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槲皮素-羟丙基-β-环糊精包合物的制备及物相鉴定

杨照罡, 古丽斯坦·阿吾提, 曹轶, 朱静, 伍博深, 王坚成, 吕万良, 张烜*, 张强   

  1. 1.北京大学药学院药剂教研室, 北京 100083;
    2.新疆药物研究所, 新疆 乌鲁木齐 830001
  • 收稿日期:2006-02-21 修回日期:2006-05-10 出版日期:2006-06-15 发布日期:2006-06-15
  • 通讯作者: 张烜*

Preparation and Physicochemical Characterization of Quercetin-HP-β-CD Inclusion Complexes

YANG Zhao-gang, Gulisitan Awuti, CAO Yi, ZHU Jing, WU Bo-shen, WANG Jian-cheng, LU Wan-liang, ZHANG Xuan*, ZHANG Qiang   

  1. 1.Department of Pharmacy, School of Pharmaceutical Science, Peking University, Beijing 100083, China;
    2. Institute of Drug Analysis, Urumqi 830001, China
  • Received:2006-02-21 Revised:2006-05-10 Online:2006-06-15 Published:2006-06-15
  • Contact: ZHANG Xuan*

摘要: 目的 用研磨法制备槲皮素-羟丙基-β-环糊精包合物, 测定包合常数及包合过程热力学参数, 并对物相进行鉴定。方法 采用研磨法制备包合物, 对其包合常数进行测定, 利用差热分析(DSC)、红外光谱分析(IR)、粉末X衍射(X-ray)、扫描电镜(SEM)等方法对其进行物相鉴定, 以溶解度和溶出实验考察其溶解性质。结果 所制备的包合物溶解度较槲皮素纯品增加约37, 5分钟的溶出百分率较槲皮素纯品提高近10倍。DSC结果表明包合物中槲皮素吸热峰位前移; IR图谱槲皮素羰基吸收峰产生位移; X-衍射图谱包合物中槲皮素吸收峰消失; 电镜扫描照片包合物中未见槲皮素晶体, 说明形成新物相。结论 研磨可使槲皮素与羟丙基β环糊精形成包合物, 改善槲皮素的溶解性。

关键词: 槲皮素, 槲皮素, 槲皮素, 羟丙基-β-环糊精, 羟丙基-β-环糊精, 羟丙基-β-环糊精, 包合物, 包合物, 包合物, 包合常数, 包合常数, 包合常数, 物相鉴定, 物相鉴定, 物相鉴定

Abstract: Aim To prepare and characterize the QURC-HP-β-CD inclusion complexes and investigate the thermodynamic parameters of the process. Methods QURC-HP-β-CD inclusion complexes were prepared by the grinding method. The equilibrium inclusion constants and thermodynamic parameters were determinated by phase solubility analysis. Dissolution tests were performed to study the dissolution rate of inclusion complexes. The formation of inclusion complexes was confirmed by differential scanning calorimetry (DSC), infrared spectroscopy (IR), powder X-ray diffractometry (PXRD) and scanning electron microscopy (SEM). Results The aqueous solubility of quercetin was greatly increased (about 37 folds) by inclusion technique, and the initial dissolution rate was markedly improved (10 folds) in the first 5 min. The results of DSC and SEM photographs showed that quercetin crystal disappeared in inclusion complexes, which indicated the formation of new phase. FT-IR spectra showed that the carbonyl absorption band of quercetin was shifted. PXRD showed that the diffraction peak of quercetin crystal disappeared. Conclusion QURC-HP-β-CD inclusion complexes are produced by the grinding method. The solubility of quercetin is improved by the inclusion technique.

Key words: quercetin, quercetin, hydroxypropyl-β-cyclodextrin, hydroxypropyl-β-cyclodextrin, inclusion complex, inclusion complex, inclusion constant, inclusion constant, Phase behavior, Phase behavior

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Supporting: *Corresponding author. Tel.: 86-10-82802683; fax: 86-10-82802791