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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Abstract

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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