[关键词]
[摘要]
目的 制备荆芥内酯聚乳酸乙醇酸纳米粒,并优化其制备工艺。方法 以粒径、分散度、包封率和载药量为指标,对溶剂挥发法、溶剂扩散法和溶剂-非溶剂法制备荆芥内酯纳米粒进行比较。在单因素考察基础上,采用正交设计法对纳米粒的处方和溶剂-非溶剂法制备工艺进行优化,并考察了4℃和25℃条件下纳米粒溶液的稳定性。结果 溶剂-非溶剂法制备的荆芥内酯纳米粒形态圆整,大小均匀,平均粒径(80.3±1.75)nm,分散度0.0144±0.00625,包封率可达52.53%±0.97%,载药量27.56%±0.91%,显著优于溶剂挥发法和溶剂扩散法,且具有良好的稳定性。结论 溶剂-非溶剂法制备荆芥内酯纳米粒具有工艺简便,粒径和分散度小,包封率和载药量高,重复性好,质量稳定的优点。
[Key word]
[Abstract]
Objective To study schizonepetin polylactic-co—glycolic acid nanoparticles(ST—PLGA—NP) and optimize its formulation.Methods ST—PLGA—NP was prepared by comparing with solvent evapora— tion method,solvent diffusion method,and solvent—nonsolvent method through taking particle diameter, dispersity,encapsulation ratio and loading dose as indexes.The orthogonal design was used for seeking the optimum formulation and preparing technics in solvent—nonsolvent method based on single factor tests. The stability of ST—PLGA—NP,which was obtained with optimum formulation,was observed at 4℃and 25℃.Results The shape of ST—PLGA—NP with solvent—nonsolvent。method was roundness,size was well—distributed,the mean diameter was(80.3±1.75)nm,the dispersxty was 0.014 4土0.006 25,the en— capsulation ratio was t/p to 52.53%士O.97%‘,the ST loading in the nanoparticles was 27.56%±0.91%, which were remarkably higher than other tWO methods,and its stability was good.Conclusion The sol— vent—nonsolvent method used for preparing ST—PLGA—NP has the advantages of simple technicS,small di— ameter and dispersity,higher encapsulation ratio and loading dose,and good repeatability and stability.
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[基金项目]
江苏省高校自然科学研究计划资助项目(02KJA360001);江苏省研究生创新工程资助项目(xm04-76)