【作者】 陈笑艳； 孙玉明； 黄佳； 钟大放；

【Author】 CHEN Xiao-yan, SUN Yu-ming, HUANG Jia, ZHONG Da-fang (Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, Shenyang 110016, China)

【机构】 沈阳药科大学药物代谢与药物动力学实验室；

【摘要】 <正> 与大多数药物相比,肽类药物结构特殊、用药剂量低、生物体内有大量相似物质干扰,导致血浆样品难于测定,药物动力学研究面临更大的挑战。阿拉瑞林是我国研究开发的人工合成的促性腺激素释放激素的九肽类似物,临床上主要用于治疗子宫内膜异位症等激素依赖性疾病,口服日剂量仅为100～300μg,由于缺少高灵敏度的分析方法,药物动力学研究仍为空白。已有文献报道,采用液相色谱-离子阱质谱(LC-MS~n)、液相色谱-单四级杆质谱以及液相色谱-飞行时间质谱(LC-TOFMS)等技术对生物样品中小肽类药物进行定量分析,但定量下限均大于更多还原

【Abstract】 A sensitive and specific liquid chromatography-electrospray ionization tandem mass spectrometric method is described for the determination of alarelin in human plasma by selected reaction monitoring (SRM) mode. The method was linear in the concentration range of 0.1—20μg/L for alarelin. The intra- and inter-day precision was within 9%. The assay accuracy was within ±1.2%. The method was successfully employed in pharma cokinetic studies after i.m. administration of 75, 150 and 225μg alarelin to 30 healthy female volunteers.更多还原