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Intestinal absorption of amiodarone in man
1INSERM U.290, Hôpital Saint-Lazare, Paris, France.
Journal of Clinical Pharmacology
|July 1, 1990
Summary
This study investigated amiodarone absorption in the jejunum. Lipid content significantly influenced drug absorption, but plasma levels were mainly affected by tissue distribution and metabolism.
Area of Science:
- Gastroenterology
- Pharmacokinetics
- Drug Absorption
Background:
- Amiodarone is an antiarrhythmic drug with variable oral bioavailability.
- Lipid content in intestinal solutions can affect drug absorption.
- Understanding amiodarone jejunal absorption is crucial for optimizing therapeutic outcomes.
Purpose of the Study:
- To determine the jejunal absorption rate of amiodarone.
- To evaluate the influence of varying lipid and caloric loads on amiodarone absorption.
- To elucidate factors contributing to amiodarone pharmacokinetic variability.
Main Methods:
- Human volunteers underwent intestinal perfusion using a nutrient solution containing 300 mg amiodarone.
- Two solutions with different caloric and lipid loads (3.3 Kcal/min and 1.3 Kcal/min) were infused into a 25 cm jejunal segment.
- Amiodarone absorption rate and lipid absorption were measured.
Main Results:
- Jejunal absorption of amiodarone ranged from 20.2% to 31.7% with the higher caloric load (solution A).
- Amiodarone absorption showed a significant positive correlation with lipid absorption.
- Maximal plasma concentrations and AUC/24 hours did not correlate with the absorbed amiodarone amount.
Conclusions:
- Lipid content significantly impacts amiodarone jejunal absorption.
- Pharmacokinetic variability of amiodarone is primarily driven by tissue distribution and metabolic pathways, not solely by absorption.
- Further research into amiodarone tissue kinetics is warranted.
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