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目的:建立3,4-O-异亚丙基莽草酸(ISA)在小鼠血浆及组织样品中的RP-HPLC分析方法;对ISA静注给药在小鼠体内分布的行为进行研究。方法:小鼠组织匀浆液(或血浆)采用酸性甲醇沉淀蛋白质并提取药物,采用RP-HPLC法测定。大连依利特HypersilODS2柱(250mm×4.6mm,5μm);流动相:甲醇-0.3%醋酸(50∶100);检测波长:220nm;柱温:室温;流速:1.0mL·min-1。动物实验使用昆明种小鼠40只,尾静脉注射ISA200mg·kg-1,给药后按时间点分为10组,分别于0,5,10,15,20,25,30,60,90,120min取各组织样品,处理后测定。测得的数据采用DAS软件进行统计,计算并分析。结果:小鼠尾静脉给药ISA200mg·kg-1后,该药可很快在体内分布,大多数组织在5min即达到较高浓度;药物在体内分布较广,主要在血液及血流丰富的组织中;药物代谢较快,给药后20min后,大部分组织中药物浓度大幅下降。结论:本文建立的分析方法准确、灵敏度较高。通过研究,为ISA临床使用治疗范围的确定、用药剂量的确定以及临床用药监测提供参考和依据。
OBJECTIVE: To establish a method for the RP-HPLC analysis of 3,4-O-isopropylidene shikimic acid (ISA) in mouse plasma and tissue samples. The distribution of ISA intravenous administration in mice was studied. METHODS: Mouse homogenates (or plasma) were subjected to acidic methanol precipitation and protein extraction and determined by RP-HPLC. Dalian elite HypersilODS2 column (250mm × 4.6mm, 5μm); mobile phase: methanol -0.3% acetic acid (50:100); detection wavelength: 220nm; column temperature: room temperature; flow rate: 1.0mL · min-1. Animal experiments using Kunming mice 40, tail vein injection of ISA200mg · kg-1, after administration by time points are divided into 10 groups, respectively, at 0,5,10,15,20,25,30,60,90,120min Take each tissue samples, after treatment determination. Measured data using DAS software for statistics, calculations and analysis. RESULTS: After iv administration of 200 mg · kg-1 of ISA in the tail vein of mice, the drug could be rapidly distributed in the body. Most of the tissues reached a higher concentration in 5 min. The drugs were widely distributed in the body mainly in blood and blood-rich Tissue; drug metabolism faster, 20min after administration, most of the tissue drug concentration decreased significantly. Conclusion: The analytical method established in this paper is accurate and sensitive. Through the research, provide the reference and basis for the determination of therapeutic range of clinical use of ISA, the determination of dosage and clinical drug monitoring.