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J Clin Pharmacol. 2000 Jul;40(7):781-4.

The absolute bioavailability of oral melatonin.

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  • 1Department of Medicine, Bassett Healthcare, Cooperstown, New York 13326, USA.

Abstract

The absolute bioavailability of oral melatonin tablets was studied in 12 normal healthy volunteers. Subjects were administered, in a randomized crossover fashion, melatonin 2 mg intravenously and 2 and 4 mg orally. Blood was sampled over approximately eight (estimated) half-lives. Both the 2 and the 4 mg oral dosages showed an absolute bioavailability of approximately 15%. No difference in serum half-life was seen in any of the study phases. Oral melatonin tablets in dosages of 2 and 4 mg show poor absolute bioavailability, either due to poor oral absorption, large first-pass metabolism, or a combination of both. Further studies examining larger doses, in an attempt to saturate first-pass metabolism if it occurs, may be warranted.

PMID:
10883420
[PubMed - indexed for MEDLINE]
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