水飞蓟宾控释制剂的制备及释放机制研究  

Preparation of silybin controlled-release formulations and study on their release mechanism

作　　者：王立[1] 杨硕[1] 马维阳 刘华石 乔晓溪[1] 张文君[1] 

机构地区：[1]哈尔滨商业大学药学院,黑龙江哈尔滨150076

出　　处：《中草药》2015年第8期1145-1150,共6页Chinese Traditional and Herbal Drugs

基　　金：黑龙江省博士后科研启动金(120575);哈尔滨商业大学研究生创新项目(YJSCX2014-337HSD)

摘　　要：目的综合利用固体分散体、泡腾技术制备水飞蓟宾(SLB)控释制剂,并考察其释药机制。方法采用单因素考察法,将药物体外释放度作为评价指标,确定SLB控释制剂的最佳处方及制备工艺。采用相似因子(f2)法考察所制控释制剂的释药机制。结果 SLB控释片片芯以SLB-聚乙二醇6000固体分散体(1∶2)为主药,以酒石酸和碳酸氢钠为泡腾剂,羧甲基纤维素钠为阻滞剂;包衣处方中醋酸纤维素为包衣材料,聚乙二醇400为致孔剂,所制控释片以零级速率释药。释放机制研究中,致孔剂、阻滞剂和泡腾剂对药物释放行为有显著影响,溶出仪转速及释放介质p H值对药物释放行为无显著影响。结论 SLB控释制剂制备工艺简单,12 h内呈现零级释放(r>0.996 5)。Objective To prepare silybin（SLB） controlled-release formulations with the utilization of solid dispersion and effervescent technology and to study their release mechanism.Methods To determine the optimal formulation and preparation of SLB controlled release formulations was by using single factor test depending on drug release in vitro.The similarity factor method was used to explore the release mechanism of the controlled release formulations prepared.Results The SLB controlled release formulations cores were prepared using SLB-polyethylene glycol 6000 solid dispersion（1：2） as main drug,tartaric acid and sodium bicarbonate as effervescence,sodium carboxymethyl cellulose as blockers.The tablets were prepared using cellulose acetate as coating materials,polyethylene glycol 400 as porogen.SLB controlled release formulations released at a rate of zero-order.In the research on the release mechanism,the coating solution with/without porogen,tablet cores with/without blockers and effervescence had a significant impact on the drug release.On the contrary,the speed of the dissolution tester and the pH value of the release medium had no significant effect on the drug release.Conclusion The preparation process of SLB controlled release formulations is simple.SLB controlled release formulations release with zero-order release in 12 h（r0.996 5）.

关 键 词：水飞蓟宾 控释制剂 固体分散体 泡腾技术 释放机制 相似因子 

分 类 号：R283.6[医药卫生—中药学]