利福平-羟丙基-β-环糊精包合物的制备和评价

Preparation and Evaluation of Rifampicin Hydroxypropyl-β-Cyclodextrin Inclusion Compound

关键词:  利福平  羟丙基-β-环糊精  包合物  制备  评价

Key words:  rifampicin  hydroxypropyl-β-cyclodextrin  inclusion complex  preparation  evaluation

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。

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 mg·mL^-1 and 32.0 mg·mL^-1. CONCLUSION The solubility of rifampicin was increased. The growth of staphylococcus and Escherichia coli could be inhibited by rifampicin HP-β-CD.