瑞戈非尼固体分散体的制备及体外溶出度考察

摘要

Objective To enhance the dissolution rate of regorafenib which is a poorly water - soluble drug by forma-tion of solid dispersion. Methods Solid dispersions of regorafenib were prepared by solvent method with polyvinylpyrroli-done K30 as a carrier. The dissolution of the solid dispersions in vitro was determined by UV spectrophotometry and the X- ray diffraction technology was used to analyse the distribution mode of regorafenib. Results The dissolution of rego-rafenib solid dispersions was much faster than that of regorafenib and the physical mixtures. The dissolution of regorafenib in vitro was increased as the increasement of the carrier proportion. Regorafenib existed as amorphous form in the carrier. Con-clusion Solid dispersion technology can significantly increase the dissolution of regorafenib in vitro.%目的：采用固体分散技术提高难溶性药物瑞戈非尼的体外溶出度。方法选用聚维酮 K30为载体，以溶剂法制备不同比例的瑞戈非尼固体分散体；采用紫外分光光度法测定其溶出度；采用 X -射线粉末衍射法分析药物在固体分散体中的存在状态。结果瑞戈非尼固体分散体的溶出度较原料药、物理混合物均有显著提高，且载体比例越大，固体分散体溶出度越大；瑞戈非尼以无定形态分散在载体中。结论采用固体分散技术可有效提高瑞戈非尼的体外溶出度。