| Intestinal absorption kinetics of amiodarone in rat small intestine. | |
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MedLine Citation:
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PMID: 9267684 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Amiodarone is a widely used antiarrhythmic agent with highly variable therapeutic effects. These seem to be related, at least in part, to the pharmacokinetics of the drug and particularly to some features of its gastrointestinal absorption process. The drug exhibits physico-chemical properties highly suitable for diffusion across lipophilic absorbing membranes, but its low aqueous solubility can act as the rate limiting step for absorption, making the process erratic and variable. In order to gain an insight into the intestinal absorption mechanism of the drug and detect possible non-linearities, a series of experiments using a classical rat gut in situ preparation were carried out with three amiodarone hydrochloride solutions (10, 75, and 200 micrograms mL-1). A synthetic non-ionic surfactant, polysorbate 80, at supramicellar concentration (2 mM) was used as the drug solubilizer. Amiodarone was assayed in biological samples by HPLC using a rapid, sensitive technique that was validated. The amiodarone first-order absorption rate constants obtained in these conditions were similar. No significant differences between ka values were found. Amiodarone absorption was clearly identified as a passive diffusion process. |
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Authors:
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R V Martín-Algarra; R M Pascual-Costa; M Merino; V G Casabó |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Biopharmaceutics & drug disposition Volume: 18 ISSN: 0142-2782 ISO Abbreviation: Biopharm Drug Dispos Publication Date: 1997 Aug |
Date Detail:
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Created Date: 1997-10-02 Completed Date: 1997-10-02 Revised Date: 2003-11-14 |
Medline Journal Info:
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Nlm Unique ID: 7911226 Medline TA: Biopharm Drug Dispos Country: ENGLAND |
Other Details:
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Languages: eng Pagination: 523-32 Citation Subset: IM |
Affiliation:
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Departamento de Farmacia y Tecnologia Farmacéutica, Facultad de Farmacia, Universidad de Valencia, Spain. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Amiodarone / administration & dosage, blood, pharmacokinetics* Animals Anti-Arrhythmia Agents / administration & dosage, blood, pharmacokinetics* Diffusion Intestinal Absorption / physiology Intestine, Small / metabolism* Male Polysorbates Rats Rats, Wistar Reproducibility of Results Solubility Water / metabolism |
| Chemical | |
Reg. No./Substance:
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0/Anti-Arrhythmia Agents; 0/Polysorbates; 1951-25-3/Amiodarone; 7732-18-5/Water |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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