罗氟司特片剂的制备及研究  

Preparation,dissolution behavior and intestinal absorption of roflumilast tablets

作　　者：王梦[1] 操锋[1] 平其能[1] 张灿[2] 

机构地区：[1]中国药科大学药剂学教研室,南京210009 [2]中国药科大学新药研究中心,南京210009

出　　处：《中国新药杂志》2014年第14期1696-1702,共7页Chinese Journal of New Drugs

摘　　要：目的:研制与原研制剂具有相似体外溶出行为及肠吸收无显著差异的罗氟司特片。方法:采用湿法制粒压片工艺制备自制片,单因素试验筛选处方。通过比较4种溶出介质(pH 1.2盐酸缓冲液,pH4.5醋酸缓冲液,0.1%SDS-pH 6.8磷酸缓冲液和水)中自制片与原研制剂的溶出行为,评价两者体外溶出行为的相似性。通过大鼠在体肠吸收实验考察黏合剂对于药物吸收的影响。结果:自制片与原研制剂在4种溶出介质中的溶出相似因子f2均大于50。在体肠吸收实验显示2种黏合剂溶液中药物的有效渗透系数无显著性差异(P>0.01)。结论:自制片与原研制剂体外溶出行为相似,黏合剂对药物的大鼠在体肠吸收无显著影响。Objective：To prepare roflumilast tablets with similar dissolution behavior to the marketed tablet,and to investigate intestinal absorption of roflumilast in rats in situ.Methods：The tablets were prepared with wet granulation followed by compression,and the prescription was optimized by the single factor test.The dissolution behaviors of the test tablets and marketed tablets were compared in different media（hydrochloric acid,acetic acid buffer solution,phosphate buffer solution containing 0.1% SDS,and water）.The similarity factor（f2） of dissolution behavior was calculated to evaluate the similarity between test tablets and marketed tablets.The influence of the adhesive for the drug absorption was studied by the in situ single-pass intestinal perfusion（SPIP） experiments in rats.Results：Compared with the marketed tablets,the similarity factor（f2） of dissolution behavior of test tablets in four dissolution media were larger than 50.In both binder solution,there was no significant difference between the effective permeability（Peff） of roflumilast（P 〉0.01）.Conclusion：The dissolution behavior in vitro of test tablets is similar to the marketed tablets,and the adhesive has no influence on the drug intestinal absorption in situ in rats.

关 键 词：罗氟司特 湿法制粒 溶出 在体肠吸收 

分 类 号：R943[医药卫生—药剂学]