姜黄素环糊精分子包合物的构建和优化

Preparation and Process Optimization of Curcumin-Cyclodextrin Inclusion Complexes

DOI:10.3969/j.issn.1673-1689.2017.11.011

中文关键词: 姜黄素 分子包合物 构建 优化

英文关键词: curcumine,preparation process,orthogonal experiment

基金项目:

作者

单位

李艺

重庆医科大学 药物高校工程研究中心重庆 400016

梅虎

重庆大学 生物工程学院重庆 400023

赵春景

重庆医科大学附属第二医院药剂科重庆 400010

王红

重庆医科大学 药物高校工程研究中心重庆 400016

罗文

重庆医科大学附属第二医院药剂科重庆 400010

张景勍

重庆医科大学 药物高校工程研究中心重庆 400016

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中文摘要:

构建、优化和计算机模拟可增溶姜黄素(CCN)的环糊精分子包合物(CCIC)。采用研磨法制备CCIC,显微观察法、差示量热扫描法、红外光谱法验证包合物的形成。以溶解度为评价指标,通过正交设计优化CCIC的制备工艺。用计算机进行CCIC的分子结构模拟。结果表明:CCIC最优制备工艺为包合投料比(摩尔比)为1∶1,研磨温度为40 ℃,包合时间为1.5 h。最优化处方工艺下姜黄素溶解度较游离药物提高了3.82×104倍。分子模拟结果显示分子包合可降低包合系统能量。因此,可成功构建、优化和计算机模拟CCIC,其溶解度较CCN大大提高。

英文摘要:

In order to improve the water solubility of curcumin(CCN),curcumin-cyclodextrin inclusion complexes(CCIC) were prepared and the preparing process was optimized. The CCIC was prepared by grinding method. Microscopic observation method,differential scanning calorimetry,and infrared spectroscopy method were used to validate the formation of the CCIC. The orthogonal design was used to optimize the preparation process of CCN. Solubility was a evaluation index. The optimal condition of these three effects to prepare CCN were that the inclusion of feed ratio was 1∶1,the grinding temperature was 40 ℃,the inclusion time was 1.5 h. The solubility of CCN in inclusion complex prepared by optional condition was(1.72±0.03) mg/mL which increased 3.82×104 times compared with free drug. The process was stable and feasible. The preparation process was repeatable and reasonable. It effectively improved the solubility of CCN in the water.

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