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Solubility, Crystallization, and Characterization of Cytidine Sulfate
ACS Omega ( IF 3.7 ) Pub Date : 2023-07-07 , DOI: 10.1021/acsomega.3c02501 Fan Leng 1 , Shuyang Zhou 1 , Shushu Li 1 , Mengjie Xu 1 , Keke Zhang 2 , Ting Guo 3 , Tianpeng Chen 1 , Pengpeng Yang 1
ACS Omega ( IF 3.7 ) Pub Date : 2023-07-07 , DOI: 10.1021/acsomega.3c02501 Fan Leng 1 , Shuyang Zhou 1 , Shushu Li 1 , Mengjie Xu 1 , Keke Zhang 2 , Ting Guo 3 , Tianpeng Chen 1 , Pengpeng Yang 1
Affiliation
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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.
中文翻译：
硫酸胞苷的溶解度、结晶和表征
胞苷是一种重要的核苷，可应用于药物开发和食品工业。硫酸胞苷是其流行的形式之一，作为医药中间体很有前景，特别是在抗病毒和抗肿瘤药物中。产品精制是产业发展的关键，而结晶是一种重要的精制方式。在这项工作中，通过紫外光谱法测量了硫酸胞苷在278.15至328.15 K的纯水中和298.15 K的水-乙醇二元溶剂中的溶解度。使用改进的 Apelblat、van't Hoff 和 CNIBS/RK 方程将溶解度数据与温度和溶剂组成相关联。在此基础上，我们对三种结晶工艺进行了研究和比较，开发了耦合法，制备出粒径大、分布集中、收率和堆积密度高的晶体。此外，通过粉末X射线衍射、傅里叶变换红外光谱、热重分析、差示扫描量热法、动态蒸气吸附分析等手段对产物的结构和稳定性进行了表征。我们的研究过程中发现硫酸胞苷只有一种晶型，偶联结晶产物稳定，有利于产业化发展。
更新日期：2023-07-07
中文翻译：
硫酸胞苷的溶解度、结晶和表征
胞苷是一种重要的核苷，可应用于药物开发和食品工业。硫酸胞苷是其流行的形式之一，作为医药中间体很有前景，特别是在抗病毒和抗肿瘤药物中。产品精制是产业发展的关键，而结晶是一种重要的精制方式。在这项工作中，通过紫外光谱法测量了硫酸胞苷在278.15至328.15 K的纯水中和298.15 K的水-乙醇二元溶剂中的溶解度。使用改进的 Apelblat、van't Hoff 和 CNIBS/RK 方程将溶解度数据与温度和溶剂组成相关联。在此基础上，我们对三种结晶工艺进行了研究和比较，开发了耦合法，制备出粒径大、分布集中、收率和堆积密度高的晶体。此外，通过粉末X射线衍射、傅里叶变换红外光谱、热重分析、差示扫描量热法、动态蒸气吸附分析等手段对产物的结构和稳定性进行了表征。我们的研究过程中发现硫酸胞苷只有一种晶型，偶联结晶产物稳定，有利于产业化发展。
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