A Randomized, Double-Blind, Crossover Study to Investigate the Pharmacokinetics of Extended-Release Melatonin Compared to Immediate-Release Melatonin in Healthy Adults
Exogenous melatonin can be helpful for treatment of some sleep disorders. However, immediate-release formulations are rapidly absorbed and cleared from the body making it difficult to provide coverage for an entire sleep period. Extended-release melatonin formulations can better mimic the naturally occurring melatonin profile and increase efficacy, but few studies have reported on their pharmacokinetics. To assess the pharmacokinetics of extended-release melatonin, we conducted a randomized, double-blind, crossover study of extended-release melatonin (4 mg) compared to immediate-release melatonin (4 mg) in 18 healthy adults, ages 18-65 years. Participants received immediate-release or extended-release melatonin in clinic after an 8 h fast, and blood samples were taken over a 10-h period. After a 7-day washout period, the same procedures were repeated with the melatonin form not previously received. Extended-release melatonin had a longer time to peak concentration (1.56 vs 0.6 h) and elimination half-life (1.63 vs 0.95 h) compared with immediate-release melatonin. Maximum concentration was lower for extended-release melatonin compared with immediate-release melatonin (7581 pg/mL vs 13120 pg/mL). Extended-release melatonin raised melatonin levels in as little as 15 min and sustained elevated melatonin levels (>300 pg/mL) for 6 h before falling below 50 pg/mL by 9 h. No clinically relevant adverse events were observed, and safety parameters remained within normal ranges for both formulations. The pharmacokinetic profile of this extended-release melatonin formulation suggests that it could be used for future efficacy studies of melatonin and sleep outcomes. This trial is registered at ClinicalTrials.gov, NCT04067791.
Medienart: |
E-Artikel |
---|
Erscheinungsjahr: |
2024 |
---|---|
Erschienen: |
2024 |
Enthalten in: |
Zur Gesamtaufnahme - volume:21 |
---|---|
Enthalten in: |
Journal of dietary supplements - 21(2024), 2 vom: 01., Seite 182-194 |
Sprache: |
Englisch |
---|
Beteiligte Personen: |
Mun, Jonathan G [VerfasserIn] |
---|
Links: |
---|
Themen: |
Delayed-Action Preparations |
---|
Anmerkungen: |
Date Completed 26.02.2024 Date Revised 07.03.2024 published: Print-Electronic ClinicalTrials.gov: NCT04067791 Citation Status MEDLINE |
---|
doi: |
10.1080/19390211.2023.2206475 |
---|
funding: |
|
---|---|
Förderinstitution / Projekttitel: |
|
PPN (Katalog-ID): |
NLM356540375 |
---|
LEADER | 01000caa a22002652 4500 | ||
---|---|---|---|
001 | NLM356540375 | ||
003 | DE-627 | ||
005 | 20240307231910.0 | ||
007 | cr uuu---uuuuu | ||
008 | 231226s2024 xx |||||o 00| ||eng c | ||
024 | 7 | |a 10.1080/19390211.2023.2206475 |2 doi | |
028 | 5 | 2 | |a pubmed24n1319.xml |
035 | |a (DE-627)NLM356540375 | ||
035 | |a (NLM)37150895 | ||
040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
041 | |a eng | ||
100 | 1 | |a Mun, Jonathan G |e verfasserin |4 aut | |
245 | 1 | 2 | |a A Randomized, Double-Blind, Crossover Study to Investigate the Pharmacokinetics of Extended-Release Melatonin Compared to Immediate-Release Melatonin in Healthy Adults |
264 | 1 | |c 2024 | |
336 | |a Text |b txt |2 rdacontent | ||
337 | |a ƒaComputermedien |b c |2 rdamedia | ||
338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
500 | |a Date Completed 26.02.2024 | ||
500 | |a Date Revised 07.03.2024 | ||
500 | |a published: Print-Electronic | ||
500 | |a ClinicalTrials.gov: NCT04067791 | ||
500 | |a Citation Status MEDLINE | ||
520 | |a Exogenous melatonin can be helpful for treatment of some sleep disorders. However, immediate-release formulations are rapidly absorbed and cleared from the body making it difficult to provide coverage for an entire sleep period. Extended-release melatonin formulations can better mimic the naturally occurring melatonin profile and increase efficacy, but few studies have reported on their pharmacokinetics. To assess the pharmacokinetics of extended-release melatonin, we conducted a randomized, double-blind, crossover study of extended-release melatonin (4 mg) compared to immediate-release melatonin (4 mg) in 18 healthy adults, ages 18-65 years. Participants received immediate-release or extended-release melatonin in clinic after an 8 h fast, and blood samples were taken over a 10-h period. After a 7-day washout period, the same procedures were repeated with the melatonin form not previously received. Extended-release melatonin had a longer time to peak concentration (1.56 vs 0.6 h) and elimination half-life (1.63 vs 0.95 h) compared with immediate-release melatonin. Maximum concentration was lower for extended-release melatonin compared with immediate-release melatonin (7581 pg/mL vs 13120 pg/mL). Extended-release melatonin raised melatonin levels in as little as 15 min and sustained elevated melatonin levels (>300 pg/mL) for 6 h before falling below 50 pg/mL by 9 h. No clinically relevant adverse events were observed, and safety parameters remained within normal ranges for both formulations. The pharmacokinetic profile of this extended-release melatonin formulation suggests that it could be used for future efficacy studies of melatonin and sleep outcomes. This trial is registered at ClinicalTrials.gov, NCT04067791 | ||
650 | 4 | |a Randomized Controlled Trial | |
650 | 4 | |a Journal Article | |
650 | 4 | |a Extended-release | |
650 | 4 | |a melatonin | |
650 | 4 | |a pharmacokinetics | |
650 | 4 | |a prolonged-release | |
650 | 7 | |a Delayed-Action Preparations |2 NLM | |
650 | 7 | |a Melatonin |2 NLM | |
650 | 7 | |a JL5DK93RCL |2 NLM | |
700 | 1 | |a Wang, Dan |e verfasserin |4 aut | |
700 | 1 | |a Doerflein Fulk, Denise L |e verfasserin |4 aut | |
700 | 1 | |a Fakhary, Mina |e verfasserin |4 aut | |
700 | 1 | |a Gualco, Scott J |e verfasserin |4 aut | |
700 | 1 | |a Grant, Ryan W |e verfasserin |4 aut | |
700 | 1 | |a Mitmesser, Susan Hazels |e verfasserin |4 aut | |
773 | 0 | 8 | |i Enthalten in |t Journal of dietary supplements |d 2008 |g 21(2024), 2 vom: 01., Seite 182-194 |w (DE-627)NLM192571656 |x 1939-022X |7 nnns |
773 | 1 | 8 | |g volume:21 |g year:2024 |g number:2 |g day:01 |g pages:182-194 |
856 | 4 | 0 | |u http://dx.doi.org/10.1080/19390211.2023.2206475 |3 Volltext |
912 | |a GBV_USEFLAG_A | ||
912 | |a GBV_NLM | ||
951 | |a AR | ||
952 | |d 21 |j 2024 |e 2 |b 01 |h 182-194 |