Abstract
The purpose of the present study was to examine a correlation between the human intestinal permeability ( P eff) and the bio-mimetic artificial membrane permeability corrected by the paracellular pathway model based on the Renkin function ( P PAMPA-PP-RF) and to construct a prediction scheme. The effect of the unstirred water layer was incorporated to the prediction scheme. Eighteen P eff values of passively absorbed drugs were employed for the analysis. The correlation coefficient (CC) between the predicted and observed log P eff was 0.91. P eff of furosemide, hydrochlorothiazide and creatinine were underestimated by P PAMPA-PP-RF. When these compounds were excluded, CC was 0.97. Without the correction for the paracellular pathway, P eff of small, cationic and hydrophilic compounds were underestimated. Therefore, P PAMPA-PP-RF was found to be an adequate in vitro surrogate for P eff.
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