Two Cocrystal Polymorphs of Palmatine Chloride with Racemic Hesperetin

被引:17
|
作者
Zhang, Yanjie [1 ]
Li, Yanguang [1 ,2 ]
Liu, Lei [1 ,2 ]
Guo, Quanhu [1 ]
Sa, Rongjian [1 ]
Zhang, Mei [1 ]
Lou, Benyong [1 ,2 ,3 ]
机构
[1] Minjiang Univ, Res & Testing Ctr Pharmaceut, Coll Mat & Chem Engn, Fuzhou 350108, Fujian, Peoples R China
[2] Fuzhou Univ, Coll Mat Sci & Engn, Fuzhou 350108, Fujian, Peoples R China
[3] Chinese Acad Sci, Fujian Inst Res Struct Matter, State Key Lab Struct Chem, Fuzhou 350002, Fujian, Peoples R China
关键词
PHARMACEUTICAL COCRYSTALS; CRYSTAL-STRUCTURES; SOLUBILITY; STABILITY; RELEASE;
D O I
10.1021/acs.cgd.1c01016
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Two polymorphic cocrystals of palmatine chloride with racemic hesperetin (Form I and Form II) have been prepared and investigated systematically. Crystal structure analysis reveals that reliable O-H center dot center dot center dot Cl- hydrogen-bonding interactions exist in both cocrystal polymorphs. However, similar O-H center dot center dot center dot Cl- hydrogen-bonding interactions resulted in completely different supramolecular arrangements. Cocrystal Forms I and II are non-hygroscopic and show high stability against temperature, humidity, and light. The cocrystal formation greatly lowers the solubility of palmatine chloride, while the solubility of hesperetin has been improved. Sustained release of palmatine chloride and enhanced release of hesperetin from two cocrystal polymorphs in pure water were achieved.
引用
收藏
页码:1073 / 1082
页数:10
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