2003
DOI: 10.1177/0091270003254575
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Furosemide Pharmacokinetics and Pharmacodynamics following Gastroretentive Dosage Form Administration to Healthy Volunteers

Abstract: The objective of this study was to evaluate the pharmacokinetic and pharmacodynamic properties of furosemide following gastroretentive dosage from (GRDF) administration. A furosemide (60 mg) GRDF, releasing the drug during 6 hours in vitro, or an immediate-release tablet was administered to healthy male volunteers (N = 14) in a crossover design. Food and liquid intake were standardized; urine was collected, weighed, and assayed for furosemide and sodium concentrations. Pharmacokinetics of furosemide following … Show more

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Cited by 51 publications
(22 citation statements)
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“…The bioequivalence of the two products could be satisfactorily concluded based on the experimental data. Determined pharmacokinetic parameters are in fair agreement with previously published data [26][27][28][29][30][31].…”
Section: Application To a Bioanalytical Studysupporting
confidence: 88%
“…The bioequivalence of the two products could be satisfactorily concluded based on the experimental data. Determined pharmacokinetic parameters are in fair agreement with previously published data [26][27][28][29][30][31].…”
Section: Application To a Bioanalytical Studysupporting
confidence: 88%
“…Therefore, the use of tolerance models to describe the pharmacodynamics of torasemide was meaningful. Tolerance phenomenon has already been observed with furosemide in both animals (Hammarlund & Paalzow, ; Li et al ., ; Uechi et al ., ; Hori et al ., ) and humans (Hammarlund et al ., ; Wakelkamp et al ., ; ‐ Wakelkamp et al ., ; Klausner et al ., ). To the best of our knowledge, acute tolerance phenomenon for torasemide in the dog has never been described before.…”
Section: Discussionmentioning
confidence: 97%
“…Furosemide is absorbed mainly in the stomach and upper small intestine 95 due to its weak acidic properties (pKa 3.9). This narrow absorption window of furosemide is the major cause of its low oral bioavailability 96. The feasibility of widening the absorption window for furosemide has been demonstrated by controlling the pH in the distal portions of the GIT through the co‐administration of Eudragit ® L100‐55 97.…”
Section: Approaches Directed Towards Gastrointestinal Factorsmentioning
confidence: 99%
“…P‐glycoprotein (P‐gp) is a type of ATPase, and an energy‐dependent transmembrane drug efflux pump which belongs to members of ATPase Binding Cassette (ABC) transporters 131. It is a 1280 long amino acid glycoprotein with a molecular weight of 170 kDa, expressed as a single chain containing two homologous portions of equal length, each containing six membrane domains and two ATP binding regions separated by a flexible linker polypeptide region between the Walker A and B motifs 96, 132. Immunohistochemical analysis using monoclonal antibodies provided evidence for localization of P‐gp in a wide range of tissues, particularly in columnar epithelial cells of the lower GIT, capillary endothelial cells of the brain and testes, canalicular surface of hepatocytes and apical surface of the proximal tubule in the kidney 133.…”
Section: Approaches Directed Towards Gastrointestinal Factorsmentioning
confidence: 99%