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PVP K30对葛根黄豆苷元溶解度和溶出的影响

郭圣荣*, 郭丽   

  1. 上海交通大学药学院, 上海 200030
  • 收稿日期:2003-08-10 修回日期:2004-02-10 出版日期:2004-03-15 发布日期:2004-03-15
  • 通讯作者: 郭圣荣*

Effects of PVP K30 on Aqueous Solubility and Dissolution Properties of Daidzein

GUO Sheng-rong*, GUO Li   

  1. School of Pharmacy, Shanghai Jiaotong University, Shanghai 200030, China
  • Received:2003-08-10 Revised:2004-02-10 Online:2004-03-15 Published:2004-03-15
  • Contact: GUO Sheng-rong*

摘要: 目的 研究PVP K30 对葛根黄豆苷元水溶解性和溶出性质的影响. 方法 测量葛根黄豆苷元及其固体分散体、物理混合物的水溶解度和溶出速度,并用X-射线衍射、IR表征药物与PVP在固态条件下的相互作用.结果 Gibbs自由能和转移焓均小于零,表明葛根黄豆苷元从磷酸盐缓冲溶液中转移到PVP的磷酸盐缓冲溶液中是一自发的过程; X-射线衍射结果表明葛根黄豆苷元在PVP固体分散体(药物:PVP<1:5)中以无定形形式存在; IR结果表明葛根黄豆苷元的羟基与PVP分子中的C=O之间存在相互作用. 结论 葛根黄豆苷元的PVP分散体可大大提高药物溶解度和溶出速度.

关键词: 葛根黄豆苷元, PVP K30, 溶解度, 固体分散体, X射线衍射法, 红外光谱

Abstract: Aim To study effects of PVP K30 on the aqueous solubility and dissolution properties of daidzein. Methods To measure the aqueous solubility and dissolution rates of daidzein in three different states (within solid dispersions, physical mixtures and as a pure drug) and investigate drug-polymer interactions in the solid state using X-ray powder diffraction and fourier-transform infrared spectroscopy. Results The negative values of the Gibbs free energy and enthalpy of transfer explained the spontaneous transfer of daidzein from phosphate buffer solution (PBS) to a solution of PVP in PBS.X-ray powder diffraction patterns showed that the drug was in the amorphous state (ratio of the drug:PVP<1:5) when dispersed in PVP K30.The infrared spectra indicated there exist interactions between the OH of daidzein and the C=O of PVP K30. Conclusion the dispersion of daidzein in PVP K30 considerably enhances the solubility and dissolution rate.

Key words: daidzein, daidzein, PVP K30, PVP K30, solubility, solubility, solid dispersion s, solid dispersion s, X-ray powder diffraction, X-ray powder diffraction, infrared spectroscopy, infrared spectroscopy

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Supporting: *Corresponding author. Tel.: 021-62932415