槲皮素环糊精包合物的制备工艺及溶解性研究
目的 筛选槲皮素-β-环糊精包合物及槲皮素-羟丙基-β-环糊精包合物的最佳制备方法及工艺条件, 并进行包合物的鉴定及溶解度测定。方法 采用溶液搅拌法、超声波法和研磨法比较包合物的制备效果; 溶液搅拌法的包合物制备工艺以包合得率为指标, 分别考察投料摩尔比、包合温度、包合时间及溶液pH值对包合物得率的影响, 并通过正交试验优化; 采用薄层鉴别法及红外光谱法对包合物进行鉴定。结果 通过比较包合物得率, 采用溶液搅拌法制备槲皮素-β-CD和槲皮素-HP-β-CD包合物更好; 包合物制备的最佳工艺条件为: 投料摩尔比为1:1、制备温度为60 ℃、制备时间为2 h、溶液pH值为7; 在此条件下制备槲皮素-β-CD包合物的平均包合得率为66.22%, 制备槲皮素-HP-β-CD包合物平均得率可达71.49%; 槲皮素-β-CD包合物溶解度为26.94 μg/mL, 槲皮素-HP-β-CD包合物在水中的溶解度可增加到2224.21 μg/mL。槲皮素在0.8~6.4 μg/mL浓度范围内呈良好的线性关系(r=0.9999)。结论 溶液搅拌法使槲皮素与环糊精衍生物形成包合物, 且明显增加了槲皮素在水中的溶解性, 有利于药物在体内的吸收并提高了生物利用率。
Objective To select the best preparation method and technological conditions of quercetin-β- cyclodextrin (quercetin-β-CD) inclusion complex and quercetin-hydroxypropyl-β-cyclodextrin (quercetin-HP-β-CD) inclusion complex, identify the inclusion complexes and study their solubility. Methods Solution mixing method, ultrasonic method and grinding method were used for the preparation of inclusion complexes and their effect were compared. Using the ratio of inclusion complexes as index, the technological conditions of solution mixing method, including the feeding molar ratio, inclusion temperature, inclusion time and medium pH value were respectively investigated, and optimized based on the orthogonal experiment. Then the inclusion complexes were identified by thin layer chromatography (TLC) and infrared spectroscopy. Results The inclusion complexes of quercetin-β-CD and quercetin-HP-β-CD were better prepared by the solution mixing method after the comparison of ratio of inclusion complexes. The optimum conditions for preparing inclusion complexes was A1B2C2D2, namely: the feeding molar ratio was 1: 1, the preparation temperature was 60 ℃, time-consuming of preparation was 2 h, and medium pH value was 7. The average inclusion ratio of quercetin-β-CD was 66.22%, and that of quercetin-HP-β-CD was 71.49%. The solubility of quercetin-β-CD inclusion complex was 26.94 μg/mL, and that of quercetin-HP-β-CD inclusion complex could be increased to 2224.21 μg/mL. The quercetin had a good linear relationship in the range of 0.8~6.4 μg/mL with the correlation coefficient of 0.9999. Conclusion The quercetin and the cyclodextrin derivative can form inclusion complexes by the solution mixing method, and then the solubility of quercetin in water can be significantly increased, which is conducive to drug absorption in the body and can increase the bioavailability.
标题：槲皮素环糊精包合物的制备工艺及溶解性研究
英文标题：Preparation technology and solubility of quercetin-cyclodextrin inclusion complexes
作者：
库尔班江.巴拉提 新疆伊犁师范学院化学与生物科学学院新疆伊宁
中文关键词:槲皮素,β-环糊精,羟丙基-β-环糊精,包合物,制备工艺,
英文关键词:quercetin,β-cyclodextrin,hydroxypropyl-β-cyclodextrin,inclusion complexes,preparation technology,
发表日期：2015-11-19
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