caa a22 4500 477056784 CHVBK 20180405111348.0 cr unu---uuuuu 170330e19961001xx s 000 0 eng 10.1007/s002280050182 doi (NATIONALLICENCE)springer-10.1007/s002280050182 Absolute bioavailability of oral immediate and slow release fluphenazine in healthy volunteers [Elektronische Daten] [R. Koytchev, R.-G. Alken, G. McKay, T. Katzarov] Objective: The present study was conducted with the aim of investigating the absolute bioavailability of fluphenazine in healthy volunteers after administration of immediate and slow release oral formulations. Methods: The oral dose was 12 mg fluphenazine hydrochloride. The intravenous bolus dose was 2.5 mg. Fourteen healthy volunteers of both sexes were enrolled in this randomised, crossover trial. Twelve volunteers completed the trial according to protocol. Results: The concentration maxima after administration of the slow release formulation were approximately half those measured after the immediate release formulation and were recorded later by a factor of 2 (immediate release: Cmax = 2.3 ng⋅ml−1, tmax = 2.8 h; slow release: Cmax = 1.2 ng⋅ml−1, tmax = 4.6 h). The concentrations measured 10 min after intravenous bolus administration of 2.5 mg fluphenazine hydrochloride were approximately 100 times higher (261 ng⋅ml−1). The geometric means for the absolute bioavailability of fluphenazine were 2.7% for the immediate release formulation and 3.4% for the slow release formulation. The absolute bioavailability of fluphenazine is thus much lower than previously generally accepted. Springer-Verlag Berlin Heidelberg, 1996 Key words Fluphenazine nationallicence bioavailability nationallicence human nationallicence slow release formulation nationallicence Koytchev R. Cooperative Clinical Drug Research and Development, Waldstrasse 23-24, D-13403 Berlin, Germany, DE aut Alken R.-G Cooperative Clinical Drug Research and Development, Waldstrasse 23-24, D-13403 Berlin, Germany, DE aut McKay G. College of Pharmacy, University of Saskatchewan, Saskatoon, Saskatchewan, Canada, CA aut Katzarov T. National Oncological Centre, Sofia, Bulgaria, BG aut https://doi.org/10.1007/s002280050182 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s002280050182 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Koytchev R. Cooperative Clinical Drug Research and Development, Waldstrasse 23-24, D-13403 Berlin, Germany, DE aut NATIONALLICENCE 700 1- Alken R.-G Cooperative Clinical Drug Research and Development, Waldstrasse 23-24, D-13403 Berlin, Germany, DE aut NATIONALLICENCE 700 1- McKay G. College of Pharmacy, University of Saskatchewan, Saskatoon, Saskatchewan, Canada, CA aut NATIONALLICENCE 700 1- Katzarov T. National Oncological Centre, Sofia, Bulgaria, BG aut Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer