栀子抗血栓缓释片的研制  

The development of sustained-release tablets of antithrombotic gardenia

作　　者：李芳[1] 张海燕[1,2] 王欣[1] 胡鹏翼[1] 雷婷婷[1] 杨明[1,3] 

机构地区：[1]江西中医学院现代中药制剂教育部重点实验室,南昌330004 [2]西南交通大学材料先进技术教育部重点实验室,成都610003 [3]成都中医药大学,成都611137

出　　处：《中国新药杂志》2013年第20期2369-2373,2404,共6页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2009ZX09310-005);江西省重大科技专项(530219)

摘　　要：目的：制备栀子抗血栓亲水凝胶骨架缓释片，建立其总环烯醚萜苷体外释放度的紫外测定方法，并考察其体外释药机制。方法：以总环烯醚萜苷体外释放度为评价指标，采用单因素试验进行处方及工艺筛选，正交试验进行优化，并进行缓释片体外释放度曲线拟合。结果：供试品及栀子苷对照品在238nm均有最大吸收，在6．51～32．55mol·L-1浓度范围内与吸光度值呈良好的线性关系（A=0．024C＋0．007，r=0．999）。溶出方法、HPMC规格及用量对释药速率有显著影响，栀子缓释片的体外释药特征符合一级动力学，释药机制符合Ritger—Peppas的非Fick’s扩散，即扩散与骨架溶蚀2种机制协同作用的结果。结论：该缓释片制备工艺简单，体外释放度测定方法简便、快速，其体外缓释效果较好。Objective：To prepare a sustained release tablet formulation for antithrombotic gardenia,establish a UV method to measure the in vitro release of the total iridoid, and investigate the in vitro release mechanism. Methods：Using release rate of total iridoid glycosides in vitro as the evaluation indicator, the prescription and process were screened by single factor experiment and optimized by orthogonal experiment,and the in vitro release curve of the sustained-release tablets was fitted. Results：The sample and geniposide reference substance had maximum absorption at 238 nm. The concentration had a good linear relationship with the absorbance value in the range 6.51 -32.55 mol. L-1. Dissolution method and the specifications and dosage of HPMC had significant effect on the drug release rate. The in vitro release characteristics of gardenia sustained-release tablets was in line with first order kinetics,and the release mechanism corresponded with the Ritger-Peppas＇ non-Fick＇s diffusion, which was the result of the synergy of the two mechanisms of diffusion and skeleton dissolution. Conclusion：The process for preparation of sustained release tablets of gardenia is simple and feasible. The tablets show good sustained release effect in vitro.

关 键 词：栀子提取物 总环烯醚萜苷 缓释片 释放度 释药机制 

分 类 号：R283.64[医药卫生—中药学] R943.41[医药卫生—中医学]