目的研究氧化苦参碱-甘珀酸钠复合物的制备方法及其药理活性。方法分别配制氧化苦参碱和甘珀酸钠溶液,将两种溶液按比例混合,分离提纯后得到复合物样品。采用紫外分光光度法确定形成常数,用X射线粉末衍射,红外光谱和核磁来表征该复合物。将制得的药物测其急性毒性,采用CCl₄制备小鼠急性肝损伤模型,检测经不同比例氧化苦参碱-甘珀酸钠复合物干预后小鼠血清天冬氨酸转氨酶(AST)、丙氨酸转氨酶(ALT)。结果氧化苦参碱-甘珀酸钠可形成1∶1的复合物;1∶1、2∶1比例形成的复合物的急性毒性均比其前体药物甘珀酸钠、氧化苦参碱低;与CCl₄模型组比较,经氧化苦参碱-甘珀酸钠1∶1、2∶1复合物处理的小鼠血清AST、ALT水平较低。结论氧化苦参碱与甘珀酸钠不同比例复合物的毒性均比其前体药物低;对小鼠急性CCl₄肝损伤有保护作用。

Objective Complex of oxymatrine(OMT)-carbenoxolone sodium(CS)was prepared,and the acute toxicity of the OMT-CS complex and their protective effects on injured liver induced by carbon tetrachloride(CCl₄)were also studied.Methods The OMT-CS complex was formed after preparing OMT and CS solutions individually then mixing them in ratio,the constant was detemined by UV-vis,the complex was characterized by powder X-ray diffraction,IR,and NMR.The sequence method was employed to test LD₅₀ of the complex by iv injection.The aspartate transaminase(AST)and alanine aminotransferase(ALT)in serum were measured in acute hepatic injuried models by CCl₄ proportionally im injected the complex in mice.Results The ratio of OMT and CS in the complex appeared to be 1∶1.The results of powder X-ray diffraction measurement indicated that a novel crystalline structure of complex was formed.The acute toxicities of LD₅₀ of the complexes in 1∶1,and 2∶1 were lower than that of both OMT and CS only.Compared with the model group by CCl₄,AST and ALT levels in serum were lower than that in the complex at 1∶1 and 2∶1 ratios.Conclusion The toxicity of the complex in different proportions on acute hepatic injuried mice by CCl₄ decreases obviously,compared with their precursor drugs.

科技部863计划资助项目(2003AA2Z3534)；宁夏大学自然科学基金资助项目(LG0516)