PCL201H1 Lecture 8: Lecture 8 Absorption Mechanisms

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11 Apr 2012
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Aquaporin channels: most allow only water but a-3 allows small water soluble molecules, pore width ~8-10 angstroms, therefore allows hydrophilic molecules <200da passage, only small molecules, diffusion, high concentration to low concentration via passive diffusion. Remember compounds that are hydrophilic have low pow. Increased molecular size, decreased permeation rate (ability of molecule to cross membrane) Lipid soluble drugs diffuse across lipid molecules of membrane. Rate of diffusion depends on: concentration of drug, pow, degree of ionization, surface area of membrane (stomach vs. small intestine) Concentration of drug and the diffusion across the membrane is not always linear: major issue with regulating drug dosage, can not always assume linear relationship. Role of pow partition coefficient major factor with regards to drug absorption. Ideally the higher pow the more rapidly absorbed. Review: optimum value for drug abosprtion due to hydrophilic barrier associated with glycocalyx: cut off phenomenon: very lipophillic reduced absorption unable to cross stagnant water layer.

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