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Kinetics and bioavailability of two formulations of amiloride in man
Author(s) -
SMITH A. J.,
SMITH R. N.
Publication year - 1973
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1973.tb08252.x
Subject(s) - amiloride , chemistry , bioavailability , sodium , kinetics , pharmacokinetics , volume of distribution , chromatography , pharmacology , endocrinology , medicine , physics , organic chemistry , quantum mechanics
Summary1 Two formulations of [ 14 C]‐amiloride were compared in six oedema‐free subjects in single‐dose (20 mg) studies separated by a two‐week interval. 2 Calculation of the elimination rate constant (K e ), half‐life ( T ½) and apparent volume of distribution (V d ) from serum and urinary data showed no significant difference between the two formulations. The V d values (350 to 380 litres) were greater than total body fluid volume suggesting extravascular sequestration of amiloride. 3 Serum and urinary amiloride levels were similar with both formulations. Pharmacokinetic parameters were similar to those of an earlier report based on one formulation. 4 The calculated amiloride concentration in the renal distal tubule (3 μ m to 20 μ m ) was similar to, but higher than, reported in vitro concentrations of amiloride which reduced sodium transport in isolated membranes.