舒胸片有效成分组微乳化剂型改造后的药效作用特点

Pharmacodynamic study of microemulsion Shuxiong Tablet

目的:经由舒胸片(三七、红花和川芎)有效成分组与其微乳化剂型的药效学比较,探讨微乳化剂型的药效特点。方法:给予舒胸片有效成分组及其微乳剂型,通过小鼠角叉菜胶足跖肿胀试验、小鼠凝血试验、大鼠动静脉旁路血栓试验、大鼠血瘀证模型试验、大鼠心肌缺血再灌注模型试验,比较两种药物的抗炎、抗凝血、抗血栓形成、抗血小板聚集及心肌保护作用疗效。结果:舒胸片有效成分组及其微乳化剂型均能降低角叉菜胶引起的小鼠足趾肿胀度,降低其足局部炎症组织中前列腺素-2(PGE-2);延长凝血时间;抑制血栓生成;抑制由ADP诱导的血小板聚集;抵抗心肌缺血,使心肌缺血引起的肌酸激酶(CK)、乳酸脱氢酶(LDH)、脂质过氧化产物丙二醛(MDA)含量降低,超氧化物岐化酶(SOD)活性升高,心肌梗死面积减少,肿瘤坏死因子(TNF-α)含量降低且基因表达减少,核因子-κβ表达降低。结论:舒胸片在相同给药剂量时,微乳化剂型的以上各项药效及生化指标明显好于有效成分组。这可能与微乳化剂型促进有效成分的吸收有关。

AIM：To compare the pharmacodynamic characteristics of Shuxiong Tablet（Radix et Rhizoma No-toginseng,Flos carthami and Rhizoma Chuanxiong） between Shuxiong microemulsion（SME） and Shuxiong effec-tive compounds group（SECG）.METHODS：SME and SECG in the equipotent dose were applied to experiments,including carrageenan-induced paw edema,clotting time in mice,thrombus in arteriovenous shut,anti-platelet ag-gregation in blood stasis rat and using ischemia-reperfusion rat model,to observe their effects on anti-inflammation,anti-coagulation,anti-thrombotic,anti-platelet aggregation and protect myocardial ischemia-reperfusion injury.RESULTS：SME and SECG both could reduce the mice paw swelling degree and the prostaglandin-2 level in the tissue,prolong the coagulation time,inhibit thrombosis and platelet aggregation induced by ADP.They also could protect myocardial ischemia-reperfusion injury：lower the creatine kinase,the lactate dehydrogenase and the lipid peroxidation product malondialdehyde,higher the superoxide dismutase,lessen the myocardial infarct size,decrease the serum tumor necrosis factor-α（TNF-α）.In addition,SME and SECG could down-regulate the expression of TNF-α mRNA and nuclear factor kappa β protein in the myocardial ischemia.CONCLUSION：The results show that the various pharmacodynamics indexes of SME are much better than that of SECG in the equipotent dose that might relate to the improvement in the absorption of effective compounds.