| 摘要: |
| 【目的】制备盐酸沙拉沙星β-环糊精包合物，并评价其溶解度和稳定性。【方法】通过L9（34）正交试验设计，优化β-环糊精饱和水溶液法制备盐酸沙拉沙星包合物的工艺。采用紫外可见分光光度法测定药物的质量浓度，考察药物和包合物的溶解度及光稳定性；用X射线衍射对制备的盐酸沙拉沙星β-环糊精包合物进行表征。【结果】盐酸沙拉沙星β-环糊精包合物的最佳制备条件为：盐酸沙拉沙星与β-环糊精投料质量比为1∶5、包合温度30 ℃、反应时间3 h，在该条件下制备的盐酸沙拉沙星β-环糊精包合物的收率为86%；其溶解度及稳定性分别是原料药的4.87倍和1.83倍；X射线衍射分析表明，盐酸沙拉沙星β-环糊精包合物制备成功。【结论】确定了盐酸沙拉沙星β-环糊精包合物的最佳制备工艺条件，在该条件下制备的包合物可以提高盐酸沙拉沙星的溶解度和稳定性。 |
| 关键词: 盐酸沙拉沙星 β-环糊精 包合物 制备工艺 |
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| 基金项目:山东省科技发展计划项目(2011GNC11105) |
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| Preparation of sarafloxacin hydrochloride β-cyclodextrin inclusion complexes |
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| Abstract: |
| 【Objective】The study aimed to prepare sarafloxacin hydrochloride β-cyclodextrin inclusion complexes and evaluate the solubility and stability.【Method】Sarafloxacin hydrochloride β-cyclodextrin inclusion complexes were prepared by saturated water solution.The preparation conditions were selected by L9(34) orthogonal experimental design.UV spectrophotometry was used to determine the content of sarafloxacin hydrochloride and evaluate solubility and light stability of sarafloxacin hydrochloride and water solutions of its inclusion complexes,and their structures were characterized by X-ray diffraction.【Result】The optimum preparation conditions of sarafloxacin hydrochloride β-cyclodextrin inclusion complexes were established as follows:the quality ratio of sarafloxacin hydrochloride and β-cyclodextrin was 1∶5,inclusion temperature was 30 ℃,reaction time was 3 h,and yield was 86%.The solubility and stability of sarafloxacin hydrochloride in β-cyclodextrin inclusion complexes were 4.87 times and 1.83 times of that of raw materials,respectively.X-ray diffraction analysis showed sarafloxacin hydrochloride β-cyclodextrin inclusion complexes were prepared successfully.【Conclusion】The optimal preparation conditions of sarafloxacin hydrochloride β-cyclodextrin inclusion complexes were determined.The preparation of sarafloxacin hydrochloride Z-cyclodextrin inclusion complexes could increase the solubility and stability of sarafloxacin hydrochloride significantly. |
| Key words: sarafloxacin hydrochloride β-cyclodextrin inclusion complex preparation condition |
