基于机械粉碎法的穿心莲内酯复合粒子制备及其溶出度研究

Study on preparation of andrographolide composite particles based on mechanical crushing method and its dissolution

目的:制备穿心莲内酯复合粒子,并对其粒子结构与溶出度进行评价。方法:采用机械粉碎法制备穿心莲内酯与聚乙二醇(PEG)6000复合粒子;通过扫描电镜(SEM)与差示扫描量热仪(DSC)表征复合粒子的结构;采用接触角测定仪测定其接触角;考察其体外溶出曲线。结果:穿心莲内酯与PEG 6000形成相互包覆的复合粒子结构,且穿心莲内酯结晶度下降。以水为测定液,穿心莲内酯与PEG 6000复合粒子粉体的接触角明显小于其原粉与物理混合物,且复合粒子的体外溶出速率明显优于其原料、超微粉及其物理混合物。结论:基于机械粉碎的穿心莲内酯复合粒子能显著提高穿心莲内酯的体外溶出度。

Objective： To prepare andrographolide composite particles, and evaluate their particle structure and dissolution. Method： The mechanical crushing method was adopted to prepare andrographolide and polyethylene glycol （PEG） 6000 composite particles. The structures were characterized by the scanning electron microscope （SEM） and the differential scanning calorimeter （DSC）. The contact angles were determined by the contact angle analyzer. The in vitro dissolution curve was detected. Result： Andrographolide and PEG 6000 gave rise to coated composite particle structures, with the decrease in the crystallinity of andrographolide. The in vitro dissolution rate of composite particles was significantly obvious than that of its raw materials, uhrafine powder and their physical mixtures. Conclusion： Andrographolide composite particles based on the mechanical crushing method could notably enhance the in vitro dissolution of andrographolide.