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目的:制备布洛芬-羟丙基-β-环糊精(IBU-HP-β-CyD)包合物,提高布洛芬(IBU)在水中溶解度。方法:冷冻干燥法制备IBU-HP-β-CyD包合物,连续变化法确定包合比例,正交设计优化处方,紫外分光光度法测定包合物的载药量和溶解度,差式扫描量热法(DSC)法鉴别包合物的形成。结果:包合比例1:1时载药量最高,所制备的三批包合物平均载药量分别为10.52%、10.21%、10.38%,溶解度分别为46.14,45.42,45.78 mg·ml~(-1)。结论:通过HP-β-CyD的包合作用使IBU的溶解度显著提高。
OBJECTIVE: To prepare inclusion compound of ibuprofen-hydroxypropyl-β-cyclodextrin (IBU-HP-β-CyD) to improve the solubility of ibuprofen in water. Methods: The IBU-HP-β-CyD inclusion complex was prepared by freeze-drying method. The inclusion ratio was determined by continuous variation method. The prescription was optimized by orthogonal design. The drug loading and solubility of inclusion complex were determined by ultraviolet spectrophotometry. Thermal analysis (DSC) method to identify the formation of inclusion complex. Results: The highest drug loading was obtained when the inclusion ratio was 1: 1. The average drug loadings of the three batches were 10.52%, 10.21% and 10.38%, respectively, and the solubilities were 46.14, 45.42 and 45.78 mg · ml ~ -1). Conclusion: The solubility of IBU is significantly increased by inclusion of HP-β-CyD.