期刊文献+

药物膜通透性体外评价方法研究进展 被引量:1

Development of in-vitro evaluation methods to access membrane permeability of drugs
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摘要 药物膜通透性是影响药物安全性和有效性的关键因素,因此在新药研发初期对药物膜通透性进行筛选是提高研发效率、降低研发成本的有效途径。体外评价方法因具有快速、简单等特点已成为药物膜通透性研究领域的热点。本文综述了近年来有关两相分配法、色谱测定法、毛细管电泳测定法、光学传感器测定法以及平行人工膜通透性测定法等体外测定方法在药物膜通透性评价中的应用进展。 Membrane permeability is one of the key properties which affect drug safety and efficacy,so its evaluation is very important for enhancing drug development efficiency and reducing drug reseach spendings.Recently,in-vitro evaluation methods have become the focus in the field of drug membrane permeability researches.In this paper,the developments of in-vitro evaluation methods are summarized,including two-phase partitioning method,chromatography method,capillary electrophoresis method,optical biosensor assay and parallel artificial membrane assay.
出处 《中国药科大学学报》 CAS CSCD 北大核心 2011年第1期16-21,共6页 Journal of China Pharmaceutical University
基金 国家自然科学基金资助项目(No.30901878)~~
关键词 新药筛选 膜通透性 体外评价方法 进展 drug screening membrane permeability in-vitro evaluation methods progress
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参考文献43

  • 1Caldwell GW. Compound optimization in early and late phase drug discovery: acceptable pharmacokinetic properties utilizing combined physicoehemieal, in vitro and in vivo screens [ J ]. Front Med Chem Online, 2004,1 ( 1 ) : 607 - 618.
  • 2Klopman G,Zhu H. Recent methodologies for the estimation of noctanol/water partition coefficients and their use in the prediction of membrane transport properties of drugs[ J]. MiniRev Med Chem,2005,5 ( 2 ) :127 - 133.
  • 3Saunders RA, Platts JA. Scaled polar surface area descriptors:development and application to three sets of partition coefficients [J].New J Chem ,2004,28( 1 ) : 166 - 172.
  • 4Engelmann FM, Rocha SVO, Toma HE, et al. Determination of noctanol/water partition and membrane binding of cationic porphyrins [ J ]. Int J Pharm, 2007,329 ( l/2 ) : 12 - 18.
  • 5Xia XR, Baynes RE, Monteiro RNA, et al. Determination of the partition coefficients and absorption kinetic parameters of chemicals in a lipophilic membrane/water system by using a membrane-coated fiber technique [ J ]. Eur J Pharml Sci, 2005,24 (1) :15 -23.
  • 6Xia XR, Baynes RE, Monteiro Riviere NA, et al. A novel in-vitro technique for studying percutaneous permeation with a membrane-coated fiber and gas chromatography/mass spectrometry: Part I. Performances of the technique and determination of the permeation rates and partition coefficients of chemical mixtures [J]. Pharmacol Res,2003,20(2) :275 -282.
  • 7Riviere JE, Baynes RE, Xia XR. Membrane-coated fiber (MCF) array approach for predicting skin permeability of chemical mixtures from different vehicles [ J ]. Toxicol Sci, 2007,99 ( 1 ) : 153 - 161.
  • 8Guo YG,Zhang J, Liu DN,et al. Determination of n-octanol-water partition coefficients by hollow-fiber membrane solvent microextraction coupled with HPLC [ J ]. Anal Bioanal Chem,2006,386 (7/8) :2 193 -2 198.
  • 9Yen TE, Agatonovic-Kustrin S, Evans AM, et al. Prediction of drug absorption based on immobilized artificial membrane(IAM) chromatography separation and calculated molecular descriptors [ J]. J Pharm Biomed Anal,2005,38(3 ) :472 - 478.
  • 10Valko K. Application of high-performance liquid chromatography based measurements of lipophilicity to model biological distribution [ J ]. J Chromatogr A,2004,1 037 ( 1/2 ) :299 - 310.

二级参考文献37

  • 1孙进,王淑君,程刚,陈济民.磷脂膜色谱及其在生物药剂学中的应用[J].药学学报,2003,38(6):475-480. 被引量:7
  • 2孙进,程刚,何仲贵,王淑君.磷脂膜色谱用于评价药物与有序磷脂膜的相互作用[J].药学学报,2003,38(9):702-706. 被引量:8
  • 3孙进,程刚,何仲贵,王淑君.磷脂膜色谱与正辛醇/水系统亲脂性测量尺度的比较[J].药学学报,2003,38(10):791-794. 被引量:4
  • 4李作俊.多相催化反应动力学基础[M].北京:北京大学出版社,1990.72-81.
  • 5傅献彩.物理化学[M].北京:高等教育出版社,1998.596.
  • 6吉林大学化学系编.催化作用基础[M].北京:科学出版社,1980.1-30.
  • 7Silverman L, Campbell R, Broach JR. New assay technologies for high-throughput screening, Curr. Opin. Chem. Biol., 1998, 2(3): 397~403.
  • 8Cook ND. Scintillation proximity assay: a versatile high-throughput screening technology. Drug Discov. Today, 1996, 1 (7): 287 ~ 294.
  • 9Grepin C, Pernelle C. High-throughput screening. Drug Discov. Today, 2000, 5(5): 212 ~ 214.
  • 10Zhang L, Zhang HX, Ren DC, et al. Technological advances in high-throughput screening for the analysis of bioactivity. Basal Med. Clin.,2001, 21(4): 306 ~ 309 .

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