Reference

Bioavailability of oral melatonin in humans

Bioavailability of oral melatonin in humans. Waldhauser, Franz; Waldhauser, Maria; Lieberman, Harris R.; Deng, Mei Hua; Lynch, Harry J.; Wurtman, Richard J. (Dep. Nutr. Food Sci., Massachusetts Inst. Technol., Cambridge, MA 02139, USA). Neuroendocrinology, 39(4), 307-13 (English) 1984. CODEN: NUNDAJ. ISSN: 0028-3835. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 Cryst. melatonin (I) [73-31-4] (80 mg) in gelatin capsules was administered to 5 young male volunteers and serum and urinary I levels was measured at intervals. Changes in serum I levels were best described by a biexponential equation with an absorption const. (ka) of 1.72 h-1 (half-life = 0.40 h) and an elimination const. (kel) of 0.87 h-1 (half-life = 0.80 h). Peak serum I levels, ranging from 350 to 10,000 times those occurring physiol. at nighttime, were obsd. 60-150 min after its administration, remaining stable for approx. 1.5 h. The fraction of ingested I that was absorbed, estd. from the area under the curve describing serum I concns. as a function of time after I administration (the concn.-time curve), varied by 25-fold among subjects. 3 Addnl. volunteers received 3 I-contg. capsules (80 mg each) at 60-min intervals. This regimen extended the duration of elevated serum I levels to 4-6 h. I excretion closely paralleled serum I levels until 9 h after the hormone's administration, after which urinary levels tended to be higher than those predicted from serum levels. However, the area under the concn.-time curve for serum I correlated well with the cumulative I excretion during the initial 15 h after I administration, indicating that either approach can be used to est. the absorption of orally administered I.

Minimizing disturbances in circadian rhythms of bodily performance and function

Minimizing disturbances in circadian rhythms of bodily performance and function. Short, Roger Valentine; Armstrong, Stuart (Monash University, Australia). Eur. Pat. Appl. EP 126630 A1 28 Nov 1984, 58 pp. DESIGNATED STATES: R: AT, BE, CH, DE, FR, GB, IT, LI, LU, NL, SE. (English). (European Patent Organization). CODEN: EPXXDW. CLASS: IC: C07D209-16; A61K031-40. APPLICATION: EP 84-303369 17 May 1984. PRIORITY: AU 83-9418 18 May 1983; AU 84-4734 27 Apr 1984. DOCUMENT TYPE: Patent CA Section: 2 (Mammalian Hormones) Section cross-reference(s): 63 The use of melatonin (I) [73-31-4] as a chronobiotic in humans to counteract disturbances in circadian rhythms of bodily performances and function as may occur in transfer of work patterns from day to night-shift or in jet-lag is described. Alleviation or prevention of ill effects assocd. with disturbances of circadian rhythm is achieved by administration of I in specified ways which are varied to suit particular needs and circumstances. Examples are given of the effectiveness of melatonin in inducing sleep during jet-lag and during rapid rotating shift work as well as the effect of I on body temp. under these conditions. A prepn. for oral administration is described which consists of I and a pharmacol. acceptable diluent, the prepn. being adapted to release I over an extended period.