| 引用本文: | 严小红,李春盈,卢俊钢,江英桥,霍秀敏,邵颖.氟康唑的多晶型及转化研究[J].中国现代应用药学,2012,29(8):712-717. |
| YAN Xiaohong,LI Chunying,LU Jungang,JIANG Yingqiao,HUO Xiumin,SHAO Yin.Study on the Polymorphism and Transformation of Fluconazole[J].Chin J Mod Appl Pharm(中国现代应用药学),2012,29(8):712-717. |
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| 摘要: |
| 目的 对氟康唑的多晶型及其相互转化进行分析研究。方法 采用红外光谱仪(IR)、近红外光谱仪(NIR)、拉曼光谱仪(RM)、X-射线粉末衍射仪(XRD)、差示扫描量热仪(DSC)和热重分析仪(TGA)对氟康唑的晶型进行了研究，并考察了温度、湿度、溶剂和研磨对其晶型转化的影响。结果 X-射线粉末衍射法作为晶型判定方法，10个厂家18批氟康唑的晶型有Ⅱ型、Ⅲ型和一水合物晶型；在不同的温度、湿度和结晶溶剂中Ⅱ型和一水合物晶型可相互转化，在氯仿中结晶和高温熔融可得到I型结晶。结论 氟康唑不同晶型谱学特征显著，可对氟康唑晶型进行质量控制，各晶型间可以相互转化并确定了转化条件。 |
| 关键词: 氟康唑 多晶型 晶型转化 |
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| 基金项目:国家科技攻关课题(2004BA720A34) |
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| Study on the Polymorphism and Transformation of Fluconazole |
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YAN Xiaohong1, LI Chunying1, LU Jungang1, JIANG Yingqiao1, HUO Xiumin2, SHAO Yin2
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1.Guangzhou Institute for Drug Control, Guangzhou 510160, China;2.Center for Drug Evaluation, SFDA, Beijing 100038, China
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| Abstract: |
| OBJECTIVE To investigate the polymorphism and transformation of fluconazole. METHODS The polymorphism of fluconazole was analyzed by IR, NIR, Raman, XRD and TGA. The influences of temperature, humidity, solvent and grind on crystal transformation were explored. RESULTS Crystal form of 18 batch of samples from 10 manufacturers were defined as form Ⅱ, form Ⅲ and monohydrate by XRD. Form Ⅱ and monohydrate were interconvertible in different temperatures, humidities and solvents. Form I of fluconazole was obtained by recrystallizing in chloroform and melting in high temperature. CONCLUSION Crystal forms of fluconazole can be controlled since their characteristics are significantly different. Form I, form Ⅱ and monohydrate are interconvertible and the transformation condition is established. |
| Key words: fluconazole polymorphism transformation |
