Critical comparison of shake-flask, potentiometric and chromatographic methods for lipophilicity evaluation (log Po/w ) of neutral, acidic, basic, amphoteric, and zwitterionic drugs

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Adriana PortElisabeth Bosch

Abstract

In the present study three different procedures have been compared for the determination of the lipophilicity of the unionized species (log Po/w) of neutral, acidic, basic, amphoteric, and zwitterionic drugs. Shake-flask, potentiometric and chromatographic approaches have been assayed in a set of 66 representative compounds in different phases of advanced development. An excellent equivalence has been found between log Po/w values obtained by shake-flask and potentiometry, while the chromatographic approach is less accurate but very convenient for screening purposes when a high-throughput is required. In the case of zwitterionic and amphoteric compounds, either for shake-flask and chromatographic methods, the pH has to be accurately selected in order to ensure the compound to be in its neutral form.

Citations

Dec 21, 2019·Journal of Computer-aided Molecular Design·Mehtap IşıkJohn D Chodera
Nov 30, 2019·Journal of Computer-aided Molecular Design·William J ZamoraF Javier Luque
Jan 16, 2020·Journal of Computer-aided Molecular Design·Evrim ArslanViktorya Aviyente
Jul 18, 2019·ChemistryOpen·Károly MazákSándor Hosztafi
Aug 3, 2020·Journal of Chromatography. a·Colin F Poole, Sanka N Atapattu
Jun 29, 2021·Journal of Computer-aided Molecular Design·Nazanin Donyapour, Alex Dickson
Jul 13, 2021·Journal of Computer-aided Molecular Design·Kenneth LopezWilliam J Zamora
Aug 30, 2019·Molecular Pharmaceutics·Federica SodanoMaria Grazia Rimoli

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