中文摘要：

绿原酸为多种中药注射液的主要成分,本文采用超高效液相色谱-四极杆飞行时间质谱法（UPLC/Q-TOF MS）鉴定大鼠注射给予绿原酸后胆汁、尿、粪和血浆中的代谢产物。利用碰撞能量梯度（MSE）和质量亏损过滤（MDF）技术,在大鼠胆汁、尿、粪和血浆中共检测到35种代谢产物。胆汁中主要代谢产物为O-甲基绿原酸谷胱甘肽结合物,其排泄量超过胆汁中全部代谢物的80%,尿中主要为原形、O-甲基结合物、水解代谢产物及葡糖醛酸结合物,粪中主要为O-甲基结合物及其半胱氨酸结合物,血浆中主要为原形化合物。绿原酸及其代谢产物经尿和粪便排泄比例相近。实验结果表明,绿原酸在大鼠体内代谢广泛,主要途径之一是与谷胱甘肽结合,提示绿原酸的烯酮双键具有亲电性,可能与蛋白的巯基共价结合,导致过敏性不良反应,应予以关注。

英文摘要：

Chlorogenic acid（5-CQA） is one of the major components in some Chinese herbal injections.However,the metabolism of 5-CQA in rats after intravenous injection has not been determined.An ultra-high performance liquid chromatography/quadrupole time-of-flight mass spectrometry（UPLC/Q-TOF MS） method was applied to identify the metabolites in bile,urine,feces and plasma after a single intravenous administration of 10 mg·kg-1 5-CQA to rats.Using MSE and mass defect filter techniques,a total of 35 metabolites were detected in bile,urine,feces and plasma.The predominant metabolites in bile were glutathione conjugates of O-methyl-5-CQA,accounting for approximately 80% of the metabolites excreted in bile.The major components in urine were parent drug,O-methyl-5-CQA,hydrolyzed metabolites and glucuronide conjugates.The major components in feces were O-methyl-5-CQA and its cysteine conjugates.The major component in plasma was the parent drug.The urinary and fecal excretion pathways were equally important to 5-CQA in rats.These results demonstrate that 5-CQA undergoes extensively metabolism in rats and are highly reactive to nucleophiles such as GSH.This finding indicates that attention should be paid on the injections containing 5-CQA,which may covalently bind to proteins,leading to allergenic drug reactions.