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Drug Metabolism and Disposition Fast Forward
First published on November 3, 2008; DOI: 10.1124/dmd.107.020313


0090-9556/09/3702-352-358$20.00
DMD 37:352-358, 2009

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Determination of Trimethylbismuth in the Human Body after Ingestion of Colloidal Bismuth SubcitrateFormula

Jens Boertz, Louise Michele Hartmann, Margareta Sulkowski, Joerg Hippler, Frank Mosel, Roland Arturo Diaz-Bone, Klaus Michalke, Albert Wolfgang Rettenmeier, and Alfred Vitalis Hirner

Institute of Environmental Analytical Chemistry (J.B., L.M.H., M.S., J.H., R.A.D.-B., A.V.H.), Department of Microbiology I (K.M.), University of Duisburg-Essen, Essen, Germany; and Institute of Hygiene and Occupational Medicine, University Hospital Essen, Essen, Germany (J.B., F.M., A.W.R.)

Biological methylation and hydride formation of metals and metalloids are ubiquitous environmental processes that can lead to the formation of chemical species with significantly increased mobility and toxicity. Whereas much is known about the interaction of metal(loid)s with microorganisms in environmental settings, little information has been gathered on respective processes inside the human body as yet. Here, we studied the biotransformation and excretion of bismuth after ingestion of colloidal bismuth subcitrate (215 mg of bismuth) to 20 male human volunteers. Bismuth absorption in the stomach and upper intestine was very low, as evidenced by the small quantity of bismuth eliminated via the renal route. Total bismuth concentrations in blood increased rapidly in the first hour after ingestion. Most of the ingested bismuth was excreted via feces during the study period. Trace levels of the metabolite trimethylbismuth [(CH3)3Bi] were detected via low temperaturegas chromatography/inductively coupled plasma-mass spectrometry in blood samples and in exhaled air samples. Concentrations were in the range of up to 2.50 pg/ml (blood) and 0.8 to 458 ng/m3 (exhaled air), with high interindividual variation being observed. Elimination routes of bismuth were exhaled air (up to 0.03{per thousand}), urine (0.03–1.2%), and feces. The site of (CH3)3Bi production could not be identified in the present study, but the intestinal microflora seems to be involved in this biotransformation if accompanying ex vivo studies are taken into consideration.


Address correspondence to: Jens Boertz, University of Duisburg-Essen, Universitaetsstrasse 3-5, 45141 Essen, Germany. E-mail: jens.boertz{at}uni-due.de







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