Characterising the behaviour of poorly water soluble drugs in the intestine: application of biorelevant media for solubility, dissolution and transport studies.

摘要: Objectives  Based on the knowledge of human intestinal fluids, compositions biorelevant media and their impact solubility, dissolution permeability studies poorly soluble drug compounds are discussed. Key findings  Human fluids show large variations with regard to composition pH, which complicate selection media. The influence concentration ratio bile salts, phospholipids hydrolysis products, such as monoglycerides free fatty acids, in well characterised media, a given provides valuable information behaviour intestine, thus enabling prediction in-vivo absorption. Summary  This review discusses implications compounds. Biorelevant contain salts when simulating fed state also acids. Solubility some drugs increase independently type surfactants included while others have higher solubility monoglyceride- acid-containing is independent log P (the octanol–water partition coefficient) drug. use improves correlation data, compared compendial although field complex this setting shows promise respect better absorption.