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/MWn). The correlation between kIAM/MWn 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/MWn 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.
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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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Yoon, C., Shin, B., Chang, H. et al. Rapid Screening of Drug Absorption Potential Using the Immobilized Artificial Membrane Phosphatidylcholine Column and Molar Volume. Chromatographia 60, 399–404 (2004). https://doi.org/10.1365/s10337-004-0410-x
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DOI: https://doi.org/10.1365/s10337-004-0410-x