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The gastrointestinal uptake of macrocyclic compounds is not fully understood. Here we applied our previously validated integrated system based on machine learning and conformal prediction to predict the passive fraction absorbed (f

The blood-brain barrier is often perceived as relatively impermeable, and various cut-off values for zero or limited brain permeability have been suggested. The validity of these values has been evaluated in this review. The barrier appears to have a very high permeability and absorptive capacity: sufficient to absorb compounds with polar surface area270 A(2), molecular weight1,000 Da, log D-3.5 and equilibrium brain-to-blood concentration ratio0.01 well. Sufficient intestinal uptake indicates good passive brain uptake potential. The uptake is potentially more sensitive to involvement and changes of active transport than in the intestines. A physiologically based in vitro-in vivo method for prediction of brain uptake is presented.

EXPERIMENTAL ESTIMATION OF THE EFFECTIVE UNSTIRRED WATER LAYER THICKNESS IN THE HUMAN JEJUNUM, AND ITS IMPORTANCE IN ORAL-DRUG ABSORPTION