Li Chao, Song Xiaowei, Song Junke, Pang Xiaocong, Wang Zhe, Zhao Ying, Lian Wenwen, Liu Ailin, Du Guanhua
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; Beijing Key Laboratory of Drug Target and Screening Research, Beijing 100050, China; State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing 100050, China.
Acta Pharm Sin B. 2016 Jan;6(1):64-70. doi: 10.1016/j.apsb.2015.10.001. Epub 2015 Nov 29.
The pharmacokinetic profile of gallocatechin-7-gallate (J10688) was studied in rats after intravenous administration. Male and female Sprague-Dawley (SD) rats received 1, 3, and 10 mg/kg (i.v.) of J10688 and plasma drug concentrations were determined by a high performance liquid chromatography-mass spectrometry (LC-MS) method. The pharmacokinetic software Data Analysis System (Version 3.0) was used to calculate the pharmacokinetic parameters. For different i.v. doses of J10688, the mean peak plasma concentration (C 0) values ranged from 11.26 to 50.82 mg/L, and mean area under the concentration-time curve (AUC0-t ) values ranged from 1.75 to 11.80 (mg·h/L). J10688 lacked dose-dependent pharmacokinetic properties within doses between 1 and 10 mg/kg, based on the power model. The method developed in this study was sensitive, precise, and stable. The pharmacokinetic properties of J10688 in SD rats were shown to have rapid distribution and clearance values. These pharmacokinetic results may contribute to an improved understanding of the pharmacological actions of J10688.
在大鼠静脉注射后研究了表儿茶素-7-没食子酸酯(J10688)的药代动力学特征。雄性和雌性斯普拉格-道利(SD)大鼠接受1、3和10mg/kg(静脉注射)的J10688,并通过高效液相色谱-质谱联用(LC-MS)法测定血浆药物浓度。使用药代动力学软件数据分析系统(版本3.0)计算药代动力学参数。对于不同静脉注射剂量的J10688,平均血浆峰浓度(C0)值范围为11.26至50.82mg/L,浓度-时间曲线下平均面积(AUC0-t)值范围为1.75至11.80(mg·h/L)。基于幂模型,J10688在1至10mg/kg剂量范围内缺乏剂量依赖性药代动力学特性。本研究建立的方法灵敏、精确且稳定。J10688在SD大鼠中的药代动力学特性显示具有快速分布和清除值。这些药代动力学结果可能有助于更好地理解J10688的药理作用。