王金凤;王芳;赵楠;杨翠燕;王国玉;魏颖;张文雅;
WANG Jin-feng;WANG Fang;ZHAO Nan;YANG Cui-yan;WANG Guo-yu;WEI Ying;ZHANG Wen-ya;208th Hospital of People's Liberation Army;

• 1:中国人民解放军第二〇八医院

摘要(Abstract)：

研究鸢尾苷元胃内漂浮型缓释片的制备工艺及释放机制。采用羟丙基甲基纤维素(HPMC_(K15M))、交联聚乙烯吡咯烷酮(PVPP)、十八醇、碳酸氢钠为辅料,湿法制粒压片,以体外漂浮性能和体外释放性能为考察指标,采用正交实验设计对处方进行筛选与优化。优化的处方为鸢尾苷元33.3%、HPMCK15 M16.7%、PVPP 20.0%、十八醇13.3%、碳酸氢钠5%、预胶化淀粉10.7%。制得的片剂在人工胃液中10 s内起漂,体外持续漂浮时间>12 h;10 h累积释放度在70%以上。Ritger-Peppas方程拟合分析表明,该缓释片有药物扩散和骨架溶蚀双重作用。鸢尾苷元胃内漂浮型缓释片外观与可压性良好,且具有良好的漂浮性能和释药特征。
To investigate the preparation technology and release mechanism of tectorigenin intragastric floating sustained-release tablets. The tablet was produced by wet granulation compression method,with hydroxypropyl methyl cellulose( HPMCK15 M),cross-linked polyvinyl pyrrolidone( PVPP),octadecanol and sodium bicarbonate as excipient. The prescriptions were screened and optimized by orthogonal experimental design with in vitro floating capacity and drug release characteristics as the evaluation indexes. The optimization results were as follows: tectorigenin 33. 3 %,HPMCK15 M16. 7 %,PVPP 20. 0 %,octadecanol 13. 3 %,sodium bicarbonate 5 %,and starch gel 10. 7 %. The prepared tablet can be floated within 10 s in the artificial gastric juice,lasting for 12 h in vitro,with a cumulative release rate of 70 % in 10 h. The analysis of Rritger-Peppas equation showed that the sustained-release tablet had two advantages of both drug diffusion and skeleton dissolution. The tablet had good appearance and compressibility,as well as favorable floating capacity and drug release characteristics.

关键词(KeyWords)： 鸢尾苷元;胃漂浮片;体外释放度;体外漂浮性
tectorigenin;gastric floating tablets;in vitro release;in vitro floating performance

Abstract:

Keywords:

基金项目(Foundation): 吉林省科技发展计划项目(20140204040YY)

作者(Authors): 王金凤;王芳;赵楠;杨翠燕;王国玉;魏颖;张文雅;
WANG Jin-feng;WANG Fang;ZHAO Nan;YANG Cui-yan;WANG Guo-yu;WEI Ying;ZHANG Wen-ya;208th Hospital of People's Liberation Army;

DOI: 10.19540/j.cnki.cjcmm.20161222.030

参考文献(References)：

• [1]国家中医药管理局中华本草编委会.中华本草.第4卷[M].上海:上海科技出版社,1999:619.
• [2]田代华.实用中药辞典.下卷[M].北京:人民卫生出版社,2002:1388,1897.
• [3]王胜鹏,陈美婉,王一涛.葛花化学成分和药理活性研究进展[J].中药药理与临床,2012,28(2):193.
• [4]王金凤,杨翠燕,张艳萍,等.鸢尾苷对高脂血症大鼠血清脂质的影响[J].基础医学与临床,2010,30(9):925.
• [5]Thinlakarathna S H,Rupasinghe H P.Flavonoid bioavailability and attempts for bioavailability enhancement[J].Nutrents,2013,5(9):3367.
• [6]赵强,陈建明.胃滞留缓释片的研究进展[J].华西药学杂志,2012,27(6):718.
• [7]王金凤,魏颖,王芳,等.HPLC法测定葛花提取物中4种异黄酮类化合物的含量[J].中国药师,2014,17(9):1496.
• [8]杜倩,印晓星,汤道权,等.银杏叶提取物胃漂浮滞留缓释片的制备及其体外释放度评价[J].中国实验方剂学杂志,2012,18(22):25.
• [9]杨立平,邓桂明,欧阳荣.乌药胃内漂浮片的制备及体外释放研究[J].中南药学,2010,8(7):493.
• [10]E M Hansuld,L Briens.A review of monitoring methods for pharmaceutical wet granulation[J].Int J Pharm,2014,472(1):192.