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Effect of Micronization on the Bioavailability and Pharmacologic Activity of Spironolactone
Author(s) -
McINNES GORDON T.,
ASBURY MICHAEL J.,
RAMSAY LAWRENCE E.,
SHELTON JOHN R.,
HARRISON IAN R.
Publication year - 1982
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1982.tb02694.x
Subject(s) - bioavailability , spironolactone , micronization , pharmacology , urine , particle size , active metabolite , chemistry , pharmacokinetics , chromatography , medicine , aldosterone
The bioavailability and pharmacologic activity of tablets containing micronized spironolactone chemical (median particle size 2.21 μm) were compared to those of tablets made from standard spironolactone chemical (median particle size 78.8 μm) in healthy men. Apart from particle size, all features of these tablets were identical. After 200‐mg single doses, the bioavailability of micronized tablets was significantly higher than that of standard tablets. Furthermore, as assessed by 24‐hour urine log 10 10 Na/K ratio, the pharmacologic activity of micronized spironolactone was significantly greater than that of the standard formulation. The significant influence on renal antimineralocorticoid activity of raised plasma and urinary levels of canrenone, quantitatively the major active metabolite of spironolactone in man, emphasizes the clinical importance of the bioavailability of spironolactone preparations. Since this study, the process used in the manufacture of spironolactone (Aldactone) tablets has been under review.