四嗪二甲酰胺环糊精包合物制备研究  

Study on the Preparation of ZGDHu-1 Cyclodextrin Inclusion Complex

作　　者：章紫梦 刘永丽[1] 蒋旻昀[1] 甘镇旗 毛颖 钟文君 Zhang Zimeng;Liu Yongli;Jiang Minyun;Gan Zhenqi;Mao Ying;Zhong Wenjun(New Dosage form and Pharmacology Research Institute,Taizhou Vocational&Technical College,Taizhou 318000,China)

机构地区：[1]台州职业技术学院药物新剂型及药理研究所,浙江台州318000

出　　处：《山东化工》2024年第10期21-23,26,共4页Shandong Chemical Industry

基　　金：浙江省大学生科技创新活动计划项目(2021R481005);浙江省高校国内访问工程师校企合作项目(FG2022255)。

摘　　要：目的:制备四嗪二甲酰胺(ZGDHu-1)环糊精包合物,对其质量进行表征。方法:采用饱和水溶液法制备四嗪二甲酰胺的甲基-β-环糊精包合物体系,通过高效液相色谱法检测药物含量,通过扫描电镜、差示扫描量热分析、包合率和溶出度对包合物质量进行考察。结果:四嗪二甲酰胺含量检测在1.078~107.9μg·mL^(-1)范围内线性关系良好,扫描电镜观察和差示扫描量热分析表明四嗪二甲酰胺以无定型状态被包埋在辅料空腔内,包合物中四嗪二甲酰胺的平均包合率为87.19%,包合物体系显著提高了四嗪二甲酰胺的溶出度,80 min累积溶出度为82.60%。结论:四嗪二甲酰胺环糊精包合物制备方法简便,包合率高,对体外溶出具有良好的改善效果。Objective:The cyclodextrin inclusion complex of ZGDHu-1 was prepared and its physicochemical property was studied.Methods:The methyl-β-cyclodextrin inclusion complex of ZGDHu-1 was prepared by the saturated aqueous solution method,and the drug content was determined by High-performance liquid chromatography method,the property of inclusion complex was investigated by the scanning electron microscopy(SEM),the differential scanning calorimetry(DSC),the inclusion rate and the released rate in vitro.Results:The linear relationship of ZGDHu-1 content analysis method was good in the range of 1.078~107.9μg·mL^(-1).The results of SEM and DSC showed that ZGDHu-1 was entrapped in the cavity of excipients in an amorphous state,the average inclusion rate of ZGDHu-1 in the inclusion complex was 87.19%.The released rate in vitro of ZGDHu-1 in the inclusion complex was significantly increased,and the cumulative released rate in vitro in 80 min was 82.60%.Conclusion:The preparation process of ZGDHu-1 cyclodextrin inclusion complex was simple,and the inclusion complex has good inclusion rate.Drug released behavior in vitro of the inclusion comples was better.

关 键 词：四嗪二甲酰胺 甲基-β-环糊精 饱和水溶液法 包合物 包合率 溶出度 

分 类 号：TQ460[化学工程—制药化工] R944[医药卫生—药剂学]