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Pharmaceutical cocrystals and salts of enrofloxacin: Structure and properties
Journal of Molecular Structure ( IF 3.8 ) Pub Date : 2022-05-19 , DOI: 10.1016/j.molstruc.2022.133335
Shuang-Yun Yang , Fei-Ke Zhao , Hong Pang , Liang-Zhu Chen , Ren-Bin Shi , Bing-Hu Fang

Enrofloxacin, a second-generation quinolone broad-spectrum antimicrobial, has limited application because of its poor solubility. The purpose of this paper was to investigate the structure and properties of newly generated enrofloxacin salts and cocrystals. The crystal structures and properties of enrofloxacin vanillin cocrystal (EFC-VNL) (1), enrofloxacin sebacate (EFC-SBA) (2), enrofloxacin malate trihydrate (EFC-MAL-3H2O) (3), enrofloxacin adipate-EtOH Salt Solvate (EFC-ADH) (4) were characterized by single crystal X-ray diffraction, powder X-ray diffraction, Fourier-transform infrared spectroscopy, and thermal difference analysis. All compounds were synthesized by slow volatilization of organic solvents at room temperature. The solubility of these salts and cocrystals in water was measured by high-performance liquid chromatography. The results showed that the newly generated enrofloxacin cocrystals and salts had higher aqueous solubility than enrofloxacin.



中文翻译:

恩诺沙星的药物共晶体和盐:结构和性质

恩诺沙星是第二代喹诺酮类广谱抗菌药物,由于溶解度差,应用有限。本文的目的是研究新生成的恩诺沙星盐和共晶体的结构和性质。恩诺沙星香草醛共晶体 (EFC-VNL) (1)、癸二酸恩诺沙星 (EFC-SBA) (2)、苹果酸恩诺沙星三水合物 (EFC-MAL-3H 2 ) 的晶体结构和性质O)(3)、恩诺沙星己二酸乙醇盐溶剂化物(EFC-ADH)(4)通过单晶X射线衍射、粉末X射线衍射、傅里叶变换红外光谱和热差分析进行了表征。所有化合物均通过有机溶剂在室温下缓慢挥发而合成。通过高效液相色谱法测量这些盐和共晶体在水中的溶解度。结果表明,新生成的恩诺沙星共晶和盐的水溶性高于恩诺沙星。

更新日期:2022-05-19
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