论文部分内容阅读
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。
Objective To prepare and evaluate rifampicin-hydroxypropyl-β-cyclodextrin inclusion complex. Methods The inclusion compound of rifampicin-hydroxypropyl-β-cyclodextrin was prepared by grinding method. The inclusion complex was identified by differential scanning calorimetry and infrared spectrophotometry. UV spectrophotometry and phase solubility method Validation of rifampicin β-cyclodextrin inclusion complex formation. In vitro broth dilution assay was used to determine the inhibitory effect of inclusion complex on Staphylococcus aureus and Escherichia coli. Results Rifampicin was able to form inclusion complexes with hydroxypropyl-β-cyclodextrin in a 1: 1 molar ratio. The inclusion compound improved the solubility of the drug. The minimum inhibitory concentrations of inclusion complexes on S.aureus and Escherichia coli were 0.125μg.mL-1 and 32.0μg.mL-1, respectively. Conclusion Hydroxypropyl-β-cyclodextrin can be coated with rifampin to improve its solubility. Inclusion of Gram-positive bacteria and negative bacteria were significantly inhibited.