Identification and physicochemical characterization of caffeine-citric acid co-crystal polymorphs

被引：26

作者：

Mukaida, Makoto ^{[1
,2
]}

Watanabe, Yuka ^{[1
]}

Sugano, Kiyohiko ^{[1
]}

Terada, Katsuhide ^{[1
]}

机构：

[1] Toho Univ, Fac Pharmaceut Sci, Dept Pharmaceut, Funabashi, Chiba 2748510, Japan

[2] AsahiKASEI Pharma Corp, Izunokuni, Shizuoka 4102321, Japan

来源：

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2015年 / 79卷

关键词：

Caffeine; Citric acid; Co-crystal; Polymorph; Raman; IR; Humidity; PHARMACEUTICAL PHASES; COCRYSTAL; SOLUBILITY; IMPROVE; COMPOUND; DRUG;

D O I：

10.1016/j.ejps.2015.09.002

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The purpose of the present study was to identify a new caffeine-citric acid co-crystal (CA-CI) polymorph and characterize three CA-CI polymorphs. The stability order among the three CA-CI polymorphs was also determined. One new and two known CA-CI polymorphs were prepared by the liquid-assisted grinding method or the slurry methods. The three CA-CIs were then identified and characterized by powder X-ray diffraction (PXRD), thermal analysis, IR spectroscopy, Raman spectroscopy, and dynamic vapor sorption (DVS). The stability order of the CA-CIs was determined by the slurry conversion method. Each CA-CI showed distinct PXRD, IR, Raman, and DVS data. The melting points of CA-CIs were 131 degrees C (a new form, Form III), 141 degrees C (Form I), and 160 degrees C (Form II). The order of thermodynamic stability was CA-CI Form II > CA-CI Form I > CA-CI Form III. CA-CI Forms I and II were relatively stable against humidity compared to CA, CI and CA-CI Form III. (C) 2015 Elsevier B.V. All rights reserved.

引用

页码：61 / 66

页数：6

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