Premium
Multiple Dose Pharmacokinetics of Four Different Doses of Nisoldipine in Hypertensive Patients
Author(s) -
Chandler Mary H. H.,
Clifton G. Dennis,
Lettieri John T.,
Mazzu Arthur L.,
Allington Douglas R.,
Thieneman Andrew C.,
Foster Thomas S.,
Harrison Michael R.
Publication year - 1992
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 - 10.1177/009127009203200614
Subject(s) - nisoldipine , pharmacokinetics , area under the curve , medicine , pharmacology , oral administration , significant difference , chemistry , calcium , nifedipine
This randomized double‐blind parallel group study characterized the pharmacokinetics of the calcium channel antagonist, nisoidipine (core‐coat tablets), administered once daily for 7 days in doses of 5 mg (n = 12), 10 mg (n = 13), 20 mg (n = 12), and 30 mg (n = 11) to patients with mild to moderate hypertension. Serial blood samples were obtained from 0 to 24 hours and from 0 to 48 hours after nisoidipine administration on days 1 and 7, respectively. Nisoldipine plasma concentrations were determined by gas chromatography with electron capture detection. No statistically significant difference was found in dose‐normalized area under the curve between the four groups. Area under the curve (standardized to body weight) correlated to dose (r = .74, P < .05). No significant difference existed in oral clearance (L/h/kg) when analyzed for equivalence across the four doses: 8.21 ± 3.47 (5 mg), 11.84 ± 13.85 (10 mg), 11.48 ± 7.49 (20 mg), and 10.36 ± 5.49 (30 mg). The present investigation characterizes the pharmacokinetics of nisoidipine core‐coat tablets in hypertensive patients and demonstrates the dose proportionality or linearity of nisoidipine plasma concentrations and area under the curve, measured over a dose range of 5 to 30 mg.