秋水仙碱磷脂复合物的制备及质量评价

Preparation and quality evaluation of colchicine phospholipid complex

目的:制备秋水仙碱磷脂复合物(Col-PC)并进行表征,探讨Col-PC对HSC-T6的作用。方法:采用溶剂法制备Col-PC,以复合率为指标,通过正交试验,确定Col-PC的最佳工艺条件。采用差示扫描量热法对所制Col-PC进行表征;通过MTT试验考察对HSC-T6细胞的抑制作用。结果:最佳工艺条件为秋水仙碱(Col)与磷脂的比为1∶3,在40℃下反应1 h,得到Col-PC复合率为88.83%(RSD=0.20%,n=3)。制备成磷脂复合物后,油水分配系数从1.187提高到1.512;Col-PC和Col对HSC-T6的IC50分别为152.7μg/mL和6.57μg/mL。结论:Col-PC的制备工艺稳定可靠、重复性好,对HSC-T6细胞的抑制作用较好,为Col新型靶向给药制剂的研发奠定基础。

Objective:To prepare and characterize the colchicine phospholipid complex(Col-PC),and to study the effect of Col-PC on HSC-T6.Methods:Prepare Col-PC by solvent method,take autumn compound rate as an index,and determine the best process conditions of Col-PC through orthogonal experiment and verification experiment.Differential scanning calorimetry was used to characterize the prepared Col-PC.The inhibitory effect on HSC-T6 cells was investigated by MTT test.Results:The optimal process conditions were that the ratio of colchicine(Col)to phospholipid was 1:3,and the reaction was carried out at 40℃for 1 h.The resulting Col-PC composite rate was 88.83%(RSD%=0.20%,n=3).After preparing the phospholipid complex,the oil-water partition coefficient increased from 1.187 to 1.512.The IC50 of Col-PC and Col to HSC-T6 were 152.7μg/mL and 6.57μg/mL,respectively.Conclusion:The preparation process of Col-PC is stable,reliable,reproducible,and has a good inhibitory effect on HSC-T6 cells,laying the foundation for the research and development of Col-PC's new targeted drug delivery formulations.