Composition and Physicochemical Properties of Fasted-State Human Duodenal and Jejunal Fluid: A Critical Evaluation of the Available Data

Various methods of sampling and analyzing intestinal fluids have been applied over the years. In this report, data that have been published to date about the composition of fasted-state human intestinal fluid (HIF) and its physicochemical properties are summarized and the influence of the methods used to generate the data is discussed. Key physiological parameters summarized include pH, buffer capacity, osmolarity, and ionic strength in both the fasted duodenum and jejunum. Furthermore, the bile salts and phospholipids in the fasted small intestine are addressed in terms of both qualitative and quantitative composition with respect to the different types and degrees of hydroxylation of bile salts. Taurocholate, glycocholate, and glycochenodeoxycholate were identified as the main bile salts. Lysolecithin was identified as the predominant phospholipid species in fasted HIF because of the enzymatic degradation of lecithin. Together with other intestinal surfactants, such as cholesterol and free fatty acids, the influence of bile acids and phospholipids on the surface tension of fasted HIF was evaluated. A good working knowledge of all the above-mentioned parameters is important to optimize the composition of biorelevant media, with a view to improving the prediction of in vivo dissolution and release performance of drugs and dosage forms. (c) 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:3398-3411, 2014