蛋白多肽类药物体内药代动力学特征及分析方法研究进展  

Pharmacokinetic Characters of Protein and Peptide Drugs and the Analyzing Methods for Metabolism of These Drugs in Vivo

作　　者：杨旭[1] 潘佳佳[1] 夏菲[1] 王妍[1] 沈子龙[1] 徐寒梅[1] 

机构地区：[1]中国药科大学生命科学与技术学院,江苏南京210009

出　　处：《药物生物技术》2014年第4期363-366,共4页Pharmaceutical Biotechnology

基　　金：国家863计划"多肽分子药靶发现与药物设计技术"(No.2012AA020304);江苏省产学研项目"多肽AP25抗肿瘤的机制研究"(SBY201020063);江苏省普通高校研究生科研创新计划资助项目"PEG修饰多肽HM-3在肿瘤研究中的应用"(No.CXZZ11_0821)

摘　　要：文章结合近年来国内外蛋白多肽类药物非临床药代动力学研究进展,通过与传统小分子药物比较,对该类药物在动物体内的药代动力学特征及分析方法进行了评述,为蛋白质多肽类新药的设计、研究与开发提供相关的依据。与传统小分子药物相比,蛋白多肽类药物在给药途径、体内分布、代谢、消除等方面都具有鲜明的自身特点。在生物体内,这类药物具有首过效应显著,体内靶向分布、受体介导消除、极少以原型药物形式排泄,血浆蛋白结合率较高等特征。在分析技术方面,文章中主要介绍了酶联免疫吸附测定、放射性同位素示踪技术、LCMS/MS技术、活体成像技术、电化学发光免疫分析以及微流控芯片免疫分析等方法。In recent years, there has been big progress in the development of non-clinical pharmacokinetic research methods in China or in foreign countries. After comparison with the traditional small molecular drugs, pharmacokinetic characters and the analy- zing methods for metabolizing of protein and peptide drugs in vivo were reviewed in this paper. This review provides the related basis for the design, development and research of this kind of new drugs. The absorption, distribution, metabolism and excretion of protein and peptide drugs have distinctive features compared with those of small molecular drugs. In living organisms, the protein and peptide drugs have an obvious first pass effect, target-specific distribution and target-mediated drug disposition. These drugs are seldom excreted as prototype drugs and they have a high plasma protein binding rate. In the analysis techniques, the traditional ELISA, radioactive tracer techniques, LC-MS/MS techniques, in vivo imaging techniques, electro-chemiluminescence immunoassay and microfluidic immunoassay chip have been introduced in the current review.

关 键 词：蛋白多肽类药物 药代动力学特征 分析方法 

分 类 号：Q516[生物学—生物化学]