β-环糊精包合物的制备及对苯佐卡因水解速度的影响

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英文篇名：Preparation of β-cyclodextrin inclusion complexes and its effect on the benzocaine hydrolysis 作者：焦姣 ; 王高峰 ; 张稳婵 ; 鱼银虎 ; 任琰晨 ; 王鑫 英文作者：JIAO Jiao;WANG Gaofeng;ZHANG Wenchan;YU Yinhu;REN Yanchen;WANG Xin;Department of Applied Chemistry,Yuncheng University; 关键词：β-环糊精 ; 苯佐卡因 ; 包合物 ; 水解速度 英文关键词：β-cyclodextrin;;benzocaine;;inclusion complex;;hydrolysis rate 中文刊名：NATR 英文刊名：Journal of Guizhou Normal University(Natural Sciences) 机构：运城学院应用化学系; 出版日期：2019-01-12 13:54 出版单位：贵州师范大学学报(自然科学版) 年：2019 期：v.37;No.143 基金：国家自然科学青年基金(No.51808485);; 运城学院院级科研项目(No.CY-2017013) 语种：中文; 页：NATR201901006 页数：7 CN：01 ISSN：52-5006/N 分类号：34-40

摘要

通过优化β-环糊精-苯佐卡因包合物(β-CD-benzocaine,β-CD-ben)的制备条件,研究其对苯佐卡因水解速度的影响。具体以β-环糊精、苯佐卡因为原料,水溶液搅拌法为制备方法,在不同投料比(苯佐卡因:β-CD分别为1∶0. 5、1∶1、1∶2和1∶3)、搅拌时间(3 h、5 h和8 h)、包合温度(40℃、55℃和80℃)、干燥后产物洗涤剂(甲醇、乙醇和异丙醇)的条件下,优化包合物的最佳制备条件,即投料比,苯佐卡因∶β-CD=1∶1,搅拌时间5 h,包合温度55℃,干燥后产物洗涤剂选择异丙醇。通过形态表观、电镜分析及X-射线衍射分析对包合物进行表征,并考察5×10﹣6g/mL的苯佐卡因溶液和β-CD-ben包合物溶液在碱性条件下的水解速度。结果表明:优化条件下制备的β-CD-ben包合物在一定程度上降低了苯佐卡因的水解程度。该研究结果对β-CD-ben包合物制备中的影响因素进行了补充,为增加不稳定药物稳定性提供了一定借鉴。
        To study the effect on the hydrolysis of benzocaine,the preparation conditions of β-cyclodextrin-benzocaine inclusion complexes( β-CD-benzocaine,β-CD-ben) were optimized,including β-cyclodextrin and benzene,through water solution mixing method to prepare β-CD-ben with the different weight ratio( benzocaine∶ β-CD = 1∶ 0. 5,1∶ 1,1∶ 2 and 1∶ 3),stirring time( 3 h,5 h and 8 h),inclusion temperature( 40 ℃,55 ℃ and 80 ℃),dried product detergent( methanol,ethanol,isopropanol) conditions. Its purpose was to get the best preparation method of inclusion complexes. The optimal conditions for the preparation of β-cyclodextrin-benzocaine inclusion complexes were as follows:the ratio of benzocaine to benzocaine for 1∶ 1,the stirring time for 5 h and the inclusion temperature for 55 ℃,together with isopropanol as for the dried product detergent. Appetence characteristics,scan electron microscopy( SEM) and X-ray diffraction( XRD) analysis were used for characterization. The hydrolysis rate of 5 × 10~(-6) g/m L benzocaine solution and inclusion complexes were compared under alkaline conditions. Hydrolysis rate results showed that β-CD-ben was reduced in a certain extent. The effects of the study on the preparation of β-CD-ben were complemented,which could provide some references for the stability of unstable drug.

引文

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