摘要
目的制备SM-1小粒径肠溶微丸,并优化其处方,以达到肠溶和便于小动物给药的目的。方法采用流化床空白丸芯上药法,在丸芯表面依次包覆含药层、羟丙基甲纤维素(HPMC)隔离层和丙烯酸树脂(EudragitL30D-55)肠溶层。以载药量、耐酸性及释放度为指标,对SM-1肠溶微丸的处方进行优化。结果隔离层增重8%,肠溶层增重15%的肠溶微丸粒径<450μm(40目筛),圆整度良好,载药量约为20%;在pH为2.0的盐酸溶液中2 h内肠溶衣层薄层完好,药物释放度<4%;在pH为6.8的PBS溶液中,45 min内释放度均>70%。结论采用流化床制备SM-1肠溶微丸工艺可行,重现性好,具有良好的肠溶特性,粒径<380μm,可用于小动物给药。
Objective To prepare and optimize the formulation of SM-1 enteric coated pellets for enteric coating and convenient administration for small animals.Methods SM-1 enteric coated pellets were prepared by fluidized bed.Three separate layers,the drug layer [the barrier layer（HPMC）,and the enteric layer（Eudragit L30D-55）] were coated onto the inert core pellets.The pellets were optimized with the drug loading,acid resistance and drug release as the process parameters.Results The SM-1 enteric-coated pellets containing 8% weight gain of barrier layer and 15% weight gain of enteric layer had good appearance,the drug loading rate was about 20% and the particle size was less than 450 μm.The accumulative release of the pellets in pH 6.8 phosphate buffer solution at 45 min was more than 70%.The accumulative release in pH 2.0 hydrochloric acid at 2 h was less than 4%.Conclusion SM-1 enteric coated pellets preparation with the fluidized bed technology is feasible and replicable.The pellets show satisfactory enteric characteristics with the particle size smaller than 380 μm,suitable for small animals.
出处
《中南药学》
CAS
2013年第5期328-331,共4页
Central South Pharmacy
基金
国家"十二五"重大科技专项资助项目(编号:2012ZX09103101-051)
关键词
SM-1
流化床
肠溶微丸
SM-1
fluidized bed
enteric-coated pellet
