Chromatographia

, Volume 60, Issue 7–8, pp 399–404 | Cite as

Rapid Screening of Drug Absorption Potential Using the Immobilized Artificial Membrane Phosphatidylcholine Column and Molar Volume

  • C. H. Yoon
  • B. S. Shin
  • H. S. Chang
  • L. S. Kwon
  • H. Y. Kim
  • S. E. Yoo
  • S. D. Yoo
Article

Abstract

The immobilized artificial membrane phosphatidylcholine (IAMPC) chromatography was evaluated for the predictability of oral absorption potential of 40 structurally unrelated drugs. The chromatographic capacity factors (kIAM) were determined as a function the pH and composition of the mobile phase, and were corrected for the molar volume of the solutes (kIAM/MW n ). The correlation between kIAM/MW n and the human fraction of intestinal absorption (Fa) was highest when measured at 20% acetonitrile (pH 5.5) with the power function n = 2.5. The best-fit equation for the sigmoid relationship between kIAM/MW n and Fa was obtained: Fa (%) = 94.3 × {1-exp[-17.9 × (kIAM/MW2.5) × 106]}^2.1 (r = 0.925). This in vitro prediction method may be useful in a rapid screening of drug candidates with high oral absorption potential in humans.

Keywords

Column liquid chromatography Immobilized artificial membrane Oral absorption potential High throughput screening Molar volume 

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Notes

Acknowledgments.

This work was supported by the Century 21 Frontier Research Program Grant CBM-C800-001 from the Ministry of Science and Technology, Korea. Seok Chun Scholarship for SDY from Sungkyunkwan University is appreciated.

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Copyright information

© Friedr. Vieweg&Sohn/GWV Fachverlage GmbH 2004

Authors and Affiliations

  • C. H. Yoon
    • 1
  • B. S. Shin
    • 1
  • H. S. Chang
    • 1
  • L. S. Kwon
    • 2
  • H. Y. Kim
    • 2
  • S. E. Yoo
    • 3
  • S. D. Yoo
    • 1
  1. 1.College of PharmacySungkyunkwan UniversitySuwonKorea
  2. 2.C&C Research LaboratoriesHwasung-siKorea
  3. 3.The Center for Biological Modulators Korea Research Institute of Chemical TechnologyYuseong-guKorea

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