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Multiple‐Dose Pharmacokinetics of Nilvadipine in Healthy Volunteers
Author(s) -
Terakawa Masetto,
Tokuma Yoji,
Kuwahara Noriyasu,
Shishido Akira,
Noguchi Hideyo
Publication year - 1988
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.1552-4604.1988.tb03157.x
Subject(s) - pharmacokinetics , dosing , chemistry , steady state (chemistry) , pharmacology , oral administration , medicine
Nilvadipine, a new antihypertensive and antianginal drug, was studied in six healthy male volunteers to evaluate its steady‐state pharmacokinetics after oral dosing. The subjects were given a single dose of 4 mg, followed by 4 mg every 12 hours for six days after a washout period of more than 3 days. The pharmacokinetics of nilvadipine were well described by a linear model of triexponential equation with zero‐order absorption. The steady state was reached by the fourth day of multiple dosing, with a twofold accumulation of trough plasma concentration and no accumulation of peak concentration. The mean plasma concentration at steady state was 1.0 ng/mL. The optical enantiomers of nilvadipine were also determined in the plasma. The plasma concentration of (+)‐nilvadipine was about two and a half times higher than that of (‐)‐nilvadipine, and this ratio was unaffected by multiple dosing.