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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 tablets of iloperidone and investigate its in vitro and in vivo sustained-release effects. Methods Hypromellone was used as a matrix material and carbomer as a blocker to prepare sustained-release tablets of iloperidone. The drug release in vitro was determined by HPLC. Results The optimized prescription consisted of the following components: 3.7% for iloperidone, 50.00% for hydroxypropyl methylcellulose (HPMC K4MCR), 47.499% for mannitol, 971 P for carbomer The fraction was 2.00%, the mass fraction of fine silica gel was 0.188% and the mass fraction of magnesium stearate was 0.313%. The tablet prepared by this prescription showed a release of more than 90% at 24 h and release behavior within p H 1.0 ~ 7.4 Not affected by the p H value, in line with the release of sustained release tablets. Conclusion The sustained-release tablets of iloperidone prepared by this method are stable in vitro and the preparation process is simple and easy to use, which is worthy of popularization.