Comparative Pharmacokinetics of Gallic Acid After Oral Administration of Gallic Acid Monohydrate in Normal and Isoproterenol-Induced Myocardial Infarcted Rats.

Comparative Pharmacokinetics of Gallic Acid After Oral Administration of Gallic Acid Monohydrate in Normal and Isoproterenol-Induced Myocardial Infarcted Rats.
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正常和异丙肾上腺素诱导的心肌梗塞大鼠口服一水没食子酸后没食子酸的药代动力学比较

DOI:
10.3389/fphar.2018.00328
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发表时间:
2018
影响因子:
5.6
通讯作者:
Wang SW
Wang SW
中科院分区:
医学2区
文献类型:
--
作者:
Yu Z;Song F;Jin YC;Zhang WM;Zhang Y;Liu EJ;Zhou D;Bi LL;Yang Q;Li H;Zhang BL;Wang SW

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没食子酸(gallic acid,GA)是一种多酚类天然产物,广泛存在于食品、饮料和中草药中,对心血管系统有良好的作用。本研究比较了GA单水合物50 mg/kg和100 mg/kg在正常和异丙肾上腺素诱导的心肌梗死大鼠体内药代动力学过程的差异。采用高效液相色谱法测定了大鼠血浆中GA的含量。结果表明,GA在正常和病理状态下的药代动力学有很大差异。GA在MI大鼠中的血药浓度-时间曲线下面积(50 mg/kg GA)和最大血药浓度(Cmax)分别是正常大鼠的1.7倍和1.3倍,而在MI大鼠中的血药浓度(Cmax)则是正常大鼠的2.5倍。此外,MI大鼠T1/2和MRT显著延长,CL显著降低。我们的研究结果表明,心肌梗死可能会改变GA的药代动力学过程,因此,在临床实践中,应重视含GA的草药制剂(或膳食营养品)在正常和病理状态下的潜在药代动力学差异。
Gallic acid (GA) is a polyphenolic natural product widely distributed in food, beverage, and traditional Chinese herbs with beneficial effects on the cardiovascular system. In this research, a comparative study was conducted to investigate the possible difference of pharmacokinetic process in normal and isoproterenol-induced myocardial infarcted rats after oral administration of GA monohydrate with the dose of 50 and 100 mg/kg, respectively. Quantification of GA in rat plasma was achieved by using a simple and rapid high-performance liquid chromatographic method. The results revealed that pharmacokinetics of GA were greatly different between normal and pathological state. GA exhibited slower absorption into the bloodstream, and yielded 1.7-fold (50 mg/kg GA) and 1.3-fold (100 mg/kg GA) less values of area under concentration–time curve as well as 2.5-fold lower of maximum blood concentration (Cmax) in MI rats than those in normal rats. In addition, significant prolonged T1/2and MRT as well as decreased CL were also registered in MI rats. Our findings suggest that myocardial infarction could alter the pharmacokinetic process of GA, and thus the potential pharmacokinetic differences of herbal preparations (or dietary nutrition) containing GA between normal and pathological conditions should be brought to the forefront seriously in clinical practice.
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