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白藜芦醇/ 羟丙基-β-环糊精包合物的表征及体外溶出研究
齐学洁1,2, 邱超2,3, 姜恒丽2,3, 崔元璐2,3
1.天津中医药大学中药学院, 天津300193;2.天津市现代中药重点实验室, 天津300193;3.天津中医药大学中医药研究院, 天津300193
摘要:
[目的] 制备并鉴定白藜芦醇/羟丙基-β-环糊精包合物,考察白藜芦醇与羟丙基-β-环糊精之间的摩尔质量比,并进行体外释放研究.[方法] 采用冷冻干燥法制备白藜芦醇/羟丙基-β-环糊精包合物,采用红外光谱(FT-IR)、差示扫描量热分析(DSC)和X-Ray衍射分析(XRD)方法对包合物进行了结构鉴定.用高效液相色谱(HPLC)法测定包合物的载药量及其体外释放.[结果] 证实白藜芦醇/羟丙基-β-环糊精包合物已经形成,主、客分子的摩尔比为1:1,包合常数为1621M-1,溶解度和溶出速率均有所增大.[结论] 白藜芦醇/羟丙基-β-环糊精包合物能显著增大药物的溶解度、稳定性和溶出速率.
关键词:  白藜芦醇  羟丙基-β-环糊精  包合物  溶解度
DOI:10.11656/j.issn.1672-1519.2013.08.19
分类号:
基金项目:国家自然科学基金资助项目(81173469).
Characterization and dissolution of resveratrol/hydroxypropyl-β-cyclodextrin inclusion complex
QI Xue-jie袁1,2, QIU Chao2,3, JIANG Heng-li2,3, CUI Yuan-lu2,3
1.Chinese Medicine School of TCM, Tianjin University of TCM, Tianjin 300193, China;2.Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin 300193, China;3.Research Center of TCM, Tianjin University of TCM, Tianjin 300193, China
Abstract:
[Objective] Resveratrol hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex is prepared and characterized, stoichiometry of host and guest is determined and the dissolubility is also investigated.[Methods] The inclusion complex was prepared by freezedrying method, and characterized by Fourier-transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and X-ray diffractometry (XRD).Drug content and release in vitro were determined by HPLC.[Results] It was defined that Resveratrol/HP-β-CD inclusion complex formed.Resveratrol/HP-β-CD was classified as AL-type with the ratio of 1:1 between host and guest, and the complexation constant was 1621M-1 by the phase solubility diagram method.Compared to the drug alone, solubility and dissolving rate of inclusion complex increased.[Conclusion] The solubility, stability and dissolving rate of drug increases in inclusion complex of Resveratrol/HP-β- CD.
Key words:  resveratrol  hydroxypropyl-β-cyclodextrin  inclusion complex  solubility
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