Zetner D, Andersen L P H, Rosenberg J
Department of Surgery, Center for Perioperative Optimization, Herlev Hospital, University of Copenhagen, Herlev, Denmark.
Drug Res (Stuttg). 2016 Apr;66(4):169-73. doi: 10.1055/s-0035-1565083. Epub 2015 Oct 29.
Melatonin is traditionally administered orally but has a poor and variable bioavailability. This study aims to present an overview of studies investigating the pharmacokinetics of alternative administration routes of melatonin.
A systematic literature search was performed and included experimental or clinical studies, investigating pharmacokinetics of alternative administration routes of melatonin in vivo. Alternative administration routes were defined as all administration routes except oral and intravenous.
10 studies were included in the review. Intranasal administration exhibited a quick absorption rate and high bioavailability. Transdermal administration displayed a variable absorption rate and possible deposition of melatonin in the skin. Oral transmucosal administration of melatonin exhibited a high plasma concentration compared to oral administration. Subcutaneous injection of melatonin displayed a rapid absorption rate compared to oral administration.
Intranasal administration of melatonin has a large potential, and more research in humans is warranted. Transdermal application of melatonin has a possible use in a local application, due to slow absorption and deposition in the skin. Oral transmucosal administration may potentially be a clinically relevant due to avoiding first-pass metabolism. Subcutaneous injection of melatonin did not document any advantages compared to other administration routes.
褪黑素传统上通过口服给药，但生物利用度较差且变化不定。本研究旨在概述有关褪黑素替代给药途径药代动力学的研究。
进行了系统的文献检索，纳入了调查褪黑素替代给药途径体内药代动力学的实验或临床研究。替代给药途径定义为除口服和静脉注射以外的所有给药途径。
该综述纳入了10项研究。鼻内给药显示出快速的吸收速率和高生物利用度。透皮给药显示出可变的吸收速率，且褪黑素可能会沉积在皮肤中。与口服给药相比，褪黑素口腔黏膜给药显示出较高的血浆浓度。与口服给药相比，皮下注射褪黑素显示出快速的吸收速率。
褪黑素鼻内给药具有很大潜力，值得在人体中进行更多研究。由于褪黑素在皮肤中吸收缓慢且会沉积，透皮应用可能在局部应用中有用。口腔黏膜给药可能因避免首过代谢而具有临床相关性。与其他给药途径相比，皮下注射褪黑素未显示出任何优势。
