PEG 6 000固体分散体系对难溶性药物水飞蓟素的增溶作用与晶格变化的关系

目的研究PEG 6 000固体分散体系对难溶性药物增溶的相关晶格变化规律。方法用熔融法制备水飞蓟素的PEG 6 000固体分散体,通过体外释药试验考察固体分散技术对水飞蓟素的增溶作用,以X-射线粉末多晶衍射结合相应的衍射峰处理软件系统分析PEG 6 000及药物的晶格参数的变化,经傅立叶变换红外光谱(FT-IR)验证PEG 6 000与药物之间的相互作用。结果与原药比较,固体分散体中药物的释放速率明显增大,PEG 6 000固体分散体系对难溶性药物水飞蓟素具有显著的增溶作用。X-射线多晶衍射分析表明,PEG 6 000及药物在固体分散体中的晶格点阵面间距离、衍射峰位移及其相对强度等发生了规律性变化,药物与载体间无相互作用。结论PEG 6 000固体分散体系的增溶作用与载体材料和药物的晶格参数的改变密切相关。

RELATIVITIES BETWEEN LATTICE CHANGES AND THE FUNCTION OF DISSOLUTION IMPROVEMENT OF POORLY SOLUBLE DRUG SILYMARIN BASED UPON PEG 6 000 SOLID DISPERSION SYSTEM

AIM To investigate the lattice mechanisms involved in the increased dissolution effect of polyethylene glycol (PEG 6 000 ) dispersion system on poorly soluble drug silymarin (SILY). METHODS Fusion method was used to prepare the solid dispersions of SILY with PEG 6 000 . Evaluation of the improvement of dissolution was performed with dissolution studies in vitro . X ray powder diffraction combined with diffraction peak pattern fitting procedure were applied to quantitatively analyze the changes of lattice parameters. The interaction of SILY and PEG 6 000 was also determined with Fourier transform infrared (FT IR) spectroscopy. RESULTS The dissolution rate of SILY was considerably increased when formulated in solid dispersion of PEG 6 000 as compared to pure SILY. The datum from the X ray diffraction showed the changes in the lattic spacings and particular diffraction peaks (position and the intensity) of PEG 6 000 and SILY. These could explain the increased rate of SILY released from solid dispersion system. The information of FT IR spectroscopy showed the absence of well defined drug polymer interaction. CONCLUSION The dissolution improvement of poorly soluble SILY from solid dispersion of PEG 6 000 can be illuminated by the changes of the lattice parameters of PEG 6 000 and the drug.