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为了探索PEG化葛根素在急性心肌缺血模型大鼠上的组织分布特点,采用健康雄性SD大鼠60只,随机分成两组,每组30只,均静脉注射给予PEG化葛根素,剂量为488 mg·kg-1,给药5 min后,一组设为正常大鼠,另一组大鼠腹腔注射给予异丙肾上腺素(剂量为50 mg·kg-1),造成急性心肌缺血模型。分别于给药后30、60、90、120、150和180 min处死部分动物,取心、肝、脾、肺、肾、脑组织脏器,利用HPLC测定各组大鼠组织脏器中葛根素的浓度。结果显示,PEG化葛根素在正常大鼠脏器中AUC大小顺序为肝>肾>心≈脾>肺>脑,而在急性心肌缺血模型大鼠中AUC大小顺序为肝≈心>肾>肺≈脾>脑,其中,在模型大鼠心脏中AUC为正常大鼠心脏中的1.7倍,且存在显著性差异(P<0.05)。结果表明,PEG化葛根素在心肌梗死早期区域具有较好的心脏靶向性,可以将药物蓄积于缺血心肌,为该药的进一步研究开发和临床应用提供重要的参考依据。
In order to explore the tissue distribution characteristics of PEGylated Puerarin in acute myocardial ischemia rats, 60 healthy male SD rats were randomly divided into two groups (30 rats in each group), all given PEGylated puerarin intravenously at a dosage of 488 mg · kg-1. After 5 min of administration, one group was set as normal rats and the other group was injected isoproterenol (50 mg · kg-1) intraperitoneally to induce acute myocardial ischemia model . Some animals, corpus, liver, spleen, lung, kidney and brain tissues were sacrificed at 30, 60, 90, 120, 150 and 180 minutes after administration respectively. The contents of puerarin concentration. The results showed that the order of AUC of PEGylated puerarin in normal rats was liver> kidney> heart ≈ spleen> lung> brain, and the order of AUC in acute myocardial ischemia rats was liver ≈ heart> kidney> Lung ≈ spleen> brain. Among them, the AUC in the model rat heart was 1.7 times that in the normal rat heart, and there was a significant difference (P <0.05). The results showed that PEGylated puerarin had good cardiac targeting in the early stage of myocardial infarction, which could accumulate the drug in the ischemic myocardium and provide an important reference for the further research, development and clinical application of this drug.