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Plasma concentrations and pharmacokinetics of dihydralazine after single oral doses to human subjects
Author(s) -
Waller A. R.,
Chasseaud L. F.,
Taylor T.,
Darragh A.,
O'Kelly D. A.
Publication year - 1979
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510010203
Subject(s) - pharmacokinetics , pharmacology , oral dose , human plasma , oral administration , medicine , plasma concentration , chemistry , chromatography
After single oral doses of 20 mg of a suspension of dihydralazine sulphate to human subjects, the peak of mean plasma concentrations of dihydralazine of 47·0 ng ml −1 ± 11·0 standard deviation (S.D.) ( n = 7) was reached at 1 h. Mean concentrations declined biphasically with apparent half‐lives of 0·57 and 4·96 h respectively. Dihydralazine was partly converted to hydralazine. The peak of mean plasma concentrations of the latter drug of 3·9 ng ml −1 ± 1·7 S.D. (n = 7) occurred at 1–2 h after dosing with dihydralazine sulphate and declined to 1–5 ng ml −1 ± 1·5 S.D. at 6 h. Of the seven subjects studied, three were classified as fast and four as slow acetylators. Mean clearances appeared to be slightly more rapid in fast acetylators (1·63 1 min −1 ± 0·32 S.D.) when compared to slow acetylators (1·31 1 min −1 ± 0·31 S.D.) but this difference and differences in plasma concentrations and in areas under the plasma drug concentration‐time curves were not significant (p > 0·1).