葛根素衍生物4ac纳米粒在小鼠体内药代动力学及组织分布考察

Study on pharmacokinetics and biodistribution of pur derivative nanopaticles in mice

目的:考察葛根素衍生物4ac纳米粒在小鼠体内的药代动力学及组织分布特征。方法:小鼠尾静脉给予4ac 15 mg.kg-1后,采用高效液相检测各时间点血浆和组织器官药物浓度,并用3p97软件计算药代动力学参数。结果:静脉给药后药时曲线符合二室开放模型,4ac纳米粒在心脏的相对摄取率是混悬液的21.18倍。结论:4ac纳米粒明显改变4ac在小鼠血浆中的药代动力学特征和组织中的靶向定位特征。葛根素衍生物4ac纳米粒在小鼠心脏的分布优于4ac混悬液,有望成为治疗心脑血管疾病的新药。

Objective： To study the pharmacokinetics and biodistribution of pur derivative nanopaticles 4ac in mice.Method： After intravenous administration of 15 mg·kg-1 of pur derivative 4ac,the plasma and tissue concentration was detected by HPLC.The pharmacokinetics parameters were calculated by the method of 3p97.Result： The concentration time curves were conformed to two compartment model.The Re of 4ac nanopaticles was 21.18 times higher than suspension.Conclusion： Our present study demonstrates that,compared to nanopaticles and suspension,nanopaticles significantly alter the pharmacokinetics in plasma and tissues targeting.Biodistribution of pur derivative 4ac nanopaticles in heart of mice was better than 4ac suspension.It will become a new drug for cardiovascular disease therapy.