2-甲氧基雌二醇氯仿溶剂化物脱溶剂动力学研究  

Research of desolvent kinetics of 2-methoxyestradiol chloroform solvate

作　　者：李雯[1,2] 张瑞云 丁远民 杨慧君 张梦改 LI Wen;ZHANG Ruiyun;DING Yuanmin;YANG Huijun;ZHANG Menggai(School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001,China;Key Laboratory of Technology of Drug Preparation(Zhengzhou University),Ministry of Education,Collaborative Innovation Center of New Drug Research and Safety Evaluation&Key Laboratory of Henan Province for Drug Quality and Evaluation,Zhengzhou 450001,China;School of Chemical Engineering,Zhengzhou University,Zhengzhou 450001,China)

机构地区：[1]郑州大学药学院,河南郑州450001 [2]药物关键制备技术教育部重点实验室,新药创制与药物安全性评价河南省协同创新中心,河南省药品质量控制与评价重点实验室,河南郑州450001 [3]郑州大学化工学院,河南郑州450001

出　　处：《南阳师范学院学报》2020年第4期29-32,共4页Journal of Nanyang Normal University

基　　金：河南省科技厅产学研资助项目(No.152107000043);郑州大学大学生创新创业训练计划资助项目(2019)。

摘　　要：在2-甲氧基雌二醇氯仿溶剂化物(2-ME.2CHCl3)制备和单晶X-射线衍射法进行结构确证的基础上,采用等温脱溶剂法和非等温脱溶剂法,进行2-ME.2CHCl3脱溶剂动力学规律研究.2-ME.2CHCl3等温脱溶剂过程的脱溶剂机理最适模型为R3,即几何边界层模型;其非等温脱溶剂过程的脱溶剂机理,在升温速率为5 K/min以下时,最适合模型为R3,在升温速率为10 K/min^20 K/min时,最适合模型为R2,属于相界面反应机理,控制步骤是相界面的推进.2-ME为进入临床研究的具有抗肿瘤作用的药物,其溶剂化物脱溶剂动力学研究,可以为其制剂研究提供重要的依据.The desolvation kinetics of 2-ME.2CHCl3 was studied by isothermal desolvation method and non isothermal desolvation method based on the preparation of 2-ME.2CHCl3 and the structural identification by single crystal X-ray diffraction.For the isothermal desolvent process of 2-ME.2CHCl3,the best desolvent mechanism model is R3,i.e.geometric boundary layer model.For the nonisothermal desolvent process of 2-ME.2CHCl3,when the heating rate is below 5K/min,the most suitable model is R3,and when the heating rate is 10 K/min^20 k/min,the most suitable model is R2.R2 model belongs to the phase interface reaction mechanism which control step is the promotion of phase interface.2-ME is an anti-tumor drug entered clinical studies,the study on the desolvent kinetics of its solvate can provide an important basis for its pharmaceutical preparation.

关 键 词：2-甲氧基雌二醇 氯仿溶剂化物 脱溶剂 动力学 

分 类 号：R917[医药卫生—药物分析学]