The Relative Bio-availability of Oral and Oromucosal Melatonin in Different Formulations in Healthy Human Volunteers.

NCT02107079 | Completed

• 2 other identifiers: Melaform2011-003068-61
• Study Type: interventional
• Target: 10
• Locations: 1 country
• Sites: 1

Brief 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).

Conditions

Pharmacokinetics of Melatonin

Keywords

melatonin; bioavailability; pharmacokinetics

Outcome Measures

Primary Outcomes (1)

• Melatonin concentration (ng/ml) in saliva

  At 15 min, 30 min, 1 hour, 1.5 hour, 2 hours, 3 hours (tablet; capsule); at 25 minutes, 40 minutes, 60 minutes, 1.5 hour, 2 hours and 3 hours (sublingual tablet )

Study Arms (3)

melatonin 1 mg immediate release tablet

ACTIVE COMPARATOR

Drug: Melatonin

melatonin 2,5mg immediate release capsule

ACTIVE COMPARATOR

Drug: Melatonin

melatonin 0.1 mg oromucosal tablet

ACTIVE COMPARATOR

Drug: Melatonin

Interventions

Melatonin DRUG

swallowing 1 piece, collecting saliva afterwards

Also known as: Melatonin 2,5 mg capsule (compounded by UMCU Pharnacy), Melatonin 1 mg tablet Thiopharma, Sleepzz 0.1 mg oromucosal tablet

melatonin 0.1 mg oromucosal tablet; melatonin 1 mg immediate release tablet; melatonin 2,5mg immediate release capsule

Eligibility Criteria

• Age: 18 Years - 35 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Volunteers (male) aged from 18 to 35 years old without insomnia.

You may not qualify if:

• Lactose intolerance.
• Hepatic disease
• Kidney disease
• Auto-immune disease
• Depression
• Neurological disorders
• Oromucosal diseases.

Sponsors & Collaborators

• Utrecht University: lead

Study Sites (1)

Pharmacy department of faculty of veterinary medicine Utrecht University

Utrecht, Utrecht, Netherlands

Location

Related Links

• CCMO protocol

MeSH Terms

Interventions

Melatonin

Intervention Hierarchy (Ancestors)

Tryptamines; Indoles; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; Hormones; Hormones, Hormone Substitutes, and Hormone Antagonists

Study Design

• Study Type: interventional
• Phase: not applicable
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER
• Responsible Party: PRINCIPAL INVESTIGATOR
• PI Title: hospital pharmacist

Study Record Dates

• First Submitted: April 3, 2014
• First Posted: April 8, 2014
• Study Start: January 1, 2012
• Primary Completion: January 1, 2012
• Study Completion: January 1, 2012
• Last Updated: April 8, 2014

Record last verified: 2014-04

Locations

NL (1)