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Enteral absorption of octreotide
G Fricker1, J Drewe, J Vonderscher
1Drug Delivery Systems, Sandoz Pharma Ltd., Basel, Switzerland.
British Journal of Pharmacology
|April 1, 1992
Summary
Octreotide, a somatostatin analogue, is absorbed intact in the small intestine, particularly the jejunum. Bile negatively impacts octreotide absorption, suggesting complex gastrointestinal peptide uptake mechanisms.
Area of Science:
- Pharmacology
- Gastroenterology
- Biochemistry
Background:
- Octreotide is a somatostatin analogue used clinically.
- Understanding its gastrointestinal absorption is crucial for optimizing drug delivery.
- Previous studies suggested oral absorption of octreotide.
Purpose of the Study:
- To investigate the in situ absorption of octreotide in the gastrointestinal tract.
- To identify preferential absorption sites for octreotide in the small intestine.
- To elucidate the mechanisms underlying octreotide absorption and the influence of bile.
Main Methods:
- In situ absorption experiments in rats.
- Intubation studies in human volunteers.
- Experiments with bile-duct cannulated rats.
- Uptake experiments using rat jejunal brush border membrane vesicles.
Main Results:
- Octreotide is absorbed intact from the gastrointestinal tract.
- The jejunum demonstrated higher octreotide absorption compared to the duodenum and ileum.
- Bile significantly decreased octreotide absorption.
- Octreotide uptake into jejunal brush border membranes exhibited saturable kinetics, indicating carrier-mediated transport.
Conclusions:
- Octreotide absorption is site-specific within the small intestine, favoring the jejunum.
- Biliary components inhibit octreotide absorption.
- Octreotide absorption involves saturable, likely carrier-mediated, transport mechanisms in the jejunum.