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目的:对聚乙二醇(PEG)化葛根素前药(mPEG5000-Pur)体内药效学进行初步评价,为开发新型无溶血不良反应的葛根素制剂奠定基础。方法:采用垂体后叶素诱导大鼠急性心肌缺血模型,观察mPEG5000-Pur对心肌的保护作用;采用氯仿诱导小鼠心律失常模型,观察mPEG5000-Pur抗心律失常的作用。结果:葛根素PEG化后增强了对大鼠缺血心肌的保护作用;并且PEG化也可增强葛根素的抗小鼠心律失常作用,但是药效不呈剂量依赖性。结论:葛根素经PEG化后仍然保持了抗心肌缺血和抗心律失常的作用,且药效均优于相应剂量葛根素注射液组,这可能与PEG化后对葛根素体内组织分布改善有关。
OBJECTIVE: To evaluate the pharmacokinetics of mPEG5000-Pur in vivo and to lay the foundation for the development of new puerarin preparations without adverse reaction to hemolysis. Methods: The rat model of acute myocardial ischemia induced by pituitrin was used to observe the protective effect of mPEG5000-Pur on myocardium. The anti-arrhythmic effect of mPEG5000-Pur was observed by using chloroform induced arrhythmia model in mice. Results: Puerarin pretreatment enhanced the protective effect of ischemic myocardium in rats. PEGylation also enhanced the anti-arrhythmic effects of puerarin in a dose-dependent manner. CONCLUSION: Puerarin still maintains anti-myocardial ischemia and anti-arrhythmic effects after PEGylation, and its pharmacodynamic effects are superior to those of puerarin injection group, which may be related to the improvement of the tissue distribution of puerarin in vivo .