摘要
目的制备酒石酸美托洛尔延迟起释缓释微丸;研究该制剂的体外释放影响因素。方法采用挤出滚圆法制备含药丸芯,以丙烯酸树脂（Eudragit NE 30D）为内层包衣材料,乙基纤维素与丙烯酸树脂（Eudragit L100）的混合膜材为外层包衣材料制备延迟起释缓释微丸。通过改变内层包衣质量增加、外层包衣质量增加及外层包衣液中乙基纤维素与Eudragit L 100的质量比来达到一定时滞后缓慢释放药物的目的。考察了处方因素和溶出条件对体外释放度的影响。结果制得时滞为4 h,4、6、10、14 h的累积释放量分别为〈10%、20%-35%、50%-70%、≥75%的延迟起释缓释微丸。结论内层包衣质量增加、外层包衣液中乙基纤维素与Eudragit L100的比例及外层包衣质量增加对延迟起释缓释微丸的释药时滞和释药速率具有显著影响,药物的体外释放情况不受溶出转速和溶出装置的影响。
Objective To prepare metoprolol tartrate delayed-onset sustained-release pellets and investigate the influence factors in vitro.Methods The metoprolol tartrate pellets prepared by extrusion-spheronization technology were coated with EudragitNE 30D as the inner coating layer and EC-EudragitL 100 as the outer coating layer.The factors including formulation and dissolution conditions,which influenced the release behavior of metoprolol tartrate delayed-onset sustained-release pellets,were studied.Results After the lag time of 4 h,the drug release from metoprolol tartrate delayed-onset sustained-release pellets was more than 80% within 14 h.Conclusions The coating levels of inner layer and outer layer and the different ratios between EC and EudragitL 100 of outer layer can influence the release behaviors significantly.The rotating speed and dissolution apparatus have little influence on the release behaviours.
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2011年第1期12-15,64,共5页
Journal of Shenyang Pharmaceutical University
关键词
酒石酸美托洛尔
延迟起释
缓释
微丸
体外释放
metoprolol tartrate
delayed-onset
sustained-release
pellet
in vitro release
作者简介
余超（1985-），女（汉族），四川乐山人，硕士研究生，E-marlyuchaoxiaomao@sina．com
程刚（1963-），男（汉族），辽宁康平人，教授，博士，主要从事缓控释制剂和生物药剂学研究，Tel．024-23986326，E-mail chenggang63@hotmail．com。
