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Int J Pharm. 1999 May 10;182(1):1-5.

Intranasal absorption of melatonin in vivo bioavailability study.

Author information

1
The Royal Danish School of Pharmacy, Department of Pharmaceutics, Universitetsparken 2, DK-2100, Copenhagen O, Denmark.

Abstract

The bioavailability of melatonin in rabbits after nasal administration of two formulations has been studied. In each case, a total amount of 1.5 mg melatonin in 50 microl was administered and compared with 1.5 mg i.v. The test solutions were formulated with 40% polyethylene glycol 300 (PEG 300), one with 1% sodium glycocholate (+GC) and one without (-GC). The bioavailability for +GC was 94% (S.D.+/-29%, n=4), whereas the bioavailability for -GC was 55% (S.D.+/-17%, n=6). These results indicate that GC has an enhancer effect (P<0.05). However, the relatively high bioavailability without GC shows that it might not be necessary to use an enhancer for a clinical relevant formulation. The pharmacokinetics of melatonin could be described by a one-compartment model, and the serum half-life was about 13 min. The absorption rate for both formulations was very fast (tmax=5 min) and Cmax mean was 493+/-290 ng/ml (n=4) and 249+/-125 ng/ml (n=6) for +GC and -GC, respectively.

PMID:
10332069
DOI:
10.1016/s0378-5173(99)00019-8
[Indexed for MEDLINE]

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