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  • Title: Naltrexone metabolism and sustained release following administration of an insoluble complex to rhesus monkeys and guinea-pigs.
    Author: Macgregor TR, Drum MA, Harrigan SE, Wiley JN, Reuning RH.
    Journal: J Pharm Pharmacol; 1983 Jan; 35(1):38-42. PubMed ID: 6131962.
    Abstract:
    Both the release and the metabolism of naltrexone have been evaluated after intramuscular administration of a sustained release [15,16-3H2]naltrexone aluminium tannate complex in guinea-pigs and rhesus monkeys. In both species, measurable excretion of radioactivity was obtained for greater than 50 days and complete recovery of the dose was obtained in the guinea-pig. The radioactivity excretion rate-time profile differed in the two species with guinea-pig yielding a continuously declining rate and monkey yielding a peak at 5 days. In selected monkey urine samples (days 4, 17-20 and 49-52) subjected to t.l.c., evidence was obtained for the presence of naltrexone, beta-naltrexol and 2-hydroxy-3-O-methyl-beta-naltrexol, mostly as glucuronide and/or sulphate conjugates. The t.l.c. data also suggest that in monkey a naltrexone metabolite builds up relative to naltrexone over the 52 day release period.
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