去甲斑蝥素骨架型缓释微丸的工艺优化

Preparation and in vitro release of sustained-release matrix pellets of norcantharidin

目的:优化去甲斑蝥素骨架型缓释微丸的制备工艺,并考察制剂体外释药特性。方法:采用挤出-滚圆技术制备去甲斑蝥素骨架型缓释微丸,以多因素综合评价指标,正交设计与多元回归分析相结合优化处方工艺。结果:以微晶纤维素(MCC)9.877%、乙基纤维素(EC)-硬脂酸(1∶1.5)、黏合剂1%羟丙甲纤维素(HPMC)13mL,80℃烘干制得的去甲斑蝥素骨架型缓释微丸具有较好的缓释效果。结论:采用挤出-滚圆技术,通过缓释材料制备的去甲斑蝥素骨架型缓释微丸,其体外释药缓慢、持续、平稳。

OBJECTIVE To prepare norcantharidin（NCTD） sustained-release pellets and investigate the in vitro drug release mechanism. METHODS Extrusion-spheronization method was used to prepare pellets. The effects of process variables and formulation variables on pellets preparation and drug release were investigated. RESULTS The main factors affecting the release rate were the type of material applied and the temperature of drying. Release of the drug from pellets was in accordance with Higuchi equation. CONCLUSION The method and the formulation are successful in providing slow and steady release of NCTD from sustained-release pellets.