【摘要】 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。更多还原

【Abstract】 The aim of this study is to explore the tissue distribution of PEGylated puerarin in acute myocardial ischemia model rats. Healthy male SD rats were randomly divided into two groups(30 each).Both were given PEGylated puerarin at a dose of 488 mg·kg-1. After 5 min of medication, one group was normal rats, another group with acute myocardial ischemia was established by peritoneal injection of 50 mg·kg-1isoprenaline. After administration, the animals were executed at 30, 60, 90, 120, 150 and 180 min, then heart,liver, spleen, lung, kidney were extracted. The content of puerarin in organ tissue was determined by HPLC.The results showed that the AUC of tissue distribution of PEGylated puerarin in normal rats was liver > kidney >heart ≈ spleen > lung > brain. While the AUC of tissue distribution of PEGylated puerarin in acute myocardial ischemia model rats was liver ≈ heart > kidney > lung ≈ spleen > brain. AUCheart of PEGylated puerarin in acute myocardial ischemia model rats was 1.7 times than that of the normal rats, and there was significant difference(P < 0.05). Thus, PEGylated puerarin had a good heart-targeting property in early myocardial infarction area,drugs could accumulate in the ischemic myocardium. It provided important information for further study and clinic use of PEGylated puerarin.更多还原