帕利哌酮缓释微丸的处方优化  

Formulation Optimization of Paliperidone Sustained-release Pellets

作　　者：郑林[1] 李黎[1] 尹罡[1] 廖蓉惠 邓盛齐[1] 陶静[1] ZHENG Lin;LI Li;YIN Gang;LIAO Ronghui;DENG Shengqi;TAO Jing(Antibiotics Research and Re-evaluation Key Lab.of Sichuan Province,Sichuan Industrial Institute of Antibiotics,School of Pharmacy,Chengdu University,Chengdu 610052)

机构地区：[1]成都大学药学院,四川抗菌素工业研究所,抗生素研究与再评价四川省重点实验室,四川成都610052

出　　处：《中国医药工业杂志》2023年第2期224-229,共6页Chinese Journal of Pharmaceuticals

基　　金：成都大学实验教学研究与改革项目(cdsyjg2022003)给予资助。

摘　　要：该研究采用挤出滚圆法制备了帕利哌酮丸芯,再用甲基丙烯酸共聚物(Eudragit)包衣制备缓释微丸,并采用正交设计分别优化了载药丸芯和缓释微丸的处方包衣工艺参数。结果表明,采用Eudragit RS30D与Eudragit RL30D作为包衣材料,且Eudragit RS30D占包衣材料总量65%时得到的优化缓释微丸在不同pH介质中的体外释放行为符合一级动力学方程。The paliperidone-loaded pill cores were prepared by the extrusion spheronization process,then the sustained-release pellets were obtained by coating with methacrylic acid copolymer(Eudragit)thin film.The formulation and process parameters of the pill cores and coated pellets were optimized by orthogonal design.The results showed that the in vitro release behavior of the optimal sustained-release pellets coated with the thin film consisted of Eudragit RS30D(which accounted for 65%of the total amount of coating materials)and Eudragit RL30D could be described by first-order kinetic equation.

关 键 词：帕利哌酮 挤出滚圆法 流化床包衣 缓释微丸 体外释放 

分 类 号：R944.9[医药卫生—药剂学]