Absolute oral bioavailability and metabolic turnover of β-sitosterol in healthy subjects

Duchateau, Guus, Cochrane, Brett, Windebank, Sam , Herudzinska, Justyna, Sanghera, Davindera, Burian, Angela, Muller, Markus, Zeitlinger, Markus and Lappin, Graham (2012) Absolute oral bioavailability and metabolic turnover of β-sitosterol in healthy subjects. Drug Metabolism and Disposition, 40 (10). pp. 2026-2030. ISSN 0090-9556

Full content URL: http://dmd.aspetjournals.org/content/40/10/2026

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The metabolic turnover, absolute oral bioavailability, clearance, and volume of distribution for β-sitosterol were measured in healthy subjects. [14C]β-Sitosterol was used as an isotopic tracer to distinguish pulse doses from dietary sources and was administered by both oral and intravenous routes. The administered doses of [14C]β-sitosterol were in the region of 3 to 4 μg, sufficiently low as not to perturb the kinetics of β-sitosterol derived from the diet. Because the plasma concentrations of [14C]β-sitosterol arising from such low doses were anticipated to be very low, the ultrasensitive isotope ratio analytical method of accelerator mass spectrometry was used. The limit of quantification for [14C]β-sitosterol was approximately 0.1 pg/ml, the oral absolute bioavailability was just 0.41%, clearance was 85 ml/h, volume of distribution was 46 L, and the turnover was 5.8 mg/day. Given the steady-state concentrations of β-sitosterol (2.83 μg/ml), then the dietary load was calculated to be approximately 1400 mg/day

Keywords:Microdosing, Absolute oral bioavailability, Metabolic turnover, Accelerator mass spectrometry
Subjects:B Subjects allied to Medicine > B230 Pharmacy
Divisions:College of Science > School of Pharmacy
ID Code:7361
Deposited On:27 Feb 2013 17:29

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