The Small Intestine and Secretions Relevant to Drug Absorption

3 The Small Intestine and Secretions Relevant to Drug Absorption 

Pancreatic fluid, secreted in the duodenum is composed of digestive enzymes and bicarbonate. The two major pancreatic proteases are the serine proteases trypsin and chymotrypsin. 

FIGURE 1.2 Schematic cross section of the small intestine wall. 

Their mode of appearance in the lumen of the intestine is rather complicated and involves activation of trypsinogen secretion by enterokinase. Once trypsin is formed it activates chymotrypsinogen. Pancreatic lipase is also secreted into the lumen with the pancreatic fluid. The digestion process of fatty acids by their lipase-mediated hydrolysis is completed by bile salts, which are also secreted in the duodenum and are crucial for micellization of lipophilic compounds. The micelles formed in the duodenum enable the absorption of hydro-phobic drugs such as steroids. They pose, however, a serious constraint for the stability of drug delivery carriers such as liposomes and emulsions. 

The major saccharidase of the small intestine is amylase that digests starch to the disaccharide maltose and the trisaccharide maltotriose. Intestinal mucus is secreted by goblet cells, which either ooze (constitutive basal secretion) or burst as a result of stimuli. In the last mode of secretion condensed mucus gel granules can expand 500-fold within 20 ms [20]. 

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