Table S2. Published values of PK parameters for exogenous melatonin in plasma from young healthy human subjects

Literature Ref / Melatonin1
Dose, mg / PK parameters / Age of subjects, yrs / # of subjects / Analytical Method
Waldhauser 1984 / 80 / t1/2 = 0.81 ± 0.07 h, Tmax = 1.75 ± 0.75h / 21-27 / 5 / RIA
Vakkuri 1985 / 100 / t1/2 = 0.68 ± 0.06 h, Tmax = 1.5 ± 0.5h / 25-48 / 5 / RIA2
Aldhous 1985 / 2.0 (capsule)
2.0(corn oil) / Tmax = 0.46 ± 0.07 h
Tmax = 0.95 ± 0.42 h / 21-39 / 5
4 / RIA
Cavallo 1996 / 0.0131 / t1/2 = 0.67 ± 0.12 h / 6-10 / 9 / RIA
Di 1997 / 0.5 / t1/2 = 0.68 ± 0.05 h / 21-32 / 4 / RIA
DeMuro 2000 / 2.0
4.0 / t1/2 = 1.0 ± 0.22 h, Tmax = 0.87 ± 0.53 h
t1/2 = 1.1 ± 0.19 h, Tmax = 1.0 ± 0.53 h / 25-45 / 12 / RIA
Fourtillan 2000 / 0.25 / t1/2 = 0.68 ± 0.19 h, Tmax = 0.38 ± 0.14 h, F = 0.13 ± 0.11 / 22-35 / 12 / GC-MS3
Härtter 2003 / 6.0 / t1/2 = 1.8 ± 0.65 h, Cl/F = 2460 ±1570 mL/h/kg / 18-40 / 12 / RIA
Markantonis 2008 / 6.0 / t1/2 = 0.76 ± 0.19 h, Tmax = 0.75 ± 0.25 h / 24-33 / 10 / HPLC-Fluorescence

t1/2= oral half-life; Tmax = time to maximum concentration; Cl/F = ratio of clearance to oralbioavailability.

1A relatively low dose of Mel was administered by 10 min iv. infusion in Cavallo’s study. Mel was administered orally in all other references.
2Melatonin was not measured in plasma; values reported here were in serum.

3Stable isotope labeled Mel-d7 was administered. Gas chromatography mass spectrometry was used to selectively detect exogenous d7-Mel in plasma. Oral

bioavailability was determined by comparing equivalent oral and I.V. doses.