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Establishment of an HPLC Method for Determination of Coumarin-3-Carboxylic Acid Analogues in Rat Plasma and a Preliminary Study on Their Pharmacokinetics
Journal of Chromatographic Science ( IF 1.5 ) Pub Date : 2021-09-07 , DOI: 10.1093/chromsci/bmab103
Yan Xiong 1 , Yong-Hong Liu 1 , Jian-Sha Li 1 , Yu-Ying Zhang 1 , Jing Zhang 1 , Tao Gong 1 , Xin-Hui Jiang 1
Affiliation  

A simple high performance liquid chromatography (HPLC) method was developed and validated for the determination of coumarin-3-carboxylic acid analogues (C3AA) in rat plasma and a preliminary study on pharmacokinetics. Ferulic acid (FA) was used as the internal standard substance, and coumarin-3-carboxylic acid (C3A) was used as a substitute for quantitative C3AA. After protein precipitation with methanol, the satisfactory separation was achieved on an ODS2 column when the temperature was maintained at 30 ± 2°C. The correlation coefficient r in the C3A linear equation is equal to 0.9990. Pharmacokinetic parameters for t1/2, Tmax, Cmax, area under the curve (AUC)0-t, average residence time (MRT), apparent volume of distribution (V z/F) and clearance (Cl/F) were 1.89 ± 0.03 h, 0.39 ± 0.14 h, 1.81 ± 0.10 g· mL−1 ·h, 7.88 ± 0.24 g·mL−1·h, 3.23 ± 0.14 h, 0.43 ± 0.03 (mg·kg−1)·(g·mL−1)−1·h−1, respectively. The high performance liquid chromatography-photo diode array detector (HPLC-PDA) method established in this study can be used to separate and determine the content of C3AA in plasma of rats after 60% ethanol extraction by gavage. The plasma concentration-time curve and pharmacokinetic parameters reflect the absorption of C3AA in rat blood after oral administration to some extent.

中文翻译:

大鼠血浆中香豆素-3-羧酸类似物HPLC测定方法的建立及药代动力学初步研究

开发并验证了一种简单的高效液相色谱 (HPLC) 方法,用于测定大鼠血浆中香豆素-3-羧酸类似物 (C3AA) 并进行药代动力学初步研究。阿魏酸(FA)用作内标物质,香豆素-3-羧酸(C3A)用作定量C3AA的替代物。用甲醇沉淀蛋白质后,当温度保持在 30 ± 2°C 时,在 ODS2 柱上实现了令人满意的分离。C3A 线性方程中的相关系数 r 等于 0.9990。t1/2、Tmax、Cmax、曲线下面积(AUC)0-t、平均停留时间(MRT)、表观分布容积(Vz/F)和清除率(Cl/F)的药代动力学参数为1.89±0.03 h, 0.39 ± 0.14 h, 1.81 ± 0.10 g·mL-1·h, 7.88 ± 0.24 g·mL-1·h, 3.23 ± 0.14 h, 分别为 0.43 ± 0.03 (mg·kg−1)·(g·mL−1)−1·h−1。本研究建立的高效液相色谱-光电二极管阵列检测器(HPLC-PDA)方法可用于分离测定大鼠60%乙醇灌胃后血浆中C3AA的含量。血浆浓度-时间曲线和药代动力学参数在一定程度上反映了大鼠口服给药后C3AA在大鼠血液中的吸收情况。
更新日期:2021-09-07
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