伊潘立酮缓释片的制备及体外释放度检查  

Studies on the preparation of iloperidone sustained-release tablets and its released behavior in vitro

作　　者：周思民[1] 王带媚[1] 白源韬 

机构地区：[1]海南省人民医院药学部,海南海口570311 [2]北京航空航天大学实验学校,北京100000

出　　处：《沈阳药科大学学报》2016年第8期609-615,共7页Journal of Shenyang Pharmaceutical University

摘　　要：目的制备伊潘立酮缓释片,考察其体内体外缓释效果。方法以羟丙甲纤维素为骨架材料,卡波姆为阻滞剂,制备伊潘立酮缓释片;用HPLC法测定药物体外释放度。结果优化后的处方组成：伊潘立酮质量分数为3.750%、羟丙基甲基纤维素（hydroxypropyl methylcellulose,HPMC K4MCR）质量分数为50.00%、甘露醇质量分数为47.499%、卡波姆971P质量分数为2.00%、微粉硅胶质量分数为0.188%、硬脂酸镁质量分数为0.313%,该处方所制得的片剂在24 h释放度大于90%,且释放行为在p H 1.0～7.4内不受p H值影响,符合缓释片的释放要求。结论用本方法制备的伊潘立酮缓释片体外释药平稳,制备工艺简单易行,值得推广。Objective To prepare sustained-release formulation of iloperidone and determine its external release. Methods Iloperidone sustained-release tablets ere prepared ith hydroxypropyl methylcellulose（ HPMC） as matrix material,and carbomeras blockers. The external release of drugas determined by HPLC. Results In the optimal formulation,3. 75%（w） of iloperidone,50. 00%（w） of HPMC K100 MCR,47. 499%（w） of mannitol,2. 00%（w） of carbomer,0. 188%（w） of aerosil and 0. 313%（w） of magnesium stearate ere selected as the main excipients. The release ratio of the optimal formulation as up to 90% in24 h and the p H value of release medium had no significant effects on the release of iloperidone sustained-release tablets. The formulation demonstrated a typical extended release profile in the in vitro test. Conclusions The release of iloperidone dihydrochloride from sustained-release pellets is slow and steady. The preparation process is simple,which is orth further development and application in the clinic.

关 键 词：伊潘立酮 缓释片 羟丙基甲基纤维素 卡波姆 体外释放度 

分 类 号：R94[医药卫生—药剂学]