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American Journal of Clinical Nutrition, Vol. 69, No. 3, 504-508, March 1999
© 1999 American Society for Clinical Nutrition


Original Research Communications

Bioavailability of biotin given orally to humans in pharmacologic doses1,2,3

Janos Zempleni and Donald M Mock

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 ({approx}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 (13–23%), biotin-d,l-sulfoxide (5–13%), bisnorbiotin methyl ketone (3–9%), and biotin sulfone (1–3%) 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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