Pharmacokinetics of Melatonin Niosomes Oral Gel in Healthy Volunteers

Melatonin is an endogenous hormone. It is able to promote nighttime sleeping and could induce sleep at daytime in adult and children with the nonpainful diagnostic procedure. However, previous formulation had problems of unstability of product and low oral bioavailability. Melatonin niosomes oral gels are formulated in order to overcome the problem of drug absorption and stability. This study is a randomized, double-blind, three phase crossover design in 15 male volunteers. Melatonin niosomes oral gel will be applied at doses 2.5, 5, and 10 mg with 7 days washout for each period. The pharmacokinetics data, sleep induction effect, and adverse event will be determined.

Study Overview

• Status: Unknown
• Conditions: Pharmacokinetics of Melatonin
• Intervention / Treatment: Drug: Melatonin

Detailed Description

This study will determine the pharmacokinetics, sleep induction effect, and adverse event after apply melatonin niosomes (MN) oral gel 2.5, 5, and 10 mg per dose in 15 male healthy volunteers. The pharmacokinetic parameters include maximum plasma concentration (Cmax), area under the curve (AUC), time to peak concentration (Tmax), elimination half-life (t1/2). Sleep induction will be determined as sleep onset and duration after use MN oral gels using actigraph and behavior observation. A polysomnography using electrode placement derive from multiple sleep latency test (MSLT) protocol will be used in some subjects. Adverse event will be evaluated by investigator.

• Study Type: Interventional
• Enrollment (Anticipated): 15
• Phase: Phase 2; Phase 1

Contacts and Locations

Study Locations

• Thailand
  • Khon Kaen
    • Amphur Muang, Khon Kaen, Thailand, 40002
      • Recruiting
      • Academic Clinical Research Office
      • Contact: Phone Number: 043-366-568-9; Email: info@acro-kku.com
      • Principal Investigator: Supawan Laohasiriwong, MD

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 30 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• male
• age 18-30 years
• body mass index 18.5-25 kg/m2
• general good health and no underlying disease by physical examination and laboratory testing (blood urea nitrogen, creatinine, bilirubin, aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase, complete blood count)
• provide signed informed consent for study participation

Exclusion Criteria:

• history of allergies to melatonin products
• use of any drugs, vitamins, or supplements within 30 days before participation
• smoke or alcohol consumption within 1 week before participation
• blood or plasma donation within 30 days before participation

Study Plan

How is the study designed?

Design Details

• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: Triple

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: melatonin niosomes oral gel 2.5 mg; apply onto oral mucosa as single use	Drug: Melatonin; Each sachet contains 0.5 g; Other Names: Melatonin niosomes oral gel 5 mg/g; Melatonin niosomes oral gel 10 mg/g; Melatonin niosomes oral gel 20 mg/g
Experimental: melatonin niosomes oral gel 5 mg; apply onto oral mucosa as single use	Drug: Melatonin; Each sachet contains 0.5 g; Other Names: Melatonin niosomes oral gel 5 mg/g; Melatonin niosomes oral gel 10 mg/g; Melatonin niosomes oral gel 20 mg/g
Experimental: melatonin niosomes oral gel 10 mg; apply onto oral mucosa as single use	Drug: Melatonin; Each sachet contains 0.5 g; Other Names: Melatonin niosomes oral gel 5 mg/g; Melatonin niosomes oral gel 10 mg/g; Melatonin niosomes oral gel 20 mg/g

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Concentration-time profile after 2.5, 5, and 10 mg Melatonin niosomes (MN) oral gel single dose administration	Blood sampling	0, 15, 30, 45, 60, 75, 90, 120, 180, 240, 300, 360 and 480 min after MN oral gel administration

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Sleep induction effect (sleep onset latency, total sleep time, and wake after sleep onset) after 2.5, 5, and 10 mg MN oral gel single dose administration	Sleep induction effect will be measured by using actigraph, behavior observation (all subjects), and Multiple sleep latency test (5 from 15 subjects).	0-480 min after MN oral gel administration

Other Outcome Measures

Outcome Measure	Measure Description	Time Frame
Adverse event after 2.5, 5, and 10 mg MN oral gel single dose administration	nausea, vomiting, headache, irritability and others	0-24 h after MN oral gel administration

Collaborators and Investigators

• Sponsor: Khon Kaen University
• Investigators: Principal Investigator: Supawan Laohasiriwong, MD, Department of Otorhinolaryngology, Faculty of Medicine, Khon Kaen University

Study record dates

Study Major Dates

• Study Start: May 1, 2016
• Primary Completion (Anticipated): August 1, 2016
• Study Completion (Anticipated): March 1, 2017

Study Registration Dates

• First Submitted: July 24, 2016
• First Submitted That Met QC Criteria: July 24, 2016
• First Posted (Estimate): July 27, 2016

Study Record Updates

• Last Update Posted (Estimate): July 27, 2016
• Last Update Submitted That Met QC Criteria: July 24, 2016
• Last Verified: July 1, 2016

More Information

Terms related to this study

• Keywords: melatonin; pharmacokinetics
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Molecular Mechanisms of Pharmacological Action; Central Nervous System Depressants; Protective Agents; Antioxidants; Melatonin
• Other Study ID Numbers: IN58358

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: Undecided