Summary
In order to study the disposition of ENDOTELON in humans, this compound was labelled withl4C by photosynthesis. ENDOTELON consists of a complex of procyanidolic oligomers extracted from the seeds of a variety of vine cultivated in the Bordeaux wine-growing region, and is prescribed for the treatment of chronic venous insufficiency and retinal lesions.
Considering the difficulty in labelling the various constituents of the product, the labelling procedure was based on providing radioactive C02 to the plant. After isolation and purification, 150 mg of active material (50 μCf) was administered orally to six healthy volunteers. Radioactivity was measured in the blood over time until 72 and 120 hours in the same subjects after drug administration. Urinary and faecal elimination was measured for a period of 167 hours. Urinary elimination of the radioactive compounds represented 12 to 27% of the administered dose and faecal elimination represented 47 to 75% depending on the subject. The radioactivity of thel4C02 eliminated in the breath was also measured, and represented around 8% of the total radioactivity for the 72-hour period after administration.
Although the disposition of ENDOTELON is based on the total radioactivity measured over time, this technique allows the evaluation of the elimination rate of the product and its metabolites from the human body.
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Benakis, A., Schopfer, C. & Ritschard, J. Disposition of14C-labelled endotelon in humans. Eur. J. Drug Metabol. Pharmacokinet. 33, 37–43 (2008). https://doi.org/10.1007/BF03191017
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DOI: https://doi.org/10.1007/BF03191017