performed on weak interactions, such as hydrogen bonding and π–π stacking interactions, which provided the research data for the study of this kind of cocrystal. American Chemical Society 2020-04-06 /pmc/articles/PMC7161028/ /pubmed/32309739 http://dx.doi.org/10.1021/acsomega.0c00692 Text en Copyright © 2020 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Yang, Dezhi
Cao, Junzi
Jiao, Lingtai
Yang, Shiying
Zhang, Li
Lu, Yang
Du, Guanhua
Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid
title Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid
title_full Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid
title_fullStr Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid
title_full_unstemmed Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid
title_short Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid
title_sort solubility and stability advantages of a new cocrystal of berberine chloride with fumaric acid
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7161028/
https://www.ncbi.nlm.nih.gov/pubmed/32309739
http://dx.doi.org/10.1021/acsomega.0c00692
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