Lipophilicity Measurement of Drugs by Reversed Phase HPLC over Wide pH Range Using an Alkaline-Resistant Silica-Based Stationary Phase, XBridge^<TM> Shield RP_<18>

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概要

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• We propose a reversed phase HPLC (RP-HPLC) with an alkaline-resistant silica-based stationary phase, XBridge^<TM> Shield RP_<18>, for the determination of the lipophilicity of drugs with diverse chemical nature ranging from acidic to basic. A set of 40 model compounds with well-defined solvatochromic parameters was selected to allow a broad distribution of structural properties. The chromatographic results showed that the lipophilicity index log k_w, obtained with XBridge^<TM> Shield RP_<18> was well correlated with experimental log P_<oct> values (r^2=0.96). Linear solvation free-energy relationship (LSER) analyses revealed that the retention mechanism of the stationary phase and 1-octanol/water partitioning were controlled by almost the same balance of intermolecular forces (hydrophobicity as expressed by the van der Waals volume V_w, H-bond acceptor basicity β, and dipolarity/polarizability π^*). The results showed that XBridge^<TM> Shield RP_<18> phase overcomes the shortcomings of the silicabased stationary phases, the application of which to lipophilicity measurements had been limited to neutral and acidic compounds.

• 公益社団法人日本薬学会の論文
• 2008-10-01

著者

• Tanaka Hideji

  Institute Of Health Biosciences The University Of Tokushima Graduate School

• LIU Xiangli

  Department of Pharmaceutical Technology, Friedrich-Schiller-Universitat Jena

• HEFESHA Hossam

  Department of Pharmaceutical Technology, Friedrich-Schiller-Universitat Jena

• SCRIBA Gerhard

  Department of Pharmaceutical Chemistry, Friedrich-Schiller-Universitat Jena

• FAHR Alfred

  Department of Pharmaceutical Technology, Friedrich-Schiller-Universitat Jena

• Fahr Alfred

  Department Of Pharmaceutical Technology Friedrich-schiller-universitat Jena

• Liu Xiangli

  Department Of Pharmaceutical Technology Friedrich-schiller-universitat Jena

• Scriba Gerhard

  Department Of Pharmaceutical Chemistry Friedrich-schiller-universitat Jena

• Hefesha Hossam

  Department Of Pharmaceutical Technology Friedrich-schiller-universitat Jena

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