Pharmaceutical Cocrystals of Nicorandil with Enhanced Chemical Stability and Sustained Release,Crystal Growth & Design

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Pharmaceutical Cocrystals of Nicorandil with Enhanced Chemical Stability and Sustained Release
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2020-09-09 , DOI: 10.1021/acs.cgd.0c01043
Chunyang Guo _{1,

2} , Qi Zhang ₃ , Bingqing Zhu ₃ , Zaiyong Zhang ₃ , Junjie Bao ₃ , Qiaoce Ding ₃ , Guobin Ren _{1,

2} , Xuefeng Mei ₃

Affiliation

Nicorandil (NCD) is a chemically unstable drug and sensitive to humidity, heat, and mechanical stress in manufacturing processes. In this work, the cocrystals of NCD with organic acids were designed and synthesized to enhance the stability of NCD. Cocrystals of NCD with 1-hydroxy-2-naphthoic acid, salicylic acid, 3-hydroxybenzoic acid, and 2,5-dihydroxybenzoic acid were obtained. Hydrothermal stability study showed that cocrystals performed with remarkable stability advantages compared with pure NCD. On the basis of mechanism research, the stability improvements of NCD molecules can be attributed to the realignments of NCD molecules in cocrystals. After the formation of cocrystals, the novel packing styles of NCD break the self-catalyzed decomposition process in pure NCD structure. Moreover, intrinsic dissolution rate characterizations showed that the formation of cocrystals could also optimize the dissolution behavior of NCD to realize the objective of sustained release.

中文翻译：

尼古兰地药物共晶体具有增强的化学稳定性和缓释性

Nicorandil（NCD）是一种化学不稳定药物，在生产过程中对湿度，热和机械应力敏感。在这项工作中，设计并合成了NCD与有机酸的共晶体以增强NCD的稳定性。获得了NCD与1-羟基-2-萘甲酸，水杨酸，3-羟基苯甲酸和2，5-二羟基苯甲酸的共晶体。水热稳定性研究表明，与纯NCD相比，共晶具有显着的稳定性优势。在机理研究的基础上，NCD分子稳定性的提高可归因于NCD分子在共晶中的重新排列。共晶形成后，NCD的新型堆积方式打破了纯NCD结构中的自催化分解过程。此外，

更新日期：2020-10-07

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