【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0.125μg.mL-1和32.0μg.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。更多还原

【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 test.RESULTS The inclusion complexes consisted of HP-β-CD and rifampicin at a molar ratio of 1∶1.The minimum inhibitory concentrations were 0.125 μg.mL?1 and 32.0 μg.mL?1.CONCLUSION The solubility of rifampicin was increased.The growth of staphylococcus and Escherichia coli could be inhibited by rifampicin HP-β-CD.更多还原