叶酸介导的多西他赛脂质体制备、质量控制及稳定性研究

发布时间：2018-07-16 22:07

【摘要】：目的:采用几种不同工艺制备叶酸介导的多西他赛脂质体,建立其质量控制方法并考察其稳定性。方法:将氢化大豆磷脂酰胆碱(HSPC)、叶酸-聚乙二醇2000-磷脂酰乙醇胺(FA-PEG2000-DSPE)及多西他赛以100∶5∶8的比例分别采用3种不同工艺制备脂质体。采用低速离心法测定包封率,动态光散射法测定粒度分布,GC法测定有机溶剂残留。结果:脂质体平均粒径为(155±10)nm,多项分散系数(Pd I)均小于0.20;脂质体包封率均大于95.0%;所制得样品于(25±2)℃条件下放置6个月,各项考察指标均未发生明显变化。结论:采用制备工艺3所制得的样品具有较高的药脂比,该制备工艺可行,质量可控,稳定性良好。体外释放曲线表明脂质体有缓释、靶向及长效作用。
[Abstract]:Objective: to prepare docetaxel liposomes mediated by folic acid by several different processes and to establish its quality control method and investigate its stability. Methods: hydrogenated soybean phosphatidylcholine (HSPC), folic acid peg 2000- phosphatidyl ethanolamine (FA-PEG2000-DSPE) and docetaxel were prepared by 3 different processes, respectively, with the ratio of 100: 5: 8. The encapsulation efficiency was measured by low velocity centrifugation, the particle size distribution was measured by dynamic light scattering, and residual organic solvents were determined by GC method. The results showed that the average particle size of liposomes was (155 + 10) nm, Pd I was less than 0.20, the encapsulation efficiency of liposomes were more than 95%, and the samples were placed at (25 + 2) C for 6 months and all the inspection indexes Conclusion: the sample prepared by the preparation process 3 has a high ratio of drug to fat. The preparation process is feasible, the quality is controllable and the stability is good. The release curve in vitro shows that the liposome has sustained release, targeting and long-term effect.
【作者单位】：江苏省中医院;江苏奥赛康药业股份有限公司;
【分类号】：R943

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