OBJECTIVE: Oral bioavailability is one of the most important properties in drug design and development. A poor oral bioavailability can result in low efficacy and unpredictable response to a drug. Several dosages of melatonin have been used for various investigations to clarify its bioavailability in humans. Aiming to search for a pharmaceutical form, which is better absorbed, the pharmacokinetic (PK) profile of the new manufactured melatonin soft gelatin (soft gel) capsule form has been evaluated and compared with the commercially available melatonin powder. RESEARCH DESIGN AND METHODS: A total of 60 healthy volunteers received 1, 3 mg of melatonin powder and 1 mg of melatonin in soft gel capsules. PK profiles were obtained by analysis of melatonin plasma concentration, and the respective melatonin bioavailability was compared. RESULTS: Melatonin soft gel capsule form showed similar PK parameters compared with the highest doses of melatonin in powder form, but its bioavailability was improved. CONCLUSIONS: Soft gel capsules improved the bioavailability of melatonin in humans even when administered dose was reduced. Considering the number of conditions in which melatonin supplementation is recommended, this evidence could support a broader use of melatonin in clinical practice.
OBJECTIVE: Oral bioavailability is one of the most important properties in drug design and development. A poor oral bioavailability can result in low efficacy and unpredictable response to a drug. Several dosages of melatonin have been used for various investigations to clarify its bioavailability in humans. Aiming to search for a pharmaceutical form, which is better absorbed, the pharmacokinetic (PK) profile of the new manufactured melatonin soft gelatin (soft gel) capsule form has been evaluated and compared with the commercially available melatonin powder. RESEARCH DESIGN AND METHODS: A total of 60 healthy volunteers received 1, 3 mg of melatonin powder and 1 mg of melatonin in soft gel capsules. PK profiles were obtained by analysis of melatonin plasma concentration, and the respective melatonin bioavailability was compared. RESULTS:Melatonin soft gel capsule form showed similar PK parameters compared with the highest doses of melatonin in powder form, but its bioavailability was improved. CONCLUSIONS: Soft gel capsules improved the bioavailability of melatonin in humans even when administered dose was reduced. Considering the number of conditions in which melatonin supplementation is recommended, this evidence could support a broader use of melatonin in clinical practice.
Authors: Simona Dinicola; Vittorio Unfer; Fabio Facchinetti; Christophe O Soulage; Nicholas D Greene; Mariano Bizzarri; Antonio Simone Laganà; Shiao-Yng Chan; Arturo Bevilacqua; Lali Pkhaladze; Salvatore Benvenga; Annarita Stringaro; Daniele Barbaro; Marialuisa Appetecchia; Cesare Aragona; Maria Salomè Bezerra Espinola; Tonino Cantelmi; Pietro Cavalli; Tony T Chiu; Andrew J Copp; Rosario D'Anna; Didier Dewailly; Cherubino Di Lorenzo; Evanthia Diamanti-Kandarakis; Imelda Hernández Marín; Moshe Hod; Zdravko Kamenov; Eleni Kandaraki; Giovanni Monastra; Mario Montanino Oliva; John E Nestler; Maurizio Nordio; Ali C Ozay; Olga Papalou; Giuseppina Porcaro; Nikos Prapas; Scott Roseff; Monica Vazquez-Levin; Ivana Vucenik; Artur Wdowiak Journal: Int J Mol Sci Date: 2021-09-30 Impact factor: 5.923