Bioavailability of nifedipine from different oral dosage forms in healthy volunteers

The absolute and relative bioavailability of nifedipine (1) from different formulations administered as single oral doses in healthy volunteers was determined. Serum concentrations of 1 were measured by GC. The absolute bioavailability of 1 was 53% because of presystemic metabolism. The bioavailabil...

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Bibliographic Details
Published inPharmazie Vol. 44; no. 5; p. 336
Main Authors Leucuţa, S E, Vida-Simiti, L, Căprioară, M G, Făgărăşan, E, Olinic, N, Manasia, M, Vlaicu, R
Format Journal Article
LanguageEnglish
Published Germany 01.05.1989
Subjects
Administration, Oral
Adult
Biological Availability
Biopharmaceutics
Capsules
Chemistry, Pharmaceutical
Female
Humans
Injections, Intravenous
Male
Nifedipine - administration & dosage
Nifedipine - pharmacokinetics
Reference Values
Solubility
Tablets
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Summary:The absolute and relative bioavailability of nifedipine (1) from different formulations administered as single oral doses in healthy volunteers was determined. Serum concentrations of 1 were measured by GC. The absolute bioavailability of 1 was 53% because of presystemic metabolism. The bioavailability of Adalat (Bayer) tablets, Nifedipina (Terapia) and Corinfar (VEB Arzneimittelwerk Dresden) sugar-coated tablets was 93%, 92% and 86% (respectively) as compared with Adalat capsules. The AUC were not significantly different. The Cmax and tmax values were different, indicating that the absorption of 1 showed differences in first-order rate constants of dissolution in the above mentioned order. Despite the differences among the formulations studied, each preparation may have its merits. In a multiple dose regimen of 20 mg 1 (Nifedipina, Terapia) t.i.d., minimal therapeutic drug levels were achieved and maintained during steady state, from the 1st d of treatment.
ISSN:0031-7144