[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
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):
LI Shasha1;  CHANG Yingjie2;  ZHAO Jie1;  DING Yuanmin1;  LI Ruipeng2;  LI Wen2; 3; 4; 5
1.School of Chemical Engineering, Zhengzhou University, Zhengzhou 450001, China; 2.School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China; 3.Henan Province Key Laboratory of Technology of Drug Preparation, Zhengzhou 450001, China; 4.Collaborative Innovation Center of New Drug Research, Zhengzhou 450001, China; 5.Safety Evaluation and Ministry of Education Key Laboratory of Henan Province for Drug Quality and Evaluation, Zhengzhou 450001, China
关键词:
Keywords:
tetracaine hydrochloride;  polymorphism;  solubility;  measurement;  correlation
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 polymorphic phenomena. The measurement of the solubility of crystalline drugs was a hot topic in the field of drug quality control. The solubility of commercial tetracaine hydrochloride was reported in the literature. The solubility of tetracaine hydrochloride was determined and correlated. On the basis of qualitative and quantitative analysis of polymorphic phenomena of tetracaine hydrochloride, balance method was selected to determin the solubility of commercial tetracaine hydrochloride in pure and mixed solvents. The results showed that tetracaine hydrochloride had the latent dissolution phenomenon in methanol-ethyl acetate mixed solvents. When the molar fraction of methanol was 0.849 2, the solubility reached the maximum. In pure solvents, the solubility datas of tetracaine hydrochloride coincided with the Apelblat equation. While in mixed solvents, the solubility datas of tetracaine hydrochloride coincided with the CNIBS/R-K equation.The correlation coefficients R2 between fitting results and experimental data was greater than 0.99. The dissolution entropy and enthalpy of tetracaine hydrochloride in the dissolution process were calculated by the van′t Hoff equation, which proved that the dissolution process of tetracaine hydrochloride was endothermic and entropy-driving.

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更新日期/Last Update: 2021-02-10