芦丁-羟丙基-β-环糊精包合物的反溶剂法制备与表征
Characterization and Preparation of Inclusion Complex of Rutin-Hydroxypropyl-β-Cyclodextrin Prepared by Antisolvent Method
DOI: 10.12677/BR.2018.73035, PDF,  被引量    国家科技经费支持
作者: 刘艳杰, 赵修华, 邱 琳, 吴微微, 李媛媛, 王 力：东北林业大学森林植物生态学教育部重点实验室，黑龙江 哈尔滨
关键词: 芦丁；羟丙基-β-环糊精；包合物；反溶剂法；饱和溶解度；体外溶出；Rutin； Hydroxypropyl-β-Cyclodextrin； Inclusion Complex； Antisolvent Method； Saturation Solubility； In Vitro Dissolution
摘要: 目的：为提高芦丁在水中的溶解度，本实验采用反溶剂法制备芦丁-羟丙基-β-环糊精(RU-HP-CD)包合物，对其结构进行表征，并考察了包合物的体外释放情况。方法：采用反溶剂法，将芦丁(RU)和羟丙基-β-环糊精(HP-CD)以摩尔比1:1溶解在二甲基甲酰胺中，并用丙酮作为反溶剂制备包合物。利用高效液相色谱法测定包合物的含药量，X-射线衍射(XRD)、红外光谱(IR)和扫描电镜(SEM)对包合物进鉴定，并对芦丁原药和包合物的体外溶出速率进行了比较。结果：经XRD和IR检测，确定芦丁与羟丙基-β-环糊精形成包合物，含药量为26.5%。SEM结果呈示出包合物的特殊形态。包合物的水中溶解度和体外溶出速率分别是原药的15倍和4倍。结论：反溶剂法获得了高含药量的RU-HP-CD，并改善了芦丁的水溶性，也为环糊精包合物的制备提供了新的方法。
Abstract: Objective: To improve the solubility of rutin in water, the inclusion complex of rutin-hydroxy- propyl-β-cyclodextrin (RU-HP-CD) was prepared by antisolvent method and characterized. In addition the dissolution rate of RU-HP-CD was also investigated. Methods: Rutin (RU) and hydroxypropyl-β-cyclodextrin (HP-CD) were dissolved in dimethylformamide in a molar ratio of 1:1, and acetone was used as an antisolvent. The content of rutin in the inclusion complexes was determined by high performance liquid chromatography. X-ray diffraction (XRD), infrared spectroscopy (IR), and scanning electron microscopy (SEM) were used to identify the inclusion complex. The dissolution rates of rutin and inclusion complex in vitro were determined. Results: The results of XRD and IR showed that inclusion complex of rutin and hydroxypropyl-β-cyclodextrin was obtained using antisolvent method, containing 26.5% rutin. SEM results showed the specific morphology of the inclusion complex. The solubility in water and in vitro dissolution rate of the inclusion complex were 15 and 4 times that of the rutin respectively. Conclusions: The water solubility of RU-HP-CD obtained by antisolvent method was improved. A new method for the preparation of cyclodextrin inclusion compound was provided in this study.
文章引用：刘艳杰, 赵修华, 邱琳, 吴微微, 李媛媛, 王力. 芦丁-羟丙基-β-环糊精包合物的反溶剂法制备与表征[J]. 植物学研究, 2018, 7(3): 277-282. https://doi.org/10.12677/BR.2018.73035

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