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国际临床研究杂志

International Journal of Clinical Research

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International Journal of Clinical Research. 2025; 9: (9) ; 10.12208/j.ijcr.20250413 .

LC-MS/MS was used to investigate the metabolism of vardenafil in the blood of mice
基于LC-MS/MS探讨小鼠血液中伐地那非的代谢规律

作者： 王礞棽, 李铭扬, 纪孟萱, 王燕燕 *

北京警察学院 北京

*通讯作者： 王燕燕,单位：北京警察学院 北京；

引用本文: 王礞棽, 李铭扬, 纪孟萱, 王燕燕 基于LC-MS/MS探讨小鼠血液中伐地那非的代谢规律[J]. 国际临床研究杂志, 2025; 9: (9) : 1-6.
Published: 2025/9/21 10:00:20

摘要

目的 通过监测小鼠血液中的伐地那非浓度变化，总结伐地那非在小鼠体内的代谢规律。建模转化为人类服药时间，帮助涉药检测。方法 血液采取血液样本采用蛋白沉淀法处理、超声提取；液相采用梯度洗脱程序，色谱柱：Thermo Hypersil GOLD C18 (2.1 mm×100 mm，1.9 µm)；柱温：30℃；流动相 A：5mmol/L 甲酸铵-0.1%甲酸水溶液，流动相 B：含 0.1%甲酸的乙腈溶液；梯度洗脱程序：0~0.5min A相90%，0.5~7min A相30%，7~9min A相5%，9~10min A相5%，10~10.01min A相90%，10.01~10.5min A相90%；流速：0.3mL/min；进样量：1µL。质谱检测采用电喷雾离子源正、负离子扫描模式（ESI+）；多反应监测扫描模式（MRM）；定性离子对489.19/312.04、489.19/298.929和489.19/151.04；定量离子对489.19/312.04。结论 实现了用药时间的逆向推算，模型预测半衰期（76.7 min）与实际报告值的相对误差小于5%。结合体表面积法获得的跨物种换算工具（预测人类半衰期误差<5%）。为涉药案件时效研判提供了简便可靠的技术支持，为公安实战中涉药案件的服药时间精准推断提供了标准化技术方案。

关键词： 液-质联用仪；伐地那非；代谢规律；药物动力学；法医

Abstract

Objective By monitoring the concentration changes of vardenafil in mouse blood, this study summarizes the metabolic profile of vardenafil in mice. The model was extrapolated topredict human dosing timelines, aiding drug-related forensic investigations.
Methods Blood samples were processed using protein precipitation and ultrasonic extraction. Liquid chromatography employed a gradient elution program with the following parameters: column, Thermo Hypersil GOLD C18 (2.1 mm × 100 mm, 1.9 µm); column temperature, 30°C; mobile phase A, 5 mmol/L ammonium formate–0.1% formic acid aqueous solution; mobile phase B, 0.1% formic acid in acetonitrile; Gradient elution procedure: 90% A phase at 0-0.5min, 30% A phase at 0.5-7min, 5% A phase at 7-9min, 5% A phase at 9-10min, 90% A phase at 10-10.01min, 90% A phase at 10.01-10.5min; flow rate, 0.3 mL/min; injection volume, 1 µL. Mass spectrometry detection utilized an electrospray ionization source (ESI+) in multiple reaction monitoring (MRM) mode, Qualitative ion pairs: 489.19/312.04, 489.19/298.929 and 489.19/151.04; Quantitative ion pair 489.19/312.04.
Conclusion   The reverse calculation of medication duration was achieved, and the relative error between the model's predicted half-life (76.7 min) and the actual reported value was less than 5%. A cross-species conversion tool obtained by the combined body surface area method (with an error of less than 5% in predicting human half-life). It provides simple and reliable technical support for the judgment of the time limit of drug-related cases and offers a standardized technical solution for the precise inference of the medication time in drug-related cases in public security practice.

Key words： LC-MS/MS; Vardenafil; Metabolic profile; Pharmacokinetics; Forensic science

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