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Comparative Pharmacokinetics of 5 mg Sustained-Release Versus 5 mg Immediate-Release Melatonin Capsules in Fasting Healthy Adults: A Randomized, Open-Label, Cross-Over Study
Thanawala, S.; Abiraamasundari, R.; Shah, R. Comparative Pharmacokinetics of 5 mg Sustained-Release Versus 5 mg Immediate-Release Melatonin Capsules in Fasting Healthy Adults: A Randomized, Open-Label, Cross-Over Study. Preprints2024, 2024080790. https://doi.org/10.20944/preprints202408.0790.v1
APA Style
Thanawala, S., Abiraamasundari, R., & Shah, R. (2024). Comparative Pharmacokinetics of 5 mg Sustained-Release Versus 5 mg Immediate-Release Melatonin Capsules in Fasting Healthy Adults: A Randomized, Open-Label, Cross-Over Study. Preprints. https://doi.org/10.20944/preprints202408.0790.v1
Chicago/Turabian Style
Thanawala, S., R Abiraamasundari and Rajat Shah. 2024 "Comparative Pharmacokinetics of 5 mg Sustained-Release Versus 5 mg Immediate-Release Melatonin Capsules in Fasting Healthy Adults: A Randomized, Open-Label, Cross-Over Study" Preprints. https://doi.org/10.20944/preprints202408.0790.v1
Abstract
Exogenous melatonin, a nutraceutical for maintaining a healthy sleep-wake cycle and managing sleep disorders, requires large, repeated doses due to low bioavailability and short half-life. This necessitates the development of a sustained-release formulation with a longer half-life and sustained plasma concentration. Therefore, exogenous novel 5 mg sustained-release melatonin capsules (Melatonin-SR, test product) were formulated. This open-label cross-over study compared the pharmacokinetics (maximum concentration [Cmax], time to reach Cmax [Tmax], area under the curve [AUC] and elimination half-life [t1/2]) and safety of Melatonin-SR with 5 mg immediate-release melatonin capsules (Melatonin-IR, reference product) after single-dose oral administration in healthy fasting adults. Sixteen participants (aged 18-45 years) were randomized (1:1) to receive either Melatonin-SR or Melatonin-IR in two periods with a 7-day washout period. Melatonin-SR reported lower Cmax (11446.87 pg/mL) compared to Melatonin-IR (22786.30 pg/mL). The mean Tmax of Melatonin-SR and Melatonin-IR was 1.26 h and 0.87 h, respectively. The mean t1/2 of Melatonin-SR (5.10 h) was prolonged by five-fold compared to Melatonin-IR (1.01 h). One adverse event (vomiting) was reported following administration of the Melatonin-IR. Melatonin-SR resulted in higher and sustained plasma melatonin concentrations for an extended period and was well-tolerated. Hence, Melatonin-SR may be a promising nutraceutical for maintaining healthy sleep.
Medicine and Pharmacology, Complementary and Alternative Medicine
Copyright:
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