Sorafenib microcrystalline preparation and preparation method and application thereof

The invention provides a sorafenib microcrystalline preparation and a preparation method and application thereof. The sorafenib microcrystalline preparation can realize long-acting inhibition of HCC cell proliferation and tumor formation by single injection of sorafenib in tumor tissues. Meanwhile, the drug release experiment definitely proves that the sorafenib microcrystalline preparation can ensure the long-term retention of the drug in tumor tissues. Although the solubility and bioavailability of sorafenib are limited, the properties of sorafenib can be improved to a certain extent after sorafenib is prepared into a microcrystal preparation, and the release rate of the drug can be adjusted by controlling the particle size of microcrystals. 本发明提供了一种索拉非尼微晶制剂及其制备方法和用途，使索拉非尼在肿瘤组织内的单次注射即能够实现长效抑制HCC细胞增殖与成瘤作用。同时，药物释放实验明确证实，索拉非尼的微晶制剂能够保证药物在肿瘤组织内部的较长期留存。尽管索拉非尼的溶解度与生物利用度有限，但将其制备为微晶制剂后能够对其性质进行一定程度的改善，通过控制微晶的粒径也能够对药物的释放速率进行调整。