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Novel Cocrystals and Eutectics of the Antiprotozoal Tinidazole: Mechanochemical Synthesis, Cocrystallization, and Characterization
Crystal Growth & Design ( IF 3.8 ) Pub Date : 2020-03-27 , DOI: 10.1021/acs.cgd.9b01435
Octavio E. Fandiño 1 , Lucía Reviglio 2 , Yamila Garro Linck 2 , Gustavo A. Monti 2 , Marina M. Marcos Valdez 1 , Sonia N. Faudone 3 , Mino R. Caira 4 , Norma R. Sperandeo 1
Affiliation  

Antiprotozoal tinidazole (TNZ) exhibits low aqueous solubility (Sw) and poor photochemical stability. In this work, TNZ was used to form cocrystals and eutectics with the aim of enhancing its solubility and physical stability. The choice of coformers was based on a crystal engineering strategy focused on the success rate of supramolecular heterosynthon formation between azoles and carboxylic acids. By liquid-assisted grinding, three cocrystals [with p-aminobenzoic acid (PABA), citric acid (CA), and salicylic acid (SA)] and two eutectics [with nicotinamide and succinic acid] were obtained and characterized using powder X-ray diffraction, 13C solid-state nuclear magnetic resonance, infrared spectroscopy, differential scanning calorimetry, thermogravimetry, and hot-stage microscopy. The crystal structures of TNZ-PABA and TNZ-SA were resolved by means of single-crystal X-ray diffraction, which revealed that they are a solvated and an unsolvated cocrystal, respectively. The Sw values of the obtained samples were determined at 37 °C, with the outcome that only the TNZ-CA cocrystal had a slightly higher Sw than pure TNZ. A physical stability study was also performed under UV–visible irradiation, and it was found that the three cocrystals showed better photostability when compared to TNZ, the two eutectics, and each respective physical mixture, a finding that could be relevant from the pharmacotechnical point of view.

中文翻译:

反原生动物替硝唑的新型共晶体和共晶:力学化学合成,共结晶和表征

抗原生动物替硝唑(TNZ)的水溶解度(Sw)低,光化学稳定性差。在这项工作中,使用TNZ形成共晶和共晶,以提高其溶解度和物理稳定性。共聚物的选择基于晶体工程策略,该策略的重点是在吡咯和羧酸之间形成超分子杂合子。通过液体辅助研磨,获得了三个共晶[与氨基苯甲酸(PABA),柠檬酸(CA)和水杨酸(SA)]和两个共晶物(与烟酰胺和琥珀酸一起)并用粉末X射线表征衍射13C固态核磁共振,红外光谱,差示扫描量热法,热重分析和热台显微镜。通过单晶X射线衍射解析了TNZ-PABA和TNZ-SA的晶体结构,这表明它们分别是溶剂化的和非溶剂化的共晶体。在37°C下确定获得的样品的Sw值,结果是只有TNZ-CA共晶体的Sw略高于纯TNZ。还在紫外可见光下进行了物理稳定性研究,结果发现与TNZ,两种低共熔晶体和每种物理混合物相比,三种共晶体表现出更好的光稳定性,这一发现可能与药物技术方面有关。视图。
更新日期:2020-03-27
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