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Solubility, Crystallization, and Characterization of Cytidine Sulfate

[Image: see text] Cytidine is an important kind of nucleoside that can be applied to drug development and food industry. Cytidine sulfate is one of its popular forms, which is promising as a medicinal intermediate, especially in antiviral and antitumor drugs. Product refining is the key point of ind...

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Autores principales: Leng, Fan, Zhou, Shuyang, Li, Shushu, Xu, Mengjie, Zhang, Keke, Guo, Ting, Chen, Tianpeng, Yang, Pengpeng
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2023
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10357447/
https://www.ncbi.nlm.nih.gov/pubmed/37483214
http://dx.doi.org/10.1021/acsomega.3c02501
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author Leng, Fan
Zhou, Shuyang
Li, Shushu
Xu, Mengjie
Zhang, Keke
Guo, Ting
Chen, Tianpeng
Yang, Pengpeng
author_facet Leng, Fan
Zhou, Shuyang
Li, Shushu
Xu, Mengjie
Zhang, Keke
Guo, Ting
Chen, Tianpeng
Yang, Pengpeng
author_sort Leng, Fan
collection PubMed
description [Image: see text] Cytidine is an important kind of nucleoside that can be applied to drug development and food industry. Cytidine sulfate is one of its popular forms, which is promising as a medicinal intermediate, especially in antiviral and antitumor drugs. Product refining is the key point of industrial development, and crystallization is a significant way of refining. In this work, the solubility of cytidine sulfate in pure water from 278.15 to 328.15 K and in water–ethanol binary solvents at 298.15 K was measured by the UV spectroscopic method. The solubility data were correlated with temperature and solvent composition using the modified Apelblat, van’t Hoff, and CNIBS/R-K equations. On this basis, we investigated and compared three crystallization processes, and the coupling method was developed to prepare crystals with a large particle size, concentrated distribution, and high yield and packing density. In addition, the structure and stability of the products were characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, and dynamic vapor sorption analysis. It was found that cytidine sulfate has only one crystal form in our research process, and the product of coupling crystallization is stable and favorable for industrial development.
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spelling pubmed-103574472023-07-21 Solubility, Crystallization, and Characterization of Cytidine Sulfate Leng, Fan Zhou, Shuyang Li, Shushu Xu, Mengjie Zhang, Keke Guo, Ting Chen, Tianpeng Yang, Pengpeng ACS Omega [Image: see text] Cytidine is an important kind of nucleoside that can be applied to drug development and food industry. Cytidine sulfate is one of its popular forms, which is promising as a medicinal intermediate, especially in antiviral and antitumor drugs. Product refining is the key point of industrial development, and crystallization is a significant way of refining. In this work, the solubility of cytidine sulfate in pure water from 278.15 to 328.15 K and in water–ethanol binary solvents at 298.15 K was measured by the UV spectroscopic method. The solubility data were correlated with temperature and solvent composition using the modified Apelblat, van’t Hoff, and CNIBS/R-K equations. On this basis, we investigated and compared three crystallization processes, and the coupling method was developed to prepare crystals with a large particle size, concentrated distribution, and high yield and packing density. In addition, the structure and stability of the products were characterized by powder X-ray diffraction, Fourier transform infrared spectroscopy, thermogravimetric analysis, differential scanning calorimetry, and dynamic vapor sorption analysis. It was found that cytidine sulfate has only one crystal form in our research process, and the product of coupling crystallization is stable and favorable for industrial development. American Chemical Society 2023-07-07 /pmc/articles/PMC10357447/ /pubmed/37483214 http://dx.doi.org/10.1021/acsomega.3c02501 Text en © 2023 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Leng, Fan
Zhou, Shuyang
Li, Shushu
Xu, Mengjie
Zhang, Keke
Guo, Ting
Chen, Tianpeng
Yang, Pengpeng
Solubility, Crystallization, and Characterization of Cytidine Sulfate
title Solubility, Crystallization, and Characterization of Cytidine Sulfate
title_full Solubility, Crystallization, and Characterization of Cytidine Sulfate
title_fullStr Solubility, Crystallization, and Characterization of Cytidine Sulfate
title_full_unstemmed Solubility, Crystallization, and Characterization of Cytidine Sulfate
title_short Solubility, Crystallization, and Characterization of Cytidine Sulfate
title_sort solubility, crystallization, and characterization of cytidine sulfate
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10357447/
https://www.ncbi.nlm.nih.gov/pubmed/37483214
http://dx.doi.org/10.1021/acsomega.3c02501
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