期刊论文详细信息
JOURNAL OF CHEMICAL ENGINEERING OF JAPAN
Solid-State Characterization of E3210 Polymorphs
Hiroshi Takiyama2  Hiroshi Ishihara4  Yoshiaki Sato1  Takao Omae3  Takuma Minamisono3  Takashi Hasebe3 
[1] Biomarkers & Personalized Medicine, Eisai Co., Ltd.;Department of Chemical Engineering, Tokyo University of Agriculture and Technology;Physical Chemistry, Analytical Research, CMC Japan, Eisai Pharmaceutical Science & Technology, Tsukuba Research Laboratories., Eisai Co., Ltd.;DDS Research, Global Formulation-Japan, Eisai Pharmaceutical Science & Technology, Tsukuba Research Laboratories., Eisai Co., Ltd.
关键词: Polymorph Selection;    Thermal Analysis;    Thermodynamic Stability;    Transition Temperature;    Polymorphism;   
DOI  :  10.1252/jcej.11we191
来源: Maruzen Company Ltd
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【 摘 要 】

References(13)Polymorphism is an interesting property of crystalline substances and is of importance in pharmaceutical development. Studies were conducted to identify the most stable of the five polymorphic (one hydrate and four anhydrous) forms of the active pharmaceutical ingredient (API) E3210. Between the different polymorphs, the transformation mechanisms and thermodynamic stability relationships were complex. Forms A and B were further characterized by differential scanning calorimetry (DSC) at various heating rates and by powder X-ray diffractometry (PXRD; isothermal and temperature-controlled). Analysis by DSC revealed that Form A displayed a single and large endothermic melting peak. Form B displayed two small peaks, one endothermic peak and the other exothermic; the endothermic peak was an enantiotropically related reversible transformation from Form B to Form B′, and the exothermic peak was a monotropically related thermodynamically irreversible transformation from Form B′ to Form A. Thus, Forms B and B′ were enantiotropically related polymorphs, and both were monotropically related to Form A. Form A was the most stable polymorphic form and Form B was metastable.

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