联苯乙酸及其前药在大鼠或人体内的代谢.PDFVIP

联苯乙酸及其前药在大鼠或人体内的代谢  沈旭 1 ，申屠建中 2*(1.浙江工业大学，杭州 310014 ；2.浙江大学第一附属医院，杭州 310003) 摘要：本文综述了近几年国内外相关报道，将代谢后主要活性产物为联苯乙酸的药物分为一类，统称为联苯乙酸的前药， 通过质谱联用技术论述了其在人体内的代谢过程与产物。联苯乙酸是发挥抗炎、镇痛作用的关键物质，但由于其水溶性 差、口服给药常造成消化道障碍等缺点，除了制成外用制剂外，目前针对联苯乙酸的研究主要集中于其相关前药的合成、 制剂、药理、药效等方面。联苯乙酸相关药物的研发成功可以较好地降低直接给联苯乙酸所带来的不良反应，为临床医 师解除患者病痛提供有效的治疗手段，具有良好的开发前景，为苯胺洛芬的人体药动学研究提供思路。 关键词：联苯乙酸；代谢；液相色谱-质谱联用技术；苯胺洛芬 中图分类号：R969.1 文献标志码：A 文章编号：1007-7693(2017)07-1068-05 DOI: 10.13748/ki.issn1007-7693.2017.07.031 引用本文：沈旭, 申屠建中. 联苯乙酸及其前药在大鼠或人体内的代谢[J]. 中国现代应用药学, 2017, 34(7): 1068-1072. Metabolism of Felbinac and Its Pro-drug in Rats or Human Body 1 2* SHEN Xu , SHENTU Jianzhong (1.Zhejiang University of Technology, Hangzhou 310014, China; 2.First Affiliated Hospital, Zhejiang University, Hangzhou 310003, China) ABSTRACT ：According to the correlative reports in recent years, the main active products of metabolism which were felbianc are divided into a class of drugs, they are referred to as the former drug of the acetic acid. The metabolic processes and products in human body are discussed by LC-MS. Felbinac is the active metabolite of many non-steroidal anti-inflammatory drugs, and it is also the key material for its anti-inflammatory and analgesic effects. The shortcoming of low water solubility, gastrointestinal disorders by the oral administration and so on, in addition to the external reagent, felbinac research mainly concentrated in the prodrug synthesis, preparation, pharmacology and efficacy at present. The successful research and development of the related drugs of felbinac can reduce the side effects brought by the direct administration of felbianc, providing effective treatment for clinicians to relieve the pain of patients, and provide a way for human to study the pharmacokinetics of felbinac trometamol. KEY WORDS: felbinac; metabolize; LC-MS; felbinac trometamo