利福平-中国现代应用药学.PDF

·药 剂 · 利福平-羟丙基-β-环糊精包合物的制备和评价 王娜 1,3 ，谭群友 2 ，刘娟 1,3 ，赵春景 3 ，张景勍 1*(1.重庆医科大学药学院药物高校工程研究中心、生物化学与分子药理学重点实 验室，重庆 400016 ；2.第三军医大学大坪医院野战外科研究所，重庆 400042 ；3.重庆医科大学附属第二医院药剂科，重庆 400010) 摘要：目的 制备并评价利福平-羟丙基-β-环糊精包合物。方法 采用研磨法制备利福平-羟丙基-β-环糊精包合物，以差 示扫描量热法、红外分光光度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 利福平能够与羟丙基-β-环糊精形成物质的 量比为 1 ∶1 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 0.125 µg·mL1 和 32.0 µg·mL1。结论 羟丙基-β-环糊精可以包合利福平并改善其溶解性能。包合物对革兰氏阳性菌和阴 性菌均有明显的抑制作用。 关键词：利福平；羟丙基-β-环糊精；包合物；制备；评价 中图分类号：R943.31 文献标志码：B 文章编号：1007-7693(2010)02-0128-05 Preparation and Evaluation of Rifampicin Hydroxypropyl-β-Cyclodextrin Inclusion Compound WANG Na1,3 2 1,3 3 1* , TAN Qunyou , LIU Juan , ZHAO ChunJing , ZHANG Jingqing (1. Medicine Engineering Research Center in University, Chongqing Key Laboratory of Biochemical Molecular Pharmacology, School of Pharmacy, Chongqing Medical University, Chongqing 400016, China; 2. Daping Hospital Research Institute of Surgery, Third Military Medical University, Chongqing 400042, China; 3. Department of Pharmacy, Second Affiliated Hospital, Chongqing Medical University, Chongqing 400010, China) ABSTRACT: OBJECTIVE To prepare and evaluate rifampicin hydroxypropyl-β-cyclodextrin(HP-β-CD) inclusion compound. METHODS The inclusion complex was prepared by grinding method and confirmed by the change of differential scanning calorimetry and the infrared absorption spectra. 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 were observed by broth dilution