Research ArticlesEvaluation of human intestinal absorption data and subsequent derivation of a quantitative structure–activity relationship (QSAR) with the Abraham descriptors
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INTRODUCTION
The prediction of human intestinal absorption is a major goal in the design, optimization, and selection of candidates for the development of oral drugs. The focus of modern drug discovery is now not simply on the pharmacological activity, but also on seeking favorable absorption, distribution, metabolism, and excretion properties.1, 2, 3, 4 The growth in drug discovery of combinatorial chemistry methods, where large numbers of candidate compounds are synthesized and screened in parallel for in
Human Intestinal Absorption Data
The names of drug and drug‐like compounds and related data are listed in Table 1 and 2. The absorption data was collected and evaluated from 244 papers.1, 2, 3, 4, 5, 8, 9, 10, 11, 12, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 52, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96
Evaluation of Human Intestinal Absorption Data
Drug absorption is a complex process that is dependent on numerous biochemical, physiological, and physicochemical factors. In a thorough review of the subject, Sietsema 263 accurately points out that the terms absorption and bioavailability are often incorrectly and interchangeably used. Sietsema defined absorption as “the drug passing from the lumen of the gastrointestinal (GI) tract into the tissue of the GI tract. Once in the tissue, the drug is considered absorbed”.
Surveying the papers, it
Acknowledgements
Y. H. Zhao and J. Le are grateful to Glaxo Wellcome and Roche Products Ltd. for a postdoctoral research fellowship and a research studentship.
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