β-环糊精对利福平的包合作用  

Study on inclusion process of rifampicin β-cyclodextrin inclusion complex

作　　者：刘娟[1,2] 谭群友[3] 鲁卫平[3] 赖超[1] 赵春景[2] 张景勍[1] 

机构地区：[1]重庆医科大学药学院药物高校工程研究中心,重庆400016 [2]重庆医科大学附属第二医院药剂科,重庆400010 [3]第三军医大学大坪医院野战外科研究所,重庆400042

出　　处：《中国医院药学杂志》2010年第1期40-42,共3页Chinese Journal of Hospital Pharmacy

基　　金：重庆市科委自然科学基金资助项目(编号:CSTC,2007B135456);2009年重庆市首批高等学校优秀人才资助计划项目

摘　　要：目的:研究β-环糊精对利福平的包合作用。方法:采用研磨法制备利福平β-环糊精包合物,以差示扫描量热法对包合物进行鉴定,采用紫外分光光度法、相溶解度法验证利福平β-环糊精包合物的形成。体外肉汤稀释试验测定包合物对金葡菌和大肠埃希菌的抑制作用。结果:利福平能够与β-环糊精形成物质的量比为1∶2的包合物,包合物改善了药物的溶解性能。包合物对金葡菌和大肠埃希菌的最低抑菌浓度分别为:0.125mg.L-1和32.0g.L-1。结论:β-环糊精可以包合利福平并改善其溶解性能。包合物对革兰阳性菌和阴性菌均有明显的抑制作用。OBJECTIVE To investigate the inclusion process of rifampicin β-cyclodextrin （β-CD）. METHODS The inclusion complex was prepared by grinding method and confirmed by the change of differential scanning calorimetry. The ultraviolet spectrophotometry and phase solubility methods were used for validating the formation of β cyclodextrin inclusion complexes of rifampicin. The inhibitory effects of inclusion complexes on Staphylococcus and Escherichia Coli by broth dilution test. RESULTS The inclusion complexes consisted of β-CD and rifampicin at a molar ratio of 1 ： 2. The solubility of rifampicin was increased. The minimal inhibitory concentration of inclusion complexes on Staphylococcus and Escherichia Coli were lower than 0. 125 mg·L^-1 and 32. 0 mg·L^-1 , respectively. CONCLUSION Rifampicin β-CD could be formed and the solubility of rifampicin could be improved. The growth of Staphylococcus and Escherichia Coli could be inhibited by rifampicin β-cyclodextrin.

关 键 词：利福平 Β-环糊精 包合物 

分 类 号：R943[医药卫生—药剂学]