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Related Experiment Videos

Evaluation of a method for high throughput solubility determination using a multi-wavelength UV plate reader.

Teng-Man Chen1, Hong Shen, Chegnyue Zhu

  • 1Aventis Pharmaceuticals, Inc, Bridgewater, New Jersey 08807, USA. teng-man.chen@aventis.com

Combinatorial Chemistry & High Throughput Screening
|December 10, 2002
PubMed
Summary

This study introduces a fast, reproducible method for determining drug aqueous solubility using a UV plate reader. This technique accurately measures solubility down to 1 micro M, aiding early drug discovery.

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Area of Science:

  • Drug Discovery and Development
  • Pharmaceutical Sciences
  • Physical Chemistry

Background:

  • Aqueous solubility is a critical physicochemical property in drug discovery.
  • In silico prediction of solubility is challenging, necessitating experimental methods.
  • High-throughput screening demands efficient experimental solubility determination.

Purpose of the Study:

  • To evaluate a multi-wavelength UV plate reader method for rapid aqueous solubility determination.
  • To assess the sensitivity, reproducibility, and correlation with established methods.
  • To demonstrate the method's utility for diverse pharmaceutical compounds.

Main Methods:

  • Utilized a multi-wavelength UV plate reader with disposable 96-well UV plates.
  • Determined thermodynamic solubility in the presence and absence of dimethyl sulfoxide (DMSO).

Related Experiment Videos

  • Compared results with High-Performance Liquid Chromatography (HPLC) method.

    • Main Results:

    • The UV plate reader method demonstrated sensitivity down to 1 micro M.
    • Excellent reproducibility and high correlation (R>0.97) with HPLC were observed.
    • The method effectively quantified solubility for diverse pharmaceutical compounds (1-1000 micro M).

    Conclusions:

    • The UV plate reader method provides a fast, sensitive, and reproducible approach for aqueous solubility determination.
    • This method supports high-throughput screening by enabling efficient solubility assessment.
    • The flexibility to test in DMSO or aqueous solutions enhances its applicability in drug discovery.