美沙拉嗪肠溶缓释微丸的制备及体外释放度考察  

Study on the preparation and in vitro dissolution of mesalamine extended-release enteric pellets

作　　者：苏诗娜 吕竹芬 梁超峰 卢克伟 陈燕忠 SU Shina;LYU Zhufeng;LIANG Chaofeng;LU Kewei;CHEN Yanzhong(Key Laboratory of Advanced Drug Delivery of Guangdong Province,Guangzhou 510006,China;Department of Pharmaceutics,Guangdong Pharmaceutical University/Guangdong Provincial Engineering Center of Topical Precise Drug Delivery System,Guangzhou 510006,China;Guangzhou General Pharmaceutical Research Institute,Guangzhou 510240,China)

机构地区：[1]广东省药物新剂型重点实验室,广东广州510006 [2]广东药科大学药学院/广东省局部精准药物递药制剂工程技术研究中心,广东广州510006 [3]广州医药工业研究总院,广东广州510240

出　　处：《广东药科大学学报》2018年第2期127-131,136,共6页Journal of Guangdong Pharmaceutical University

基　　金：广州市科技计划项目(201508010050);2015广东省普通高校创新团队建设项目(2015KCXTD026);2015广东省普通高校特色创新类项目(2015KTSCX075)

摘　　要：目的制备美沙拉嗪肠溶缓释微丸,并考察其体外溶出行为。方法采用微晶纤维素、羟丙甲纤维素(HPMC)K4M和尤特奇~NE30D制备缓释骨架丸芯,以尤特奇~S100和L100为肠溶材料包衣,制备美沙拉嗪肠溶缓释微丸。采用单因素试验,以释放度和相似因子f2为指标筛选处方中尤特奇~NE30D用量、HPMC型号和用量、丸芯干燥条件、包衣材料用量及包衣增重。结果丸芯最优处方为美沙拉嗪213.15 g、微晶纤维素52.50 g、HPMC K4M 7.00 g和尤特奇~NE30D 221.67 g,包衣处方中尤特奇~S100和L100比例为2∶3(质量比),最佳包衣增重为14%。自制制剂和原研制剂在pH6.8磷酸盐缓冲液的体外释放行为相似。结论成功制得美沙拉嗪肠溶缓释微丸,其体外溶出行为与原研制剂相似。Objective To prepare mesalamine extended-release enteric pellets and study its in vitro dissolution.Methods Microcrystalline cellulose(MCC),hypromellose K4M(HPMC K4M)and Eudragit NE30D were used to prepare the extended-release matrix core.Mesalamine extended-release enteric pellets were prepared by using Eudragit S100 and L100 as enteric coating material.Single factor test was used to screen the amount of Eudragit NE30D,the amount of Eudragit S100 and L100,amount of HPMC and weight of coating layer in the formulation by using dissolution rate and the similar factor f 2 as indexes.Results The optimal formulation of mesalamine extended-release matrix core was as follows:Mesalamine 213.15 g,MCC 52.50 g,HPMC K4M 7.00 g,Eudragit NE30D 221.67 g,the ratio of Eudragit S100 and L100 was 2∶3 and the optimum coating weight gain was 14%.The in vitro release of self-made and original preparations was similar in pH6.8 phosphate buffer.Conclusion Mesalamine extended-release enteric pellets have been prepared successfully,and its in vitro dissolution behavior is similar to the original preparations.

关 键 词：美沙拉嗪 肠溶缓释微丸 体外释放度 尤特奇NE30D 

分 类 号：R944.4[医药卫生—药剂学]