Novel Glutaric Acid Cocrystal Formation via Cogrinding and Solution Crystallization

被引:21
作者
Bian, Lin [1 ]
Zhao, Haiping [1 ]
Hao, Hongxun [1 ]
Yin, Qiuxiang [1 ]
Wu, Songgu [1 ]
Gong, Junbo [1 ,2 ]
Dong, Weibing [3 ]
机构
[1] Tianjin Univ, Sch Chem Engn & Technol, State Key Lab Chem Engn, Tianjin 300072, Peoples R China
[2] Tianjin Univ, Tianjin Key Lab Modern Drug Delivery & High Effic, Tianjin 300072, Peoples R China
[3] Tianjin Univ, Sch Sci, Dept Chem, Tianjin 300072, Peoples R China
基金
中国国家自然科学基金;
关键词
Cocrystal screening; Crystallization; Mechanochemical method; Process analytical technology; ANALYTICAL TECHNOLOGY PAT; CO-CRYSTAL; SUPERSATURATION; SOLUBILITY; PIRACETAM; IMPROVE;
D O I
10.1002/ceat.201200720
中图分类号
TQ [化学工业];
学科分类号
0817 ;
摘要
An efficient and reliable approach to discover new pharmaceutical cocrystals in the early development stage is proposed and used to develop cocrystals of piracetam with some aliphatic diacids. A 1: 1 cocrystal of piracetam and glutaric acid was screened by a mechanochemical method and identified by powder X-ray diffraction and differential scanning calorimetry. Followed by solution crystallization, this cocrystal was reproduced. To better understand the mechanism of cocrystal formation in solution crystallization, process analytical technologies including focused beam reflectance measurement, attenuated total reflectance-Fourier transform infrared, and particle vision measurement were applied to investigate the cocrystallization process of piracetam with glutaric acid. The mechanism of cocrystal formation during solution-mediated phase transformation is discussed in detail.
引用
收藏
页码:1292 / 1299
页数:8
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