Pharmacokinetic Concepts in Brain Drug Delivery

摘要: This chapter presents the pharmacokinetic principles of blood–brain barrier (BBB) transport and intra-brain distribution drugs in order to provide a basis for understanding drug delivery brain from clinically relevant perspective. The most important concentrations measure when determining are those unbound drug, because it is that causes pharmacological effect by interacting with target. Therefore, this also discusses basis, kind information provided, vivo relevance methods used obtain reliable, therapeutically useful estimates delivery. main factors governing permeability BBB (influx clearance), extent nonspecific binding tissue, efflux clearance drug. ratio influx clearances provides an estimation equilibration across BBB, described K p,uu,brain. parameter important, as active uptake and/or transporters influence absolute relation plasma. advantage using p,uu,brain during discovery process lies its ability predict potential success intended action within or, conversely, few or no side effects brain.