穿心莲总内酯亲水凝胶骨架片制备及体外释药机制研究.docVIP

穿心莲总内酯亲水凝胶骨架片制备及体外释药机制研究 　　[摘要]该实验研究了穿心莲总内酯骨架片的处方工艺及其体外释药行为。通过单因素试验，以不同型号及用量的羟丙甲基纤维素（HPMC）为主要考察因素，以3种内酯成分累积释放度为评价指标，优选出最佳处方，所制缓释片无突释现象，缓释周期14 h。采用零级、一级、Higuchi及Peppas方程判断穿心莲3种内酯类成分的释药机制，结果表明总内酯释放行为符合Higuchi模型，释放机制为骨架溶蚀机制。该法制备的穿心莲总内酯骨架片制备工艺简单易行，具有良好的释放性能。 　　[关键词]穿心莲;总内酯;缓释片;制备;释放 　　[收稿日期]2014-10-15 　　[基金项目]国家重点基础研究发展计划（973 ）项目（2012CB724001） 　　[通信作者]*萧伟，博士生导师，研究员，Tel： （0518E-mail： wzhzh-nj@163.net 　　[作者简介]徐芳芳，E-mail： shannaifen@163.com 　　Preparation of hydrophilic matrix sustained release tablets of total lactones from 　　Andrographis paniculata and study on its in vitro release mechanism 　　XU Fang-fang1，2， SHI Wei1，3， ZHANG Hui2，3， GUO Qing-ming2，3， WANG Zhen-zhong2，3， 　　BI Yu-an2，3， WANG Zhi-min3， XIAO Wei2，3* 　　（1. Nanjing University of Chinese Medicine， Nanjing 210000， China; 　　2. Jangsu Kanion Pharmaceutical Co.， Ltd.， Lianyungang 222001， China; 　　3. State Key Laboratory of New-tech for Chinese Medicine Pharmaceutical Process， Lianyungang 222001， China） 　　[Abstract]In this study， hydrophilic matrix sustained release tablets of total lactones from Andrographis paniculata were prepared and the in vitro release behavior were also evaluated. The optimal prescription was achieved by studying the main factor of the type and amount of hydroxypropyl methylcellulose （HPMC） using single factor test and evaluating through cumulative release of three lactones. No burst drug release from the obtained matrix tablets was observed. Drug release sustained to 14 h. The release mechanism of three lactones from A. paniculata was accessed by zero-order， first-order， Higuchi and Peppas equation. The release behavior of total lactones from A. paniculata was better agreed with Higuchi model and the drug release from the tablets was controlled by degradation of the matrix. The preparation of hydrophilic matrix sustained release tablets of total lactones from A. paniculata with good performance of drug release was simple. 　　[Key words]Andrographis paniculata; tota