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槲皮素PVP固体分散体的制备及物相鉴定

朱静, 杨照罡, 陈晓梅, 孙葭北, 古丽斯坦·阿吾提, 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:2006-10-10 修回日期:2007-02-10 出版日期:2007-03-15 发布日期:2007-03-15
  • 通讯作者: 张烜*

Preparation and physicochemical characterization of solid dispersion of quercetin and polyvinylpyrrolidone

Jing Zhu, Zhao-GangYang, Xiao-Mei Chen, Jia-Bei Sun, Gulisitan Awuti, Xuan Zhang*, Qiang Zhang   

  1. 1. Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing 100083, China;
    2. Institute of Drug Analysis, Urumqi 830001, China
  • Received:2006-10-10 Revised:2007-02-10 Online:2007-03-15 Published:2007-03-15
  • Contact: Xuan Zhang*

摘要:

目的 用溶剂法制备槲皮素-PVP固体分散体并考察其溶出特性并对物相进行鉴定。方法 采用溶剂法制备槲皮素-PVP固体分散体,通过溶出实验对槲皮素溶出率的测定研究固体分散体的溶出性质, 利用差热分析(Differentialscanning calorimetry, DSC)、红外光谱分析(Infrared spectroscopy, IR)、粉末X衍射(X-ray powder diffractometry, PXRD)、扫描电镜(Scanning electron microscopy, SEM)等方法对其进行物相鉴定。结果 槲皮素-PVP固体分散体的溶出速率相对其物理混合物有了明显的改善; 溶解实验显示固体分散体中槲皮素的溶解度有了显著的提高; 热差分析及粉末X衍射结果表明固体分散体中槲皮素呈非结晶形式; 扫描电镜下固体分散体中无槲皮素晶体。结论 采用溶剂法制备槲皮素-PVP固体分散体可显著提高槲皮素的溶解度及溶出速度。

关键词: 槲皮素, 槲皮素, 槲皮素, PVP, PVP, PVP, 固体分散体, 固体分散体, 固体分散体, 溶出率, 溶出率, 溶出率

Abstract: Aim The objective of this study was to prepare and characterize quercetin-polyvinylpyrrolidone (Qurc-PVP) solid dispersion with the intention of improving its dissolution properties. Methods Qurc-PVP solid dispersion was prepared by solvent method. The release rate of quercetin was determined from dissolution studies and the physicochemical properties of solid dispersion were investigated by differential scanning calorimetry (DSC), infrared spectroscopy (IR), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM). Results The results showed that the dissolution rate of quercetin was significantly improved by solid dispersion compared to that of the pure drug and physical mixture. Solubility studies revealed a markedly increase in the solubility of quercetin. The results of DSC and PXRD showed that the quercetin in solid dispersion was amorphous form. From SEM analysis, there was no quercetin crystal observed in the solid dispersions. Conclusion The solubility and dissolution of quercetin were improved by solid dispersion technique.

Key words: Quercetin, Quercetin, Polyvinylpyrrolidone PVP, Polyvinylpyrrolidone PVP, Solid dispersion, Solid dispersion, Dissolution rate, Dissolution rate

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