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晶体工程改善硝苯地平光稳定性研究

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为改善硝苯地平光稳定性差的问题,本研究基于晶体工程原理设计共晶并采用悬浮液法制备得到硝苯地平-咪唑新共晶。利用粉末X-射线衍射法、红外光谱法、差示扫描量热法、热重分析法对新共晶进行表征,确证共晶物质的形成。使用粉末X-射线衍射法与高效液相色谱法考察了硝苯地平原料和共晶的光稳定性。结果表明,硝苯地平-咪唑共晶在一定程度上改善了硝苯地平的光敏性。本研究为硝苯地平共晶开发以及成药性改善提供指导。
Study on improving the photostability of nifedipine by crystal engineering
In order to improve the poor photostability of nifedipine,this study designed a cocrystal based on the principles of crystal engineering and prepared nifedipine-imidazole cocrystal by suspension method.The new cocrystal was characterized by powder X-ray diffraction(PXRD),differential scanning calorimetry(DSC),thermogravimetric analysis(TG)and infrared spectroscopy(IR)to confirm the formation of the cocrystal.The photostability of nifedipine and its cocrystal was measured by powder X-ray diffraction and high-performance liquid chromatography(HPLC).The results showed that the nifedipine-imidazole cocrystal improved the photostability of nifedipine to a certain extent.This study provides guidance for the development of nifedipine cocrystals and the improvement of its druggability.

crystal engineeringnifedipinecocrystalcharacterizationphotostability

孟欣、邹瑶、刘梅菊、邢逞、龚宁波、吕扬

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北京协和医学院、中国医学科学院药物研究所,晶型药物研究北京市重点实验室,北京 100050

晶体工程 硝苯地平 共晶 表征 光稳定性

2024

药学学报
中国药学会 中国医学科学院药物研究所

药学学报

CSTPCD北大核心
影响因子:1.274
ISSN:0513-4870
年,卷(期):2024.59(12)