天山雪莲亲水凝胶缓释骨架片主要活性成分体外释放影响因素的研究

Influence Factors on the Release of the Main Active Composition of Saussurea involucrate from Gel Sustained-Release Matrix Tablets

目的制备天山雪莲缓释骨架片,考查主要活性成分体外释药的影响因素。方法以羟丙甲纤维素(HPMC)为缓释骨架材料,采用湿法制粒、压片,制备天山雪莲缓释骨架片。测定天山雪莲缓释片中主成分绿原酸、芦丁在不同时间点的释放度,通过对体外释放曲线、2,6,12 h累积释放度的综合评分K值及释放曲线相似因子f2的综合比较,考查2种主成分体外释药的影响因素。结果骨架材料HPMC黏度和填充剂淀粉用量是影响绿原酸、芦丁释药速率的主要因素,HPMC的粒径、黏合剂及制片压力等因素对二者释放的影响不大;微晶纤维素(MCC)可以增加二者后期的释放量。结论 HPMC K15M能有效控制天山雪莲缓释骨架片中2种主成分的释放。

OBJECTIVE To prepare Saussurea involucrate sustained-release tablets and to study influence factors on release of the main active composition of Saussurea involucrate.METHODS The Saussurea involucrate sustained-release tablets was compressed after wet granulating the extracts of Saussurea involucrate with HPMC.Then,the influence factors on release of two main active composition of Saussurea involucrate were investigated by determining release rate of chlorogenic acid and rutin at different time to draw release curve and to calculate K（index which was comprehended with cumulative release at 2,6,12 h,respectively）and f 2（similar factor of release curve）.RESULTS The main influence factors on release rate of two main active composition of Saussurea involucrate were viscosity of HPMC and amount of used starch.The particle diameter of HPMC,adhesive and pressure show no effect on release.The later release amounts of two main active composition were increased by MCC.CONCLUSION The release of two main active composition of Saussurea involucrate could be controlled effectively by selecting HPMC K15M as matrices.