Cocrystal of Sulfamethazine and p-Aminobenzoic Acid: Structural Establishment and Enhanced Antibacterial Properties

文献类型： 外文期刊

第一作者： Pan, Xiaohong

作者： Pan, Xiaohong;Zheng, Yilin;Chen, Ron;Qiu, Saifei;Rao, Wenhua;Chen, Saili;You, Yuxin;Guan, Xiong;Pan, Xiaohong;Zheng, Yilin;Chen, Ron;Qiu, Saifei;Rao, Wenhua;Chen, Saili;You, Yuxin;Guan, Xiong;Chen, Zhi;Lu, Jian;Lu, Jian;Xu, Lei

作者机构：

期刊名称：CRYSTAL GROWTH & DESIGN （ 影响因子：4.076； 五年影响因子：3.924 ）

ISSN： 1528-7483

年卷期： 2019 年 19 卷 4 期

页码：

收录情况： SCI

摘要： The engineering of pharmaceutical cocrystals has been effectively utilized to improve the physicochemical properties such as stability and solubility, and thus it could optimize the solid formations of active pharmaceutical ingredients. This work focuses on the sulfamethazine p-aminobenzoic acid (STH-PABA) cocrystal regulated by molecular synthons constructed from mutual N center dot center dot center dot H center dot center dot center dot o interactions. The STH-PABA cocrystal was produced by means of the slow evaporation crystallization method, and the cocrystal structure was determined through X-ray crystallography. Meanwhile, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Fourier transform infrared spectroscopy, Raman, and NMR were applied to analyze the features of the STH-PABA cocrystal. Special attention was paid to in vitro antibacterial activity and microscopic investigations. Our findings indicated that the formation of cocrystals could enhance the solubility and slightly improve the release behavior of STH, and increase the leaking of bacterial cell inclusion that leads to enhanced antibacterial activity.

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