稳定的新型雷贝拉唑钠肠溶微丸  

A new stable rabeprazole sodium enteric-coated pellets

作　　者：顾鑫[1] 邓盛齐[1] 张亦斌[1] 李楠[1] 陶静[1] 郑林[1] Gu Xin Deng Sheng-qi Zhang Yi-bin Li Nan Tao Jing Zheng Lin(Chengdu Engineering Research Center of Innovative Antibiotics, Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu 610052)

机构地区：[1]成都抗生素创制工程技术研究中心,四川抗菌素工业研究所,成都大学,成都610052

出　　处：《中国抗生素杂志》2016年第12期935-941,共7页Chinese Journal of Antibiotics

基　　金：四川省科技计划应用基础计划(No.2015JY0031)

摘　　要：目的制备在肠道内更稳定的可释放两次的雷贝拉唑钠。方法用挤出滚圆法制备雷贝拉唑钠载药微丸丸芯并优化其处方及工艺。载药丸芯包裹隔离层后分别包裹两种肠溶层,制成雷贝拉唑钠肠溶微丸,混合后对释放度和稳定性进行测定。结果载药丸芯处方为10%无水碳酸钠,10%甘露醇,20%雷贝拉唑钠,20%低取代羟丙基纤维素,40%微晶纤维素,以5%羟丙基甲基纤维素的水-乙醇(65:35,W/W)溶液为黏合剂。以欧巴代胃溶型包衣液为隔离层,增重8%,欧巴代肠溶型94系列和尤特奇S100包衣材料为肠溶层,增重15%和20%,得到的微丸含量为97%。混合微丸在p H6.8的磷酸盐缓冲液中60min释放度为40%,120min释放度为70%,在p H8.0的三羟甲基氨基甲烷缓冲液中60min释放度大于80%,且较为稳定。结论成功制备了雷贝拉唑钠肠溶微丸,可在更稳定的p H环境下释放,并具有潜在的两次释放的特征。Objective To prepare stable rabeprazole sodium emetic-coated pellets with the capability of dual release. Methods The drug loaded cores of pellets were prepared by extrusion-spheronization. The formulation and production technology were then optimized. The cores were coated with isolated layer and two kinds of enteric layer respectively to prepare rabeprazole sodium enteric-coated pellets. Finally, the two kinds of pellets were mixed, and the release rate and stability were measured. Results The pellet cores contained 10% of Na2CO3, 10% ofmannitol, 20% of rabeprazole sodium, 20% of L-HPC, 40% of MCC, and 5% of HPMC E5 solution with water/ethanol （65：35, W/W） as the adhesive. Cores were then coated with Opadry （gastric） with 8% weight gain as an isolated layer, and Opadry （enteric, 94 Series） with 15% weight gain and Eudragit S I00 with 20% weight gain respectively as the enteric layer. The content of rabeprazole sodium enteric-coated pellets were about 97%. The release rate of the mixed pellets in pH 6.8 phosphate buffer was about 40% （60min） and 70% （120min）, and more than 80% in pH 8.0 THAM buffer （60min）. The stability test indicated that the enteric-coated pellets were stable. Conclusion Rabeprazole sodium enteric- coated pellets were prepared. The pellets were stable and with potential dual release behavior.

关 键 词：雷贝拉唑钠 载药丸芯 肠溶微丸 两次释放 

分 类 号：R9[医药卫生—药学]