Comparison of mucosal drug conjugative rates along the gastrointestinal tract of female sheep.

The comparative distribution of p-nitrophenol UDP-glucuronosyl-transferase, 1-chloro-2,4-dinitrobenzene glutathione-S-transferase and sulphamethazine N-acetyltransferase activities was studied along the gastrointestinal mucosa of female Lacaune sheep. Gastrointestinal mucosa was characterized by a very low and unequal N-acetyltransferase activity when activities were expressed per g of wet organ. The duodenum contained highest activities (4.1 nmol/g min). When results were expressed per mg of cytosolic protein, the duodenal activity (0.64 nmol/mg min) was sixfold higher than in liver (0.11 nmol/mg min). There was a lack in N-acetyltransferase activity accepting isoniazid as substrate. Glucuronosyltransferase activity was approximately threefold higher in microsomal fractions of the mucosal lining of gastric and colonic intestine (0.43-0.58 nmol/g min) than in small intestine or caecum (0.10-0.26 nmol/mg min). Concerning cytosolic glutathione S-transferase activity, two- to threefold higher activities were obtained in omasum, jejunum, duodenum and ileum (1021-2164 nmol/g min) than in other parts (341-799 nmol/g min) when results were expressed per g of wet organ. These data were compared with corresponding hepatic activities determined in the same six female sheep.