水飞蓟素纳米结晶微丸的表征及稳定性考察

Characterization of Silymarin Nanocrystal Pellets and Investigation of Its Stability

摘要:

目的：制备水飞蓟素纳米结晶微丸并表征其性质、考察其稳定性。方法：采用流化床喷雾干燥技术制备水飞蓟素纳米结晶微丸，通过激光粒度法，紫外光谱法（UV），差示扫描量热法（DSC），红外光谱法（FT-IR）及X-射线衍射法（XRD）对其进行表征，并考察水飞蓟素纳米结晶微丸的初步稳定性（高温、高湿、光照试验）。结果：水飞蓟素纳米结晶微丸再分散后平均粒径（251.6±3.8）nm，多分散指数0.184±0.015。通过UV和FT-IR分析显示药物的化学结构未发生改变，DSC和XRD分析显示药物以无定型或分子状态分散于载体中；分别在60℃，相对湿度75%和照度（4 500±500）Lux的条件下，水飞蓟素纳米结晶微丸外观性状、再分散性能、水飞蓟素含量及溶出度均未发生明显变化。结论：水飞蓟素纳米结晶微丸释药快速、稳定性良好，有望进一步制成口服固体制剂，为水飞蓟素的应用与推广提供参考。

Abstract:

Objective: To prepare silymarin nanocrystal pellets and rsearch for its characterization and stability test. Method: Silymarin nanocrystal pellets were prepared by fluid-bed spray drying technology and characterized by laser particle size analysis,ultraviolet spectroscopy (UV),infrared spectroscopy (FT-IR),differential thermal analysis (DSC) and X-ray diffraction (XRD).Preliminary stability were investigated (high temperature,high humidity and light test). Result: Average particle size of silymarin nanocrystal pellets was (251.6±3.8) nm,and the polydispersity index (PDI) was 0.184±0.015.The chemical structure of silymarin did not change by the analysis of UV and FT-IR.Silymarin was dispersed in carrier with an amorphous or molecular state.Under the conditions of 60℃,relative humidity of 75% and light irradiation of (4 500±500) Lux,the appearance,redispersion,content of silymarin and dissolution rate of nanocrystal pellets were not changed obviously. Conclusion: Silymarin nanocrystal pellets offers rapid drug release and good stability,which is expected to be further developed into oral solid preparations.