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Ranitidine bioavailability and kinetics in normal male subjects
Author(s) -
Garg Dyal C,
Weidler Donald J,
Eshelman Fred N
Publication year - 1983
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1983.60
Subject(s) - ranitidine , bioavailability , chemistry , histamine , pharmacology , volume of distribution , pharmacokinetics , pentagastrin , crossover study , urine , oral administration , volunteer , endocrinology , stomach , medicine , gastric acid , biochemistry , agronomy , biology , alternative medicine , pathology , placebo
Ranitidine is a potent histamine H 2 ‐receptor blocker that inhibits histamine‐ and pentagastrin‐induced gastric acid secretion. After doses of 100 mg both intravenously and orally ranitidine kinetics and bioavailability were investigated in a single dose two‐way crossover study in 12 normal men. Serum concentrations of ranitidine were determined by radioimmunoassay and urine concentrations by an ion‐pair HPLC method. Intravenous data were fitted to exponential equations with the computer program NONLIN; model‐independent kinetic parameters were calculated. Elimination t½, plasma clearance, renal clearance, hepatic clearance, and volume of distribution for ranitidine after intravenous injection were 2 hr, 10.4 ml/(min × kg), 7.2 ml/(min × kg), 3.1 ml/(min × kg), and 1.82 l/kg, respectively; after oral doses mean t½ was 2.7 hr and mean bioavailability was 52%. The average cumulative urinary‐excretion of ranitidine as percent of dose was 69.4 ± 6.1% and 26.7 ± 7.2% after intravenous and oral doses. Clinical Pharmacology and Therapeutics (1983) 33, 445–452; doi: 10.1038/clpt.1983.60