The A In Adme

In this book we will focus on physicochemical profiling in support of improved prediction methods for absorption, the "A" in ADME. Metabolism and other components of ADME will be beyond the scope of this book. Furthermore, we will focus on properties related to passive absorption, and not directly consider active transport mechanisms. The most important physicochemical parameters associated with passive absorption are acid-base character (which determines the charge state of a molecule in a solution of a particular pH), lipophilicity (which determines distribution of a molecule between the aqueous and the lipid environments), solubility (which limits the concentration that a dosage form of a molecule can present to the solution and the rate at which the molecule dissolves from the solid form), and membrane permeability (which determines how quickly molecules can cross membrane barriers). Current state of the art in measurement of these properties, as the ever important function of pH, will be surveyed, and in some cases (permeability), described in detail.

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