水飞蓟素-聚乙二醇6000固体分散体系的制备及其特征考察

水飞蓟素-聚乙二醇6000固体分散体系的制备及其特征考察

李凤前^*, 胡晋红, 姜远英

1.第二军医大学长海医院药学部, 上海 200433;
2.第二军医大学药学院, 上海 200433

收稿日期:2002-10-16 修回日期:2003-05-10 出版日期:2003-06-15 发布日期:2003-06-15
通讯作者: 李凤前*

Preparation and Characterization of Solid Dispersions of Silymarin with Polyethylene Glycol 6000

LI Feng-qian^*, HU Jin-hong, JIANG Yuan-ying

1.Department of Pharmaceutical Sciences, Changhai Hospital, Second Military Medical University, Shanghai 200433, China;
2.School of Pharmacy, Second Military Medical University, Shanghai 200433, China

Received:2002-10-16 Revised:2003-05-10 Online:2003-06-15 Published:2003-06-15
Contact: LI Feng-qian*

摘要/Abstract

摘要： 目的制备水飞蓟素固体分散体, 加快药物的溶出, 并进行特征考察. 方法以聚乙二醇6000(PEG 6000)为材料, 采用熔融法将难溶性药物水飞蓟素制成固体分散体, 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, 并以X-射线粉末衍射、傅立叶变换红外光谱(FT-IR)考察水飞蓟素固体分散体的特性. 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 6000固体分散体系能显著加快水飞蓟素的溶出. X-射线粉末衍射分析表明, PEG 6000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均发生了规律性变化, FT-IR分析表明PEG 6000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均发生了规律性变化, FT-IR分析表明PEG 6000与药物间无相互作用. 结论 PEG 6000固体分散体系的对难溶性药物溶出和扩散的加快, 与载体材料和药物的晶格参数的改变密切相关.

关键词: 水飞蓟素, 固体分散体系, X-射线粉末衍射, 傅立叶变换红外光谱, 溶出, 聚乙二醇6000

Abstract: Aim To prepare and characterize solid dispersions of silymarin with the intention of improving their dissolution properties. Methods The solid dispersions were prepared by the fusion method with polyethylene glycol 6000 (PEG 6000) as the carrier. Evaluation of the properties of the dispersions was performed using dissolution studies, X-ray powder diffraction and Fourier-transform infrared (FT-IR) spectroscopy. Results The rate of dissolution of silymarin was considerably improved as compared with pure silymarin when formulated in solid dispersions with PEG 6000. The data of the X-ray diffraction showed some changes in the parameters of lattice spacing [d], peak position and relative intensities. FT-IR together with those from X-ray diffraction showed the absence of well-defined drug-polymer interactions. Conclusion The dissolution improvement of poorly soluble silymarin could be illuminated by the changes of the lattice parameters of PEG 6000 and the drug.

Key words: silymarin, silymarin, solid dispersions, solid dispersions, X-ray powder diffraction, X-ray powder diffraction, FT-IR spectroscopy, FT-IR spectroscopy, dissolution, dissolution, PEG 6000, PEG 6000

中图分类号:

R943

Supporting: Foundation item: Supported by the National 863 Program Project of China, No.2002AA2Z346C.
^*Corresponding author. Tel.: 86-21-25070674; fax: 86-21-25070668

李凤前^*, 胡晋红, 姜远英. 水飞蓟素-聚乙二醇6000固体分散体系的制备及其特征考察[J]. .

LI Feng-qian^*, HU Jin-hong, JIANG Yuan-ying . Preparation and Characterization of Solid Dispersions of Silymarin with Polyethylene Glycol 6000[J]. .

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