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The Use of Metabolism Versus Partition Coefficient in Predicting Human Intestinal Permeability Classification


Authored by Nasir Idkaidek

Aim: The aim of this review commentary is to compare measured permeability class versus predicted one using metabolism and partition coefficient values for WHO essential drugs list.
Methods: Predicted permeability classes were based on partition coefficient or metabolism. Comparisons were then done against measured permeability classes.
Results and discussion: Predictions were close to measured permeability classes for many drugs using all prediction methods using metoprolol coefficients as reference marker and high extraction ratio for high permeability. However, some false negative and false positive predictions were observed. This can lead to wrong permeability classification and hence wrong biopharmaceutics classification (BCS). The best method with least false predictions in the studied compounds was using more than 90% metabolism as indicator of high permeability, Hence it is suggested to be used for better permeability classification prediction.

 

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