丹参酮-丹酚酸-三七总皂苷均衡缓释给药系统的研究  

Development of synchronized and sustained release system capsule of Salvia miltiorrhiza and Panax notoginseng

作　　者：张秋燕[1] 李娜[2] 崔翰明[1] 

机构地区：[1]中国中医科学院广安门医院中药研发中心,北京100053 [2]扬子江药业集团南京中药所,江苏南京210049

出　　处：《中国医药导报》2016年第18期131-134,145,共5页China Medical Herald

基　　金：国家重大新药创制专项资助项目(2012zx09102201-006);广安门医院科研专项所级滚动培育项目(2014S 303)

摘　　要：目的研制一种能实现丹参-三七多组分同步均衡缓释给药的系统。方法分别采用骨架溶蚀、固体分散体、脂质体和膜包衣控释技术将总丹酚酸、总丹参酮和三七总皂苷制成具有不同释药特性的微丸,根据其释药速度(速释、迟释和缓释微丸)将不同组分微丸进行组合,计算相似因子(f2),选择释药曲线相似度较高者进行多成分组合,并与普通胶囊对比,实现12 h内同步均衡缓慢释放的组合方式。结果丹酚酸、丹参酮和三七总皂苷的速释丸∶迟释丸∶缓释丸组合比例分别为1∶3∶2、1∶1∶2、2∶3∶5时,丹参酮ⅡA、隐丹参酮和丹酚酸B的释放f_2为52.00,四种三七皂苷和丹酚酸B的释放相似因子为60.96,丹参酮ⅡA、隐丹参酮和三七总皂苷的释放相似因子为57.13,各有效组分的释药曲线相似性较高,释药速率较普通胶囊明显减缓,可实现不同组分同步均衡缓慢释放的设想。结论应用多元微丸释药系统将性质差异较大的多类组分分别制成具有不同释药特性的微丸,并按一定方式组合,可实现多组分同步均衡缓慢释放,为多种不同组分提供一种实现缓释的新方法。Objective To develop a synchronized and sustained release system of Salvia miltiorrhiza and Panax notoginseng. Methods Matrix erosion, solid dispersion system, liposome and membrane controlled-release technology,Salvianolic acid were used. Tanshinone and Panax Notoginseng Saponin were prepared to micro-pill with different drug release rate, such as quick-release, delayed-release and sustained-release pills. Then the micro-pills of each component were combined according to its release rate, and the similarity factor（f_2） were calculated and the combinations of the similar release curve were selected to combine again. Compared with general capsules, the suitable combination could be achieved a synchronous equilibrium release system for the release within 12 hours for each target ingredient. Results The proportion of quick release, delayed and slow release micro-pill were 1 ∶3∶2 for Salvianolic acid, 1∶1∶2 for Tanshinone and 2∶3∶5 for Notoginseng Saponins, the obtained release f2 from Tanshinone compared with Salvianolic acid was52.00, the f2 from Salvianolic acid compared with Panax Notoginseng Saponins was 60.96, the f2 from Tanshinone compared with Panax Notoginseng Saponins was 57.13. The drug release curve of each effective component was similar, and the release rate was slow down significantly compared with the ordinary capsule. Conclusion The micro-pill have different release rate that can achieve the purpose of multi-component release synchronously, balanced, and delayed by multiple unit micro-pill release system, which provide a new method for realizing slow release system.

关 键 词：丹参总酚酸 总丹参酮 三七总皂苷 同步均衡释药系统 缓控释 

分 类 号：R914.1[医药卫生—药物化学]