Intestinal drug absorption prediction

Stenberg, P., Norinder, U., Luthman, K., Artursson, P. Experimental and computational screening models for the prediction of intestinal drug absorption. 

Fig. 5.2. Two-step process for evaluation of intestinal drug absorption. The first step represents the prediction of intestinal permeability (e.g., over Caco-2 monolayers) from in-silico models or from physico-chemical...

Fig. 7.5. The Biopharmaceutics Classification System (BCS) provides a scientific basis for predicting intestinal drug absorption and for identifying the rate-limiting step based on primary biopharmaceutical properties such as solubility and effective intestinal permeability (Pefr). BCS serves as a product control instrument. The BCS divides drugs into four different classes based on their solubility and...

Let us conclude this section by proposing that provided that the drug is sufficiently soluble in the gastrointestinal fluids, the complex process of intestinal drug absorption can often be satisfactorily described by focusing on passive transport across the cell membrane, and that the development of models that predict passive transcellular permeability is particularly important. Such models are the focus of the remaining part of this chapter. 

Cao XH, Gibbs ST, Fang LY, Miller HA, Landowski CP, Shin HC, Lennernas H, Zhong YQ, Amidon GL, Yu LX and Sun DX (2006) Why Is It Challenging to Predict Intestinal Drug Absorption and Oral Bio availability in Human Using Rat Models. Pharm Res 23 pp 1675-1686. 

Shah P, Jogani V, Bagchi T, Misra A (2006) Role of Caco-2 cell monolayers in prediction of intestinal drug absorption. Biotechnol Prog 22 186-198... 

Caco-2 cells, especially the human intestinal epithelial cell line, have been proposed and used for the simulation and prediction of intestinal drug absorption after oral administration. These membranes of cells have useful properties for correlation with in vivo data such as enzymatic and transporter systems [24]. 

Palm. K., Artursson. P. and Luthmann, K. Experimental and Theoretical Predictions of Intestinal Drug Absorption. In Computer-Assisted Lead Finding and Optimization Current Tools for Medicinal Chemistry, Eds van de Waterbeemd, H., Testa, B. and Folkers, G., Wiley-VCH, Weinheim, 1997, pp. 277-289. 

Waterbeemd, H. V. (2000), Intestinal permeability Prediction from theory, in Oral Drug Absorption Prediction and Assessment, Marcel Dekker, New York, pp. 31-49. 

Badhan, R. et al., Methodology for development of a physiological model incorporating CYP3A and P-glycoprotein for the prediction of intestinal drug absorption, J. Pharm. Sci., 98(6), 2180, 2009. 

Physiological Factors and Experimental Parameters Influencing the Accuracy of Predictions of Intestinal Drug Absorption... 

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