【摘要】 目的制备布地奈德肠溶缓释微丸,并对其体外释药特性和大鼠灌胃后各肠段内容物中药物残余量进行比较研究。方法采用转篮法对制备的布地奈德肠溶缓释微丸进行体外释放度试验,比较微丸在不同释放介质中的释放曲线;测定微丸在大鼠灌胃后各肠段内容物中药物的残余量,并与对照制剂进行比较。结果试验组和对照组微丸在0.1 mol·L^-1HCI溶液中2h和PBS 6.8中10 h的释药曲线基本重合,f₂相似因子为90.1;在0.1 mol·L^-1HCl溶液12 h的累积释放率均<10%,在PBS 6.0、PBS 6.8和PBS 7.5缓冲液3种介质中12h的释药曲线f₂相似因子分别为54.2、50.3和57.8;两者在大鼠灌胃后2、4、6、8h各肠段残余总量和回结肠残余量的P值均>0.05。结论布地奈德肠溶缓释微丸与对照制剂具有相似的体外释药特性,大鼠灌胃后各肠段药物残余量无显著差异。更多还原

【Abstract】 AIM To prepare enteric-coated sustained-release budesonide pellet and to study its in vitro release profiles,the residue drug amount in various intestine segments of rats after intragastric administration.METHODS The in vitro drug release of budesonide pellets in different media was carried out using basket method compared with Ento- cort^TM EC as control preparations.The residue drug amount in various intestine segments of rats after intragastric adminis- tration was measured by HPLC.RESULTS The f₂ value of release curve of self-made pellets compared with the control preparations in 0.1 mol·L^-1 HCI for 2 h followed by phosphate buffered solution pH=6.8（PBS 6.8）for 10 h was 90.1. The cumulative release percentage of both test and control groups in 0.1 mol·L^-1 HC1 for 12 h was less than 10%.The f₂ value of the budesonide pellets in different media of PBS 6.0,PBS 6.8 and PBS 7.5 was 54.2,50.3 and 57.8 re- spectively.The P value of the residue drug amount in various intestine segments of rats between test and control groups was higher than 0.05.CONCLUSION There are no significant differences in the in vitro release profiles and the residue drug amount in various intestine segments of rats after intragastric administration between the test and control groups.更多还原