【摘要】 目的建立LC-MS/MS法测定大鼠尿液和粪便中WSJ-537的浓度,并研究其在大鼠体内的排泄行为。方法使用乙腈沉淀法进行排泄物样品预处理,选用乙氧苯柳胺作为内标进行检测。色谱柱:Acquity^TM UPLC BEH C₁₈柱（2.1 mm×50 mm,1.7μm）;流动相:水（含0.1%甲酸）-乙腈（含0.1%甲酸）,梯度洗脱;流速:0.3 mL·min^-1。LC-MS/MS法测定大鼠尿液和粪便中WSJ-537的浓度。结果WSJ-537在4～4000 ng·mL^-1与峰面积线性关系良好,所建立方法的准确度、精密度、提取回收率、基质效应和稳定性均符合要求。WSJ-537单剂量灌胃给药5.2 mg·kg^-1后,大鼠尿液中的累积排泄总量为（235.09±316.88）ng,大鼠粪便中的累积排泄总量为（3742.74±2267.77）ng,排出体外的原形药物总量约占总给药量的0.36%。结论该方法预处理步骤简便,分析时间短,线性范围宽,灵敏度高,可用于研究WSJ-537在大鼠体内的排泄行为。更多还原

【Abstract】 Objective To determine the concentration of WSJ-537 in the urine and feces of rats by LC-MS/MS, and study the excretion behaviors in vivo. Methods The excretion sample was precipitated with acetonitrile. Elofesalamide was used as the internal standard. An Acquity^TM UPLC BEH C₁₈ column（2.1 mm×50 mm, 1.7 μm） was used. The mobile phase was 0.1% formic acid-water and 0.1% formic acid-acetonitrile with gradient elution. The flow rate was 0.3 mL·min^-1. The concentration of WSJ-537 in the urine, feces of rats was determined. Results The linearity of WSJ-537 was good at 4 ～ 4000 ng·mL^-1. The accuracy, precision, extraction recovery, matrix effect and stability of the established method all met the requirements. After a single dose oral administration of WSJ-537 at 5.2 mg·kg^-1, the cumulative excretion in the urine in rats was（235.09±316.88） ng, and the cumulative excretion in the feces in rats was（3742.74±2267.77） ng. The proportion of WSJ-537 excreted in vitro in the form of prototype compounds accounted for about 0.36% of the total administration. Conclusion The method has simple pretreatment procedure, short analysis time, wide linear range, and high sensitivity, and can be used to study the excretion behaviors of WSJ-537 in rats.更多还原