摘要
通过建立一种以咖啡酸为内标的HPLC方法以检测小鼠各组织中双咖酚酸的浓度,研究双咖酚酸在小鼠体内的药代动力学特征及组织分布状况。将健康小鼠按25 mg·kg-1的剂量腹腔注射给药后,收集不同时间点的含药血浆及心、肝、脾、肺、肾,检测双咖酚酸在各组织中的分布,并利用DAS2.1.1软件拟合房室模型,计算药动学参数。实验结果显示,所建立的HPLC法能够满足生物样品定量检测的方法学要求;小鼠腹腔注射双咖酚酸后在小鼠体内呈单室模型分布,达峰时间(t max)为0.083 h,最大血药浓度(C max)为28.667 mg·L-1,消除半衰期(t 1/2z)为7.974 h;双咖酚酸在主要组织中的分布顺序为:肾﹥血浆﹥心﹥脾﹥肺﹥肝。以上结果表明,小鼠腹腔注射双咖酚酸后,在各组织中快速分布,其中肾中浓度最高。
A HPLC method using caffeic acid as an internal standard is established to detect the concentration of bisphenolic acid in tissues of mice.The pharmacokinetic characteristics and tissue distribution of bisphenolic acid in mice are explored.After intraperitoneal administration of 25 mg·kg-1 to mice,the concentration of bisphenolic acid in plasma,heart,liver,spleen,lung and kidney are determined at different time point,the compartment model is fited and the pharmacokinetic parameters are calculated with DAS 2.1.1 software.The results show that the adopted HPLC method meets the requirements for quantitative analysis of biological sample.Single-compartment model is fitted to bisphenolic acid and its main pharmacokinetic parameters are as follows:t max of 0.083 h,C max of 28.667 mg·L-1,t 1/2z of 7.974 h,and the distribution of bisphenolic acid in main tissues is in the order of kidney>plasma>heart>spleen>lung>liver.These results indicate that bisphenolic acid is rapidly distributed in various tissues of mice after intraperitoneal administration,and the drug concentration in the kidney is the highest.
作者
赵莹
鲁文雪
高玉白
周凤梅
曲桂武
ZHAO Ying;LU Wen-xue;GAO Yu-bai;ZHOU Feng-mei;QU Gui-wu(Anti-Aging Research Institute,Binzhou Medical University,Yantai 264003,China;Shandong Luye Pharmaceutical Co Ltd,Yantai 264670,China)
出处
《烟台大学学报（自然科学与工程版）》
CAS
2021年第1期48-54,共7页
Journal of Yantai University(Natural Science and Engineering Edition)
基金
山东省自然科学基金资助项目(ZR2016HL55)。
关键词
双咖酚酸
药代动力学
组织分布
bisphenolic acid
pharmacokinetics
tissue distribution
