伊马替尼-槲皮素共无定型纳米制剂的制备与表征

Preparationand Characterizationof Co-Amorphous Nanoparticles of Imatinib-Quercetin

目的研究制备伊马替尼-槲皮素共无定型纳米制剂,以提高药物在水中的溶解度。方法通过加热搅拌法获得伊马替尼-槲皮素的共无定型物质。以聚维酮K30为稳定剂,采用反溶剂沉淀法将伊马替尼-槲皮素制成纳米制剂。对纳米制剂和共无定型物进行表征分析,并比较纳米制剂、共无定型物以及原料药的饱和溶解度。结果伊马替尼-槲皮素纳米制剂的粒径为(157.3±4.5)nm,分散指数(PDI)=0.135,粒径较小且分布均匀;纳米制剂中伊马替尼和槲皮素的含药量分别为20.21%和3.53%;与共无定型物和原料药比较,均有显著提高。结论制备获得的伊马替尼-槲皮素纳米制剂粒径较小且分布均匀,能显著增加难溶药物伊马替尼和槲皮素的溶解度。

Objective A new co-amorphous nanoparticles of imatinib-quercetinwas prepared in order to improve the solubility of imatinib and quercetin.Methods The co-amorphous material of imatinib-quercetin was obtained by heating and stirring,and the co-amorphous nanoparticles of imatinib-quercetinwas prepared by anti-solvent method using PVP K30 as a stabilizer.Then the characterization and analysis were carried out on the nanoparticles and co-amorphous substance,including powder X-ray diffraction(PXRD),differential scanning calorimetry(DSC),infrared spectroscopy(IR),andsaturation solubility.Results The nanoparticles with small particle size[(157.3±4.5)nm,PDI=0.135]was well distributed.The drug loading rates of imatinib and quercetin were 20.21%and 3.53%,respectively,which were significantly improved compared to co-amorphous substance and raw materials.Conclusion The nanoparticles of imatinib-quercetin can significantly improve the saturation solubility of theinsoluble imatinib and quercetin.