沙拉沙星/β-环糊精包合物的制备表征和细胞毒性研究  

Preparation,characterization and cytotoxicity of sarafloxacin with β-cyclodextrin inclusion complex

作　　者：姜兴粲 李冰 张继瑜[1,2,3] JIANG Xingcan;LI Bing;ZHANG Jiyu(Key Laboratory of Veterinary Pharmaceutical Development,Ministry of Agriculture and Rural Affairs,Lanzhou 730050,China;Key Laboratory of New Animal Drug Project of Gansu Province,Lanzhou 730050,China;Lanzhou Institute of Husbandry and Pharmaceutical Sciences,Chinese Academy of Agricultural Sciences(CAAS),Lanzhou 730050,China)

机构地区：[1]农业农村部兽用药物创制重点实验室,兰州730050 [2]甘肃省新兽药工程重点实验室,兰州730050 [3]中国农业科学院兰州畜牧与兽药研究所,兰州730050

出　　处：《黑龙江畜牧兽医》2020年第24期129-133,177,共6页Heilongjiang Animal Science And veterinary Medicine

基　　金：“十二五”国家科技支撑计划项目(2015BAD1101);国家现代农业产业技术体系专项(CAR-37)。

摘　　要：为了制备沙拉沙星(SAR)/β-环糊精(β-CD)包合物并对其进行结构表征和细胞毒性评价,试验对SAR/β-CD包合物的制备参数进行筛选,采用差示扫描量和热重法对SAR/β-CD包合物进行表征,采用液相色谱法对制得的SAR/β-CD包合物制剂进行相对含量及有关物质检测,采用CCK8法进行细胞毒性研究。结果表明:筛选试验得到包合物的制备工艺为搅拌温度50℃,搅拌时间4 h,SAR与β-CD的摩尔比1∶2。SAR/β-CD包合物与其物理混合物不同,具有更加稳定的热力学性质,证明成功制得SAR/β-CD包合物。体外大鼠正常肝细胞(BRL)毒性试验结果表明,SAR/β-CD包合物的毒性明显低于原料药。说明本研究优化的SAR/β-CD包合物的制备工艺稳定可行,药物性质明显提高。In order to prepare the sarafloxacin(SAR)withβ-cyclodextrin(β-CD)inclusion complex and to evaluate its structure and cytotoxicity,the preparation parameters of SAR/β-CD inclusion complex were screened.The inclusion complex of SAR/β-CD was characterized by differential scanning calorimetry and thermogravimetry,and the relative content and related substances of the SAR/β-CD inclusion complex were determined by liquid chromatography.Finally,the cytotoxicity was studied by CCK8 method.The results showed that the preparation process of the inclusion complex obtained by screening test was stirring temperature 50℃,stirring time 4 h,and the molar ratio of SAR toβ-CD was 1∶2.SAR/β-CD inclusion complex was different from the physical mixture and had more stable thermodynamic properties.It was proved that SAR/β-CD inclusion complex had been successfully prepared.The results of cytotoxicity test of normal rat hepatocytes(BRL)in vitro showed that the toxicity of the inclusion complex was significantly lower than that of the raw material drug.It indicated that the process optimized of SAR/β-CD indusion complex was stable and feasible,and the drug properties were obviously improved.

关 键 词：沙拉沙星 Β-环糊精 制备 表征 含量 细胞毒性 

分 类 号：S859.53[农业科学—临床兽医学] S859.796[农业科学—兽医学]