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目的提高水飞蓟宾的生物利用度。方法采用固体分散载体和阻滞性高分子材料,使用固体分散与球晶制粒相结合的技术制备水飞蓟宾缓释微球。运用差示热分析及X-射线粉末衍射检测水飞蓟宾在微球中分散状态,采用扫描电子显微镜观察微球的形态、表面结构和内部结构,并对微球的特性如平均粒径、粒径分布、松密度进行评价。结果研制微球的大小可由搅拌速度来控制,水飞蓟宾从缓释微球中的释放速度随分散剂的量的增加而增加,阻滞剂可延缓药物的释放。微球中药物的释放速度能够通过调节分散剂和阻滞剂的比例来控制。X射线衍射与差示热分析结果表明:水飞蓟宾以无定型高度分散在微球中。在40℃,相对湿度75%条件下,加速三个月,药物释放与含量不会改变。结论水飞蓟宾缓释微球可通过采用固体分散与球晶制粒相结合的技术一步制成。该制备过程简便、重现性好、成本低,是水不溶性药物制备缓释微球的有效方法。
Objective To improve the bioavailability of silybin. Methods Silicone silanol sustained release microspheres were prepared by using solid dispersion carrier and block polymer, and the combination of solid dispersion and spherulite granulation. The dispersion state of silibinin in the microspheres was detected by differential thermal analysis and X-ray powder diffraction. Morphology, surface structure and internal structure of the microspheres were observed by scanning electron microscopy. The properties of microspheres such as average particle size, Particle size distribution, bulk density were evaluated. Results The size of the microspheres was controlled by the stirring speed. The release rate of silybin from the sustained-release microspheres increased with the amount of dispersant, and the blockers could delay the release of the drug. The release rate of drug in microspheres can be controlled by adjusting the ratio of dispersant to blocker. The results of X-ray diffraction and differential thermal analysis show that silybin is dispersed in the microspheres at an amorphous height. At 40 ℃, relative humidity of 75%, accelerated three months, drug release and content will not change. Conclusion Silybin sustained-release microspheres can be made in one step using a combination of solid dispersion and spherulite granulation. The preparation process is simple, reproducible, and low in cost, and is an effective method for preparing sustained-release microspheres from water-insoluble drugs.