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A new method for quantitative assessment of mechanisms of partitioning and absorption of drugs: linear solvation energy relationships

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Author:: No author available

Journal Title:: ACTA PHARMACEUTICA SINICA

Issue:: 1

DOI:: 10.3321/j.issn:0513-4870.2007.01.003

Key Word:: 线性溶剂化能量方程;吸收;分配

Abstract：线性溶剂化能量方程是研究药物定量结构-保留/活性关系、预测色谱系统中药物保留指数的重要工具.根据线性溶剂化方程建立了生物膜多种体外模拟模型中药物保留因子与其分子描述符之间的定量关系,以及阐明药物-膜作用机制.此外,根据线性溶剂化方程建立了定量结构-活性关系用于预测药物肠吸收、血脑屏障通透性和皮肤透过性.本文综述了线性溶剂化能量方程在定量评价药物分配机制和吸收方面的重要意义及其广泛应用,并指出了该方程的局限性,为研究药物分配和吸收提供新思路.

Reference

[1]孙进,程刚,何仲贵,等.磷脂膜色谱用于评价药物与有序磷脂膜的相互作用[J].2003,(9).
[2]孙进,王淑君,程刚,等.磷脂膜色谱及其在生物药剂学中的应用[J].2003,(6).
[3]Fuguet, E.,Rafols, C.,Bosch, E.,etc.Solute-solvent interactions in micellar electrokinetic chromatography[J].2002,942(1).
[4]M H, Abraham,H S, Chadha,G S, Whiting,etc.Hydrogen bonding. 32. An analysis of water-octanol and water-alkane partitioning and the delta log P parameter of seiler.[J].1994,83.
[5]J A, Gratton,M H, Abraham,M W, Bradbury,etc.Molecular factors influencing drug transfer across the blood-brain barrier.[J].1997,49(12).
[6]Khaledi MG.,Trone MD..Characterization of chemical selectivity in micellar electrokinetic chromatography. 4. Effect of surfactant headgroup[J].1999,71(7).
[7]Abraham MH,Martins F.Human skin permeation and partition: General linear free-energy relationship analyses.[J].2004,93(6).
[8]M A, García,M F, Vitha,J, Sandquist,etc.Study of retention in micellar liquid chromatography on a C8 column by the use of linear solvation energy relationships.[J].2001,918(1).
[9]Abraham MH,Le J,Hersey A,etc.Rate-limited steps of human oral absorption and QSAR studies.[J].2002,19(10).
[10]孙进,出口芳春,陈济民,等.通过喹诺酮抗生素与磷脂膜的相互作用预测肺泡巨噬细胞单层的体外摄取[J].2002,(5).
[11]Agnes Taillardat-Bertschinger,Pierre-Alain Carrupt,Bernard Testa,etc.Immobilized Artificial Membrane HPLC in Drug Research[J].2003,46(5).
[12]Zhao YH,Le J,Abraham MH,etc.Evaluation of human intestinal absorption data and subsequent derivation of a quantitative structure-activity relationship (QSAR) with the Abraham descriptors.[J].2001,90(6).
[13]Bevan CD,Abraham MH,Valko K,etc.Rapid-gradient HPLC method for measuring drug interactions with immobilized artificial membrane: comparison with other lipophilicity measures.[J].2000,89(8).
[14]Foley JP,Pascoe RJ.Characterization of surfactant and phospholipid vesicles for use as pseudostationary phases in electrokinetic chromatography.[J].2003,24(24).
[15]Agnes Taillardat-Bertschinger,Maria I.La Rotonda,Maria Tiziana Quercia,etc.Structural Properties Governing Retention Mechanisms on Immobilized Artificial Membrane (IAM) HPLC Columns[J].2002,85(2).
[16]Mitchell RC,Leitao ARE,Chadha HS,etc.Determination of Solute Lipophilicity, as Log P(Octanol) and Log P(Alkane) Using Poly(Styrene-Divinylbenzene) and Immobilised Artificial Membrane Stationary Phases in Reversed-Phase High-Performance Liquid Chromatography[J].1997,766(1).
[17]Gil-Agusti, M.,Esteve-Romero, J.,Abraham, M. H..Solute-solvent interactions in micellar liquid chromatography[J].2006,1117(1).
[18]Yasushi Ishihama,Michael H. Abraham,Clara Rafols,etc.Linear free energy relationship analysis of microemulsion electrokinetic chromatographic determination of lipophilicity[J].1996,752(1).
[19]Abraham MH.,Cometto-Muniz JE.,Kumarsingh R.,etc.Connection between chromatographic data and biological data[J].2000,745(1).
[20]Abraham MH,Hersey A,Luscombe CN,etc.Quantitative relationship between rat intestinal absorption and Abraham descriptors.[J].2003,38(11).
[21]M H, Abraham,K, Takács-Novák,R C, Mitchell.On the partition of ampholytes: application to blood-brain distribution.[J].1997,86.
[22]Valko K.Application of high-performance liquid chromatography based measurements of lipophilicity to model biological distribution[J].2004,1037(1).
[23]Platts JA,Abraham MH,Zhao YH,etc.Correlation and prediction of a large blood-brain distribution data set--an LFER study.[J].2001,36(9).
[24]Asakawa N,Oda Y,Uchikawa K,etc.Evaluation of Solute Hydrophobicity by Microemulsion Electrokinetic Chromatography[J].1995,67(9).
[25]Abraham MH.The factors that influence permeation across the blood-brain barrier.[J].2004,39(3).