托吡酯缓释微丸的制备与体外释放研究  

Preparation and in vitro dissolution study of Topiramate sustained-release pellets

作　　者：何磊[1] 吉顺莉[1] 包瑞 HE Lei;JI Shunli;BAO Rui(Department of Pharmacy,the Affiliated Hospital of Nantong University,Nantong,Jiangsu,226001 P.R.China;School of Pharmacy,Jiangsu University,Zhenjiang,Jiangsu,212013 P.R.China)

机构地区：[1]南通大学附属医院药学部,江苏南通226001 [2]江苏大学药学院,江苏镇江212013

出　　处：《华西药学杂志》2020年第5期491-495,共5页West China Journal of Pharmaceutical Sciences

基　　金：奥赛康医院药学基金(编号:A201818);南通市科技计划项目(编号:MSZ18071);常州四药医院药学科研基金项目(编号:mtyx1820)。

摘　　要：目的制备托吡酯缓释微丸,优化缓释薄膜包衣工艺参数,并评价其与参比制剂体外释药的相似性。方法采用空白丸芯载药技术制备托吡酯载药微丸,再以乙基纤维素作为缓释薄膜包衣材料制备托吡酯缓释微丸;以喷液速度、雾化压力和进风温度作为工艺考察参数,以微丸的包衣效率和黏连率作为评价指标,通过Box-Behnken实验设计优化缓释薄膜包衣的工艺参数。采用f2相似因子法比较自制托吡酯缓释微丸与参比制剂在4种释放介质中释药行为的相似性。结果最优缓释薄膜包衣工艺为:喷液速度为8.0 mL·min^-1,雾化压力为0.4 MPa,进风温度为50℃;在4种释放介质中,自制托吡酯缓释微丸与参比制剂的f2相似因子>50,具有较好的相似性。结论采用最佳包衣工艺参数制备的托吡酯缓释微丸包衣效率较高,黏连率较低;自制托吡酯缓释微丸与参比制剂的体外释药行为相似性较高,有望工业化生产。OBJECTIVE To prepare Topiramate sustained-release pellets by optimizing the coating parameters,and to evaluate the similarity of in vitro dissolution between sustained-release and reference preparation.METHODS Firstly,the Topiramate pellets were prepared by fluid bed coating technology,and then the ethyl cellulose was used as the sustained-release film coating material to prepare Topiramate sustained-release pellets.The spray speed,atomization pressure and inlet air temperature were used as investigation factors,while the coating efficiency and pellets adhesion rate were used as evaluation indexes.Then the coating process parameters were optimized by Box-Behnken experimental design.The in vitro dissolution similarity of homemade Topiramate sustained-release pellets and the reference preparation in four dissolution media were compared based on the f2 similarity factor.RESULTS The optimal process parameters of sustained-release film coating were as follows:spray speed of 8.0 mL·min^-1,atomization pressure of 0.4 MPa,and inlet air temperature of 50℃.The f2 similar factor of the homemade Topiramate sustained-release pellets and the reference preparation in four dissolution media were greater than 50,and had good similarity.CONCLUSION The Topiramate sustained-release pellets prepared by the optimal coating process parameters have higher coating efficiency and lower adhesion rate.The in vitro dissolution of homemade Topiramate sustainease-pellets and the reference preparation have higher similarity,and it is expected to further enlarge production.

关 键 词：托吡酯 缓释微丸 包衣工艺 体外药物释放 包衣效率 黏连率 Box-Behnken实验设计 f2相似因子 

分 类 号：R94[医药卫生—药剂学]