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Original Research Communications |
Background: Patients with carboxylase deficiency are treated with pharmacologic doses of biotin.
Objective: We sought to determine the bioavailability of biotin at pharmacologic doses.
Design: Biotin was administered orally (2.1, 8.2, or 81.9 µmol) or intravenously (18.4 µmol) to 6 healthy adults in a crossover design with
2 wk between each biotin administration. Before and after each administration, timed 24-h urine samples were collected. Urinary biotin and biotin metabolites were analyzed by an HPLC avidin-binding assay.
Results: Urinary recoveries of biotin plus metabolites were similar (
50%) after the 2 largest oral doses and the 1 intravenous dose, suggesting 100% bioavailability of the 2 largest oral doses. For unexplained reasons, the apparent recovery of the smallest oral dose was about twice that of the other doses. For all 4 doses, biotin accounted for >50% of the total of biotin and biotin metabolites in urine. Bisnorbiotin (1323%), biotin-d,l-sulfoxide (513%), bisnorbiotin methyl ketone (39%), and biotin sulfone (13%) accounted for the remainder. The percentage excretion of biotin was greater when biotin was administered intravenously and for the largest oral dose than for the 2 smallest oral doses.
Conclusion: Our data provide evidence that oral biotin is completely absorbed even when pharmacologic doses are administered. Biotin metabolites account for a substantial portion of total urinary excretion and must be considered in bioavailability studies. We speculate that renal losses of biotin (as a percentage of the dose administered) are moderately elevated when pharmacologic doses of biotin are administered.
Key Words: Biotin biotin metabolites bioavailability humans urine multiple carboxylase deficiency
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