生物测定法在丹参亲水凝胶骨架片体外释放评价中的应用研究  

Study on application of bioassay method in drug-release evaluation in vitro of Salvia miltiorrhiza hydrophilic gel matrix tablets

作　　者：李东影[1,2,3] 刘晓谦[1,2] 冯伟红[1,2] 王智民[1,2] 易红[1] 孟庆举[1] 

机构地区：[1]中国中医科学院中药研究所,北京100700 [2]中药质量控制技术国家工程实验室,北京100700 [3]天津中医药大学,天津300193

出　　处：《中国中药杂志》2013年第22期3880-3887,共8页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81274079);国家重点基础研究发展计划(973)项目(2012CB724000);国家"重大新药创制"科技重大专项(2012ZX09103201-009;2012ZX09103201-027)

摘　　要：该研究探讨生物活性测定法在中药缓控释制剂评价中应用的适宜性,建立一种快速的多组分制剂体外释药评价方法,用表征总体行为的生物活性测定法代替目前单一成分的药物释放度测定法,以更好地指导缓控释制剂处方设计。通过HPLC测定不同溶出介质,不同释药速率及成分间不同配伍比例的丹参亲水凝胶骨架片中各有效成分(丹酚酸B、原儿茶醛、迷迭香酸)的累积释放度及紫外分光光度法测定释放液的抗氧化活性,对药物各成分经时曲线与总抗氧化活性经时曲线之间的相关性进行评价。发现各成分的释放曲线与抗氧化活性经时曲线的相关系数r均大于临界r=0.898(P<0.001)。说明3个酚酸类成分的体外释放曲线与总的抗氧化活性经时曲线有很好地相关性,用生物活性测定方法代替成分体外溶出,用于制剂质量评价及处方设计具有可行性,且该法还具有简单、快捷的特点。To investigate the feasible application of the bioassay method in the evaluation of traditional Chinese medicine sus- tained-release preparations, develop a rapid drug-release evaluation method in vitro for multi-component preparations, and replace the biological activity determination method characterizing the overall behavior with the existing drug-release evaluation method for single component, in order to give better instruction for sustained-release preparations. HPLC was adopted to determine dissolution media, drug releasing rates, and accumulative releasing of active ingredients （ salvianolic acid B, protocatechuic aldehyde and rosmarinic acid） of Salvia Miltiorrhiza hydrophilic gel matrix tablets. The ultraviolet spectroscopy was adopted to determine the antioxidant activity of release media, and evaluate the correlation between the drug-time curve of various drug components and the drug-time curve of the total antioxidant activity. The correlation coefficient between the drug-release curve of various components and the drug-time curve of the total antioxidant activity was higher than the critical value r 0. 898 （P 〈 0. 001 ）. This indicated that the drug-release curve of the three phenolic acids and the drug-time curve of the total antioxidant activity had a good correlation in different conditions, such as dis- solution media, release rates and component ratios. The bioassay method for determination was feasible, simple and convenient for preparation quality evaluation and prescription design in the place of in vitro dissolution.

关 键 词：生物测定法 体外释药 抗氧化活性 亲水凝胶骨架片 多组分制剂 丹参 

分 类 号：R283[医药卫生—中药学]