Solubility Behavior and Polymorphism of l-Arginine l-Pyroglutamate in Nine Pure Solvents and a Binary Water + Ethanol System

Author(s):  
Shen Hu ◽  
Jiaming Han ◽  
Haoyou Liu ◽  
Jingxuan Qiu ◽  
Yue Zhao ◽  
...  
Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 298
Author(s):  
Yefen Zhu ◽  
Yanlei Kang ◽  
Ling Zhu ◽  
Kaxi Yu ◽  
Shuai Chen ◽  
...  

Canagliflozin (CG) was a highly effective, selective and reversible inhibitor of sodium-dependent glucose co-transporter 2 developed for the treatment of type 2 diabetes mellitus. The crystal structure of CG monohydrate (CG-H2O) was reported for the first time while CG hemihydrate (CG-Hemi) had been reported in our previous research. Solubility and dissolution rate results showed that the solubility of CG-Hemi was 1.4 times higher than that of CG-H2O in water and hydrochloric acid solution, and the dissolution rates of CG-Hemi were more than 3 folds than CG-H2O in both solutions. Hirshfeld surface analysis showed that CG-H2O had stronger intermolecular forces than CG-Hemi, and water molecules in CG-H2O participated three hydrogen bonds, forming hydrogen bond networks. These crystal structure features might make it more difficult for solvent molecules to dissolve CG-H2O than CG-Hemi. All these analyses might explain why the dissolution performance of CG-Hemi was better than CG-H2O. This work provided an approach to predict the dissolution performance of the drug based on its crystal structure.


1993 ◽  
Vol 22 (7) ◽  
pp. 601-623 ◽  
Author(s):  
S. E. Ziemniak ◽  
M. E. Jones ◽  
K. E. S. Combs

Author(s):  
Xiaoyang Liu ◽  
Kathryn E. O’Harra ◽  
Jason E. Bara ◽  
C. Heath Turner

2013 ◽  
Vol 15 (7) ◽  
Author(s):  
Haibo Wang ◽  
Quan Jin ◽  
Lufeng Yang ◽  
Yingliang Liu
Keyword(s):  

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