通脉复方微丸多元释药系统中川芎酚酸速释单元的制备工艺研究

Preparation Technology of Chuanxiong Phenolic Acid Fast Release Unit in Multi-drug Delivery System of Tongmai Compound Micro-pellets

目的:优选通脉复方微丸多元释药系统中川芎酚酸速释单元的处方和制备工艺。方法:采用单因素试验,以微丸圆整度为指标,考察润湿剂种类与用量、载药量、微粉硅胶用量;以累积溶出百分率为指标,考察崩解剂种类、崩解剂用量。以微丸的圆整度和收率的综合评分为指标,以挤出频率、滚圆频率、滚圆时间为考察因素,采用正交试验优选挤出滚圆法制备工艺。结果:川芎酚酸速释微丸处方总量以50g计算,主药20g,微粉硅胶2g,微晶纤维素26g,崩解剂为羧甲基淀粉钠2g,润湿剂为1%CaCl223mL。采用挤出滚圆法制备,其挤出频率20Hz,滚圆频率50Hz,滚圆时间6min。结论:优选工艺合理,制得的制剂稳定,为通脉复方微丸多元释药系统的制备奠定了基础。

OBJECTIVE：To optimize the formula and preparation technology of Chuanxiong phenolic acid fast release unit in Tongmai compound micro-pellets.METHODS：The type and amount of wetting agent,drug-loading amount,amount of silica gel superfine powder were investigated by single factor test with roundness of micro-pellets as index.The type and amount of disintegrant were investigated with the percentage of accumulative dissolution as index.The extrusion spheronization preparation technology was optimized by orthogonal design with frequency of extrusion,frequency of spheronization and time of spheronization as factors using roundness and yield of micro-pellets as index.RESULTS：The total dose of the formula of Chuanxiong phenolic acid fast release micro-pellets was calculated as 50 g：principal agent of 20 g,silica gel superfine powder of 2 g,MCC of 26 g,CMS-Na of 2 g as disintegrant,1% calcium chloride of 23 mL as wetting agent.Extrusion spheronization method was applied with extrusion frequency of 20 Hz,spheronization frequency of 50 Hz and spheronization time of 6 min.CONCLUSION：The optimal process is rational and the preparation is stable,and it lays a foundation for multi-drug delivery system of Tongmai micro-pellets.