舒胸滴丸的处方筛选及药效学研究  

Formulation optimization and pharmacological research of Shuxiong dripping pills

作　　者：杨丽丽[1] 刘康[1] 黄罗生[1] 黄芳 

机构地区：[1]中国药科大学,南京211198

出　　处：《海峡药学》2012年第8期35-39,共5页Strait Pharmaceutical Journal

基　　金：国家科技重大专项2009ZX09103-344

摘　　要：目的采用均匀设计法对舒胸滴丸的处方进行优选,并对优化组方进行初步的药效学研究。方法舒胸滴丸5种组分分别是川芎嗪、阿魏酸、川芎挥发油、三七总皂苷及红花中间体。以离体主动脉环舒张率(主要优化参数)、抗血小板聚集率(辅助优化参数)为考察指标,采用均匀设计法筛选最优组方。采用异丙肾上腺素(ISO)制备小鼠心肌缺血损伤模型、结扎左冠状动脉造成大鼠急性心肌缺血模型,观察优化组方对小鼠、大鼠心肌损伤后血清磷酸肌酸激酶(CK)和乳酸脱氢酶(LDH)水平的影响,对大鼠心电图变化和心肌组织形态学的影响。结果优化组方的组成为川芎嗪0.32μg.mL-1;阿魏酸1.2μg.mL-1;川芎挥发油67μL.L-1;三七总皂苷4μg.mL-1;红花中间体400μg.mL-1。优化组方可使去甲肾上腺素预收缩的离体主动脉环舒张率为98.43%,抗血小板聚集率为9.48%;与模型组相比,优化组方显著降低心肌缺血小鼠、大鼠血清的CK、LDH水平,显著降低缺血引起心电图T波升高,明显改善冠脉结扎致心肌细胞形态学变化,肌纤维排列较整齐。结论舒胸滴丸优化组方对扩张血管和抗血小板聚集作用显著有效,且对异丙肾上腺素诱发的小鼠心肌缺血、结扎冠脉引发的大鼠急性心肌缺血的损伤有保护作用。OBJECTIVE To optimize the formulation of shuxiong dripping pills（SXDP） by uniform design,and investigate the preliminary pharmacological action of the optimized prescription.METHODS SXDP was made up of Ligustrazine,ferulaic acid（FA）,Chuanxiong naphtha,total saponins of Panax notoginseng（PNS） and intermediates of Honghua（Flos Carthami）.The relaxation of isolated aortic rings and inhibition of platelet aggregation were used to evaluate the effect of different mixtures.Uniform design and correlation analysis were adopted for the formulation optimization.The myocardial ischemia injury model was induced by subcutaneous injections of isoproterenol in mice,and ligating the left anterior descending branch of coronary artery in rats,the activities of lactate creatine phosphskinase（CK） and dehydrogenase（LDH） in serum were assayed by using commercial kits,then electrocardiogram changes and the morphology of cardiac tissue were observed.RESULTS The optimal formulation of SXDP was Ligustrazine 0.32μg·mL-1,FA 1.2μg·mL-1;Chuanxiong naphtha 67μL·L-1;PNS 4μg·mL-1 and intermediates of Honghua（Flos Carthami） 400μg·mL-1.In in-vitro test,after treatment of the optimized formulation,the relaxation rate of isolated aortic rings was 98.43%,and the inhibition rate of platelet aggregation was 9.48%.In in-vivo experiment,compared with model group,the activities of serum CK and LDH were dromatically decreased by SXDP.The T wave of SXDP group was much lower than that of control group.SXDP can improve the morphological changes of ischemic myocardial cells,the cardiac muscle fibers were arranged in order.CONCLUSION The optimized prescription of SXDP had particular function on the relaxation of blood vessels and anti-platelet aggregation and effect on myocardial ischemia injury induced by isoproterenol in mice and ligating the left anterior descending branch of coronary artery in rats.

关 键 词：舒胸滴丸 均匀设计 动脉环舒张 抗血小板聚集 心肌缺血 

分 类 号：R969[医药卫生—药理学]