穿心莲总内酯亲水凝胶骨架片的制备及体外释药机制研究(1)
[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： (0518)81152337，E-mail： wzhzh-nj@163.net
, http://www.100md.com
[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;
, http://www.100md.com
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.
, http://www.100md.com
[Key words]Andrographis paniculata; total lactones; matrix tablets; preparation; release
doi：10.4268/cjcmm20150115
穿心莲是爵床科植物穿心莲Andrographis paniculata (Burm.f.)Nees的干燥全草或叶，具有清热解毒、消炎、消肿止痛的作用，主要用于治疗细菌性痢疾、尿路感染、急性扁桃体炎、肠炎、咽喉炎、肺炎和流行性感冒等[1]，其主要活性成分为穿心莲内酯、脱水穿心莲内酯和新穿心莲内酯[2];亲水凝胶骨架片是缓释制剂骨架片中的一种，能够降低血药浓度波动，减少给药次数，提高药物疗效，并且制备工艺简单，易投入工业化生产[3-7]，因此本实验制备了穿心莲总内酯亲水凝胶骨架片，并对该制剂的释药行为和释药机制进行了研究[8-11]，以期为穿心莲总内酯新型剂型的开发提供一定的依据。, http://www.100md.com(徐芳芳 石伟 张晖 郭庆明 王振中 毕宇安 王智民 萧伟)
[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： (0518)81152337，E-mail： wzhzh-nj@163.net
, http://www.100md.com
[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;
, http://www.100md.com
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.
, http://www.100md.com
[Key words]Andrographis paniculata; total lactones; matrix tablets; preparation; release
doi：10.4268/cjcmm20150115
穿心莲是爵床科植物穿心莲Andrographis paniculata (Burm.f.)Nees的干燥全草或叶，具有清热解毒、消炎、消肿止痛的作用，主要用于治疗细菌性痢疾、尿路感染、急性扁桃体炎、肠炎、咽喉炎、肺炎和流行性感冒等[1]，其主要活性成分为穿心莲内酯、脱水穿心莲内酯和新穿心莲内酯[2];亲水凝胶骨架片是缓释制剂骨架片中的一种，能够降低血药浓度波动，减少给药次数，提高药物疗效，并且制备工艺简单，易投入工业化生产[3-7]，因此本实验制备了穿心莲总内酯亲水凝胶骨架片，并对该制剂的释药行为和释药机制进行了研究[8-11]，以期为穿心莲总内酯新型剂型的开发提供一定的依据。, http://www.100md.com(徐芳芳 石伟 张晖 郭庆明 王振中 毕宇安 王智民 萧伟)