[1]李雯,李莎莎,常英杰,等.盐酸丁卡因多晶型制备和溶解度测定与关联[J].郑州大学学报(工学版),2020,41(06):92-96.[doi:10.13705/j.issn.1671-6833.2020.06.008]
 Li Shasha,Chang Yingjie,Zhao Jie,et al.Preparation of Polymorphism of Tetracaine Hydrochloride and Measurement and Correlation of the Solubility[J].Journal of Zhengzhou University (Engineering Science),2020,41(06):92-96.[doi:10.13705/j.issn.1671-6833.2020.06.008]
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盐酸丁卡因多晶型制备和溶解度测定与关联()
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《郑州大学学报(工学版)》[ISSN:1671-6833/CN:41-1339/T]

卷:
41卷
期数:
2020年06期
页码:
92-96
栏目:
出版日期:
2020-12-31

文章信息/Info

Title:
Preparation of Polymorphism of Tetracaine Hydrochloride and Measurement and Correlation of the Solubility
作者:
李雯李莎莎常英杰赵洁丁远民李瑞鹏
郑州大学化工学院,河南郑州450001, 郑州大学药学院,河南郑州450001, 郑州大学药学院,河南郑州450001, 药物关键制备技术教育部重点实验室,河南郑州450001, 新药创制与药物安全性评价河南省协同创新中心,河南郑州450001, 河南省药品质量控制与评价重点实验室,河南郑州450001

Author(s):
School of Chemical Technology, Zhengzhou University, 450001, Zhengzhou, Henan, School of Pharmacy, Zhengzhou University, Zhengzhou 450001 Henan, School of Pharmacy, Zhengzhou University, 450001, Zhengzhou, Henan, Key Laboratory of the Ministry of Education, Pharmaceutical Key Preparation Technology, Henan Zhengzhou 450001, new drug creation and drug safety evaluation Henan Province Henan Province Collaborative Innovation Center, Henan Zhengzhou 450001, Henan Provincial Pharmaceutical Quality Control and Evaluation Key Laboratory, Henan Zhengzhou 450001

关键词:
Keywords:
DOI:
10.13705/j.issn.1671-6833.2020.06.008
文献标志码:
A
摘要:
盐酸丁卡因具有多晶型现象,可以晶型A或晶型B室温长期保存,研究发现,晶型A和晶型B在有机溶剂中易发生溶剂介导转晶型现象,转化为两种晶型的混合物,进一步研究发现,盐酸丁卡因原料药市售品均为晶型A和晶型B的混合物,晶型定量研究发现晶型A:晶型B=4:1.采用平衡法测定了商品化盐酸丁卡因原料药在纯溶剂及混合溶剂中的溶解度.溶解度数据表明,溶解度随温度的升高而增大.在甲醇-乙酸乙酯混合溶剂中的溶解度随着甲醇摩尔分数先增加后降低,当甲醇摩尔分数为0.8492,溶解度达到最大值.应用适合的模型对溶解度数据进行拟合,拟合结果与实验数据基本吻合.利用van?t Hoff 方程估算得到盐酸丁卡因在溶解过程中的溶解熵和溶解焓,说明其溶解过程是吸热和熵驱动的.
Abstract:
Tetracaine hydrochloride has a polymorphic phenomenon and can be stored at room temperature for a long time in Form A or Form B. It was found that Form A and Form B are prone to solvent-mediated crystal transformation in the organic solvent s, and are converted into a mixture of two crystal forms. Further studies showed that the commercial products of tetracaine hydrochloride were all mixtures of crystalline A and B with a ratio of 1:4. The solubility of commercial tetracaine hydrochloride was investigated in pure solvents and mixed solvents using the balance method . The solubility data showed that the solubility of tetracaine hydrochloride increased with the increase of temperature. The solubility of tetracaine hydrochloride can firstly increase and then decrease with the molar fraction of methanol in methanol-ethyl acetate mixed solvents. When the molar fraction of methanol was 0.8492, the solubility of tetracaine hydrochloride in the mixed solvent reached the maximum. The solubility data of tetracaine hydrochloride were fitted by suitable equation model, and the fitted results were in good agreement with the experimental data. The enthalpy and entropy of dissolution of tetracaine hydrochloride were estimated based on regression of the solubility data by using the van?t Hoff equation, and the dissolving process was endothermic and entropy-driving.
更新日期/Last Update: 2021-02-10