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Furosemide Pharmacokinetics and Pharmacodynamics following Gastroretentive Dosage Form Administration to Healthy Volunteers

From the Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, Hebrew University of Jerusalem, Israel (Mr. Klausner, Dr. Stepensky, Dr. Friedman, Dr. Hoffman); the Clinical Sciences Department, School of Veterinary Medicine, Hebrew University of Jerusalem, Israel (Dr. Lavy); and the Department of Radiology, National Medical Center, Budapest, Hungary (Dr. Cserepes, Dr. Barta).

The objective of this study was to evaluate the pharmacokinetic and pharmacodynamic properties of furosemide following gastroretentive dosage form (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 the GRDF administration, as compared to the tablet, showed lower C_max and indicated a prolonged absorption phase leading to longer mean residence time in the stomach. The sustained input of the drug significantly improved diuretic and natriuretic efficiencies during the first 5 hours and thereby increased the total effects measured over 24 hours. The unfolding controlled-release GRDF of furosemide improved the pharmacodynamic actions due to the sustained absorption in the stomach and jejunum, which delayed the body's counteractivity to the drug effect.

Key Words: Furosemide • gastroretentive • humans • pharmacokinetics • pharmacodynamics • controlled release

Address for reprints: Professor Amnon Hoffman, Department of Pharmaceutics, School of Pharmacy, Hebrew University of Jerusalem, P.O. Box 12065, Jerusalem 91120, Israel.