Partition coefficient vs. binding constant: How best to assess molecular lipophilicity

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Gregor Cevc

Abstract

Partition coefficient, P, is the preferred descriptor of molecular lipo- or hydrophilicity, and thus of relationships between a solute (S, e.g., a drug), a polar medium (W, e.g., an aqueous buffer), and an essentially apolar, organic, medium or a drug carrier (O). The coefficient is commonly identified with the linear ratio of solute quantities in the two media, P=nSO/nSW, even to characterise solute association with or binding to a surface (e.g., of a HPLC column or a drug carrier). To check the latter practice correctness-and credibility of the prevailing P definition-this paper compares an ideal solute distribution between two separate homogeneous fluid media (i.e., partitioning) to solute association with a uniform surface immersed in one such medium (i.e., binding). This reveals that solute partitioning and binding fundamentally differ and can only exceptionally be described, or analysed, with similar equations. Nonlinearised formulae that describe partitioning (Eq. (9)) and binding (Eq. (11)) can yield similar lipophilicity descriptor values only if solute preparation is relatively dilute; employing a large organic medium fraction is helpful in this respect. Additional prerequisites for partitioning and binding models mat...Continue Reading

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Citations

Apr 17, 2016·Journal of Pharmaceutical and Biomedical Analysis·Klára L Valkó
Mar 31, 2017·Scientific Reports·Tiago N FigueiraMiguel A R B Castanho
May 10, 2019·APL Bioengineering·Elaine J SuAmy E Herr
Nov 7, 2017·Chemistry and Physics of Lipids·Mustafa M A ElsayedGregor Cevc
Apr 25, 2018·Langmuir : the ACS Journal of Surfaces and Colloids·Gregor CevcBert Nickel

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