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本文调研了与吉非替尼晶型有关的大量文献,从晶型种类、晶型制备、晶型表征以及晶型讨论4个方面进行了综述。吉非替尼现已发现有8种晶型,各种晶型物质可通过直接或间接的制备方式来获得,已应用于对这些晶型进行分析表征的技术有单晶X射线衍射分析、粉末X射线衍射分析、差示扫描量热分析、热重分析、红外光谱分析、熔点分析等分析方法。通过对表征结果的比较总结,对吉非替尼多晶型形成原因进行了分析,并在已有研究基础上探讨了选择Form 1成为药用晶型的原因。本文对部分实验结果提出了质疑,指出了现有文献对于吉非替尼多晶型的的研究缺乏系统性,现有研究数据并不完整,特别是缺乏关于吉非替尼各晶型的溶解度、生物学等关键数据。因此,对吉非替尼的多晶型研究还需要更系统更深入。
In this paper, a large number of literature related to the gefitinib polymorphism were investigated. Four types of crystal types, crystal preparation, crystal characterization and crystal form were reviewed. Gefitinib has now been found in eight kinds of crystal form, a variety of crystalline material can be obtained by direct or indirect preparation, has been applied to the analysis of these crystalline forms of characterization of single crystal X-ray diffraction analysis, powder X-ray diffraction analysis, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy, melting point analysis and other analytical methods. Based on the comparative summary of the characterization results, the reasons for the formation of gefitinib polymorphism were analyzed. Based on the previous studies, the reason for selecting Form 1 as the medicinal crystal form was discussed. In this paper, some experimental results were questioned, pointing out that the existing literature on the lack of systematic research on the gefitinib polymorphism, the existing data is not complete, in particular, the lack of solubility of gefitinib polymorphs , Biology and other key data. Therefore, the study of polymorphism of gefitinib needs to be more systematic and in-depth.