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

doi:10.1365/s10337-004-0410-x

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

Department of Pharmacy

Research output: Contribution to journal › Article › peer-review

16 Scopus citations

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 (k_IAM) were determined as a function the pH and composition of the mobile phase, and were corrected for the molar volume of the solutes (k _IAM/MWⁿ). The correlation between k_IAM/MW ⁿ and the human fraction of intestinal absorption (F_a) 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 k _IAM/MWⁿ and F_a was obtained: F_a (%) = 94.3 × {1-exp[-17.9 × (k_IAM/MW^2.5) × 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.

Original language	English
Pages (from-to)	399-404
Number of pages	6
Journal	Chromatographia
Volume	60
Issue number	7-8
DOIs	https://doi.org/10.1365/s10337-004-0410-x
State	Published - Oct 2004

Keywords

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

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@article{03c8d0462b3a42ee83287dfa9005cf0f,

title = "Rapid screening of drug absorption potential using the immobilized artificial membrane phosphatidylcholine column and molar volume",

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 (k IAM/MWn). 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 k IAM/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.",

keywords = "Column liquid chromatography, High throughput screening, Immobilized artificial membrane, Molar volume, Oral absorption potential",

author = "Yoon, \{C. H.\} and Shin, \{B. S.\} and Chang, \{H. S.\} and Kwon, \{L. S.\} and Kim, \{H. Y.\} and Yoo, \{S. E.\} and Yoo, \{S. D.\}",

year = "2004",

month = oct,

doi = "10.1365/s10337-004-0410-x",

language = "English",

volume = "60",

pages = "399--404",

journal = "Chromatographia",

issn = "0009-5893",

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number = "7-8",

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TY - JOUR

T1 - Rapid screening of drug absorption potential using the immobilized artificial membrane phosphatidylcholine column and molar volume

AU - Yoon, C. H.

AU - Shin, B. S.

AU - Chang, H. S.

AU - Kwon, L. S.

AU - Kim, H. Y.

AU - Yoo, S. E.

AU - Yoo, S. D.

PY - 2004/10

Y1 - 2004/10

N2 - 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 (k IAM/MWn). 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 k IAM/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.

AB - 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 (k IAM/MWn). 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 k IAM/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.

KW - Column liquid chromatography

KW - High throughput screening

KW - Immobilized artificial membrane

KW - Molar volume

KW - Oral absorption potential

UR - https://www.scopus.com/pages/publications/7744228108

U2 - 10.1365/s10337-004-0410-x

DO - 10.1365/s10337-004-0410-x

M3 - Article

AN - SCOPUS:7744228108

SN - 0009-5893

VL - 60

SP - 399

EP - 404

JO - Chromatographia

JF - Chromatographia

IS - 7-8

ER -

Rapid screening of drug absorption potential using the immobilized artificial membrane phosphatidylcholine column and molar volume

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Keywords

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