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Physicochemical profiling (solubility, permeability and charge state).

A Avdeef1

  • 1pION INC, Woburn, MA 01801, USA. aavdeef@pion-inc.com

Current Topics in Medicinal Chemistry
|March 20, 2002
PubMed
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Physicochemical profiling helps predict drug absorption by measuring solubility and permeability. Early identification of molecules with poor oral absorption properties can reduce costly development failures.

Area of Science:

  • Pharmacology
  • Drug Discovery
  • Physical Chemistry

Background:

  • Pharmacokinetic (PK) failures lead to ~30% of drug candidate rejection.
  • Poor oral absorption due to low solubility and permeability significantly increases development costs.
  • Reliable in vitro methods are crucial for early identification of molecules with favorable pharmaceutical properties.

Purpose of the Study:

  • To review recent advancements in physicochemical profiling for predicting oral drug absorption.
  • To highlight the importance of solubility, permeability, and related parameters in drug discovery.
  • To discuss the application of the Biopharmaceutics Classification System (BCS) framework in early-stage research.

Main Methods:

  • Focus on instrumental methods for measuring key physicochemical parameters: permeability (Pe), solubility (S), ionization constant (pKa), lipophilicity (log P, log D), and retention (R).

Related Experiment Videos

  • Discussion of factors influencing these parameters, including pH, lipophilicity, protein binding, and unstirred water layers.
  • Application of Fick's first law to understand passive diffusion across lipid membranes.

    • Main Results:

    • Physicochemical profiles provide valuable insights into a molecule's potential for oral absorption.
    • The BCS framework integrates permeability and solubility to predict in vivo drug product performance.
    • Measurements of pH-dependent properties are critical for ionizable compounds.

    Conclusions:

    • Early physicochemical profiling is essential for mitigating PK-related failures in drug development.
    • Instrumental methods offer robust tools for assessing drug absorption properties.
    • Integrating these profiles aids medicinal chemists in selecting viable drug candidates.