Über die Beziehungen zwischen der Lipidlöslichkeit von Pharmaka und ihrem pharmakokinetischen Verhalten

Summary

Some correlations between the physicochemical properties of drugs and their pharmacokinetic behaviour are outlined. Based on the permeability characteristics of simple model membranes (porous membrane, lipid membrane) permeation and distribution of drugs in the animal body can be described and understood on simple physico-chemical terms. Some clinically important aspects — the absorption of drugs from the intestinal tract, the passage through the blood-brain-barrier and the renal excretion as governed by passive tubular reabsorption — are discussed in more detail. Thereby it appears that the solubility of a drug in lipid material, which may be suitably expressed as partition coefficient between an organic solvent and a buffer solution of pH 7.4, is a major factor in determining its pharmacokinetic behaviour.