Pharmacokinetics of vibunazole (BAY n 7133) administered orally to healthy subjects

The role of gastric acidity in the absorption of the new antifungal drug vibunazole was studied in six healthy volunteers. Vibunazole was administered orally as 400 mg tablets to fasting subjects under three conditions: after 400 mg cimetidine orally, after 30 ml diluted hydrochloric acid orally, an...

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Bibliographic Details
Published in:Journal of antimicrobial chemotherapy 1985-07, Vol.16 (1), p.75-79
Main Authors: van Gulpen, C., Kelder, O., Mattie, H., van der Meer, J. W. M., van't Wout, J.
Format: Article
Language:English
Subjects:
Administration, Oral
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal agents
Biological and medical sciences
Female
Gastric Juice - physiology
Humans
Hydrogen-Ion Concentration
Intestinal Absorption
Male
Medical sciences
Metabolic Clearance Rate
Pharmacology. Drug treatments
Triazoles - administration & dosage
Triazoles - metabolism
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Summary:The role of gastric acidity in the absorption of the new antifungal drug vibunazole was studied in six healthy volunteers. Vibunazole was administered orally as 400 mg tablets to fasting subjects under three conditions: after 400 mg cimetidine orally, after 30 ml diluted hydrochloric acid orally, and alone. Plasma concentrations of vibunazole were determined with HPLC. The plasma concentration profile of vibunazole could be described adequately by a one-compartmental open model with first-order absorption. Kinetic parameters after oral administration did not differ between the three modes of administration. The mean peak time was 1 h 29 min (after lag-time). The mean peak concentration was 2·76 mg/l. The mean elimination half-life of vibunazole was 2h 22 min. The mean absorption lag-time was 30 min, with considerable variation.
ISSN:0305-7453
1460-2091
DOI:10.1093/jac/16.1.75