The Relative Bio-availability of Oral and Oromucosal Melatonin in Different Formulations in Healthy Human Volunteers.
Status:
Completed
Trial end date:
2012-01-01
Target enrollment:
Participant gender:
Summary
The circadian rhythm, the sleep-wake cycle, is mainly regulated by melatonin. The synthesis
of melatonin is stimulated by the absence of light, leading to peak serum levels before
bedtime. In humans, this endogenous "signaling" neurohormone induces sleep. Exogenous
melatonin can be beneficial in different sleep disturbances including delayed sleep phase
insomnia, melatonin- deficiency-related insomnia (especially in elderly) and shift work sleep
disorder. Melatonin is known for its low and variable bioavailability in humans due to a high
first pass effect and variable pharmacokinetics and short half-life. In order to prevent
exposure of patients with unnecessary high dosages of melatonin and in order to achieve a
short Tmax and high bio-availability of melatonin, a proper formulation needs to be defined.
This study, a three-phased cross-over study, aims to define a proper formulation for oral and
oromucosal melatonin for the treatment of insomnia by investigating the Tmax and relative
bioavailability derived from melatonin levels in salivary samples of healthy volunteers after
administration of melatonin in different formulations: 2,5mg melatonin immediate release
capsule (produced by Apotheek UMCU), 1mg melatonin immediate release tablet (produced by
Tiofarma), low-dose 0.1mg melatonin original Sleepzz tablet (produced by Vemedia
Manufacturing BV).