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Intestinal Sorption of Anisotropine Methylbromide in the Rat

The uptake into the circulation and the binding of anisotropine methylbromide to the intestine and the residuum in the intestinal lumen were studied in rats using the acute in vivo intestinal loop technique. The presence of food in the intestine decreases the uptake rate but has no effect on the tot...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1972-08, Vol.61 (8), p.1223-1227
Main Authors: Pfeffer, Morris, Schor, Joseph M.
Format: Article
Language:English
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Summary:The uptake into the circulation and the binding of anisotropine methylbromide to the intestine and the residuum in the intestinal lumen were studied in rats using the acute in vivo intestinal loop technique. The presence of food in the intestine decreases the uptake rate but has no effect on the total uptake. The sum of drug bound to intestinal tissue and that taken into the circulation, over the concentration range studied, is a constant 48% of the dose administered. Tissue binding is describable by a Langmuir adsorption isotherm. In vitro everted intestinal sac experiments confirm the extent of this binding. The material bound to the intestinal wall is released into the lumen of the gut and is unavailable for circulatory uptake. There are gradients for both intestinal binding and circulatory uptake, both generally being greater in the anterior portion of the small intestine and decreasing in the posterior portion. Neither binding nor uptake is correlated with the quantity of protein in the intestinal tissue. Bile does not affect circulatory uptake but decreases binding. There is no evidence for the existence of a saturable transport process effecting the sorption of this drug.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600610811