肝靶向氧化苦参碱毫微粒的制备工艺优化

Preparation Technology Optimization of Liver-targeted Oxymatrine Nanoparticle

[目的]优选氧化苦参碱聚氰基丙烯酸正丁酯毫微粒(OM-PBCA-NP)的制备工艺。[方法]以可生物降解的氰基丙烯酸正丁酯为聚合材料,采用乳化聚合、一步法载药制备OM-PBCA-NP;以包封率和载药量为评价指标,通过单因素试验初选、正交设计法精选,优化制备工艺;以RP-HPLC法测定氧化苦参碱含量。[结果]按优化工艺条件,制得载药毫微粒:平均粒径118.3nm,分布范围90～130nm,载药量16.9%,包封率72.7%,RSD1.23%(n=5)。[结论]优化筛选后的处方工艺稳定可行,可为开发OM-PBCA-NP新剂型提供参考。

[ Objective ]The research aimed to optimize the preparation technology of oxymatrine-polybutylcyanoacrylate-nanoparticles. [Method ] OM-PBCA-NP was prepared by emulsion polymerization and one-step drug method with biodegradable butylcyanoacrylate for polymer materials. The procedure was optimized by single factor test and uniform design test with the ebedding ratio and drug loading as the test standard. [Resuh] OM-PBCA-NP was prepared by this optimum conditions： the mean diameter of the nanoparticles was 118.3 nm, the range of distribution was 90 - 130 nm, the mean drug loading was 16.9% and the mean ebedding ratio was 72.7 % , RSD was 1.23 % （ n = 5 ）. [ Conclusion ] The prescription of the screening process optimization was practicable, the reference was provided by the development of OM-PBCA-NP new dosage form.