姜黄素羟丙基-β-环糊精包合物的制备及其性质研究

目的 制备姜黄素-羟丙基-β-环糊精(CUR-HP-β-CD)包合物,并对其进行性质考察.方法 采用搅拌-冷冻干燥法制备CUR-HP-β-CD包合物,以HPLC法测定姜黄素(CUR)的量;运用正交试验法,以包合率和包合物收率为综合指标,优化CUR-HP-β-CD包合物的制备工艺;采用紫外光谱、X射线衍射分析、熔点测定验证包合物;通过相溶解度法考察包合物中主客体分子之间的包合物物质的量之比,并对其油水分配系数、表观溶解度和水溶液的稳定性进行了考察.结果 采用搅拌-冷冻干燥法,在温度40℃、CUR与羟丙基-β-环糊精(HP-β-CD)质量比为1∶5(mg/g)、包合时间3h的条件下制备CUR-HP-β-CD包合物.经验证包合率达97％、包合物得率达99％,其冻干粉经鉴别已形成包合物,工艺优化成功.25℃下能形成物质的量之比为1∶1的包合物,相溶解度图呈AL型,表观溶解度35 μg/mL.样品溶液在室温(25～30℃)自然放置50d后测得包合物质量分数为95％,而CUR原料药则全部分解.结论 以最佳工艺条件制备的CUR-HP-β-CD包合物重现性好,工艺稳定,能显著提高CUR的溶解度及稳定性.

Preparation of curcumine-hydroxypropyl-β-cyclodextrin inclusion complex and its properties

Objective To prepare the curcumine-hydroxypropyl-β-cyclodextrin(CUR-HP-β-CD) inclusion complex and observe its properties.Methods The inclusion complex was prepared by the stirring-freeze-dry method and the content of CUR was determined by HPLC.The preparation technology was optimized by orthogonal test with inclusion rate and yield of inclusion complex as indexes.The inclusion complex was identified by ultraviolet(UV) spectrometry,X-ray diffraction(XRD),and melting point detection.The molar ratio between host and guest molecules was researched by phase solubility method.And the oil-water partition coefficient,apparent solubility,and the stability of aqueous solution were also observed.Results Using stirring-freezedry method,the optimum preparation procedure was: inclusion temperature 40 ℃,the ratio of CUR with HP-β-CD 1∶5(mg/g),and inclusion time 3 h.The average inclusion rate of the complex was 97%,and the yield was 99%.Results showed that freeze-dried powder was made into inclusion complex.The 1∶1 molar ratio inclusion complex of CUR with HP-β-CD could be formed at 25 ℃.The phase diagram was ALtype with apparent solubility of 35 μg/mL.The content of inclusion complex remained 95% after placing in the natural environment at room temperature for 50 d,while CUR raw material decomposed thoroughly.Conclusion The prepared CUR-HP-β-CD with optimized technology has good reproducibility,stable technology,and could obviously improve the stability and the solubility of CUR.