摘要
目的制备氟比洛芬肠溶微球并考察处方影响因素,测定体外溶出度。方法以Eudragit S100为囊材,采用乳化溶剂扩散法制备氟比洛芬肠溶微球。考察温度、药物与载体的质量比、搅拌速率等对微球外观形态、收率、载药量和包封率的影响。结果 Eudragit S100与药物质量比以4:1混合时可得到成形性较好、表面光滑、均匀圆整、分散性好的氟比洛芬肠溶微球。差示扫描量热法(DSC)分析结果表明,氟比洛芬以无定型分散在载体中,氟比洛芬微球的粒径范围为60～90μm,收率为75%,载药量为7.0%,包封率为31%。氟比洛芬微球在pH值为7.4的磷酸缓冲液中4h药物释放90%。结论用Eudragit S100为囊材,乳化溶剂扩散法适合于氟比洛芬肠溶微球的制备,操作方法简单。
Objective To prepare the enteric microspheres of flurbiprofen,investigate the influencing factors,and to evaluate the release in vitro.Methods The enteric microspheres of flurbiprofen were prepared with enteric polymer Eudragit S100 in one step by quasi-emulsion solvent diffusion method.The formulation of the microspheres,preparation conditions and solvent system were investigated.The microspheres were characterized with regard to their shape,size distribution,recovery and release-profiles in phosphate buffer(pH 7.4).Results When the ratio of the enteric polymer(Eudragit S100)-drug was 4:1,the microspheres are of a very round form with smooth surface and good dispersion.The drug was coated perfectly,and the new phase was generated.The size distribution of microspheres was in the range of 60 ～ 90 μm,the yield of microspheres was 75%,drug loading was 6.8%,and encapsulation efficiency was about 31%.The drug release was rapid in pH 7.4 phosphate buffer,and the cumulative release reached 90%.Conclusion It is easy to produce enteric microspheres with solid dispersion structure by the emulsion solvent diffusion method.
出处
《中国药剂学杂志（网络版）》
2012年第3期50-55,共6页
Chinese Journal of Pharmaceutics：Online Edition
基金
辽宁省科技厅博士启动资金资助项目(20091080)
