Macgregor T R, Drum M A, Harrigan S E, Wiley J N, Reuning R H
J Pharm Pharmacol. 1983 Jan;35(1):38-42. doi: 10.1111/j.2042-7158.1983.tb04260.x.
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.
在豚鼠和恒河猴中，通过肌肉注射[15,16 - 3H2]纳曲酮铝鞣酸复合物缓释制剂后，对纳曲酮的释放和代谢进行了评估。在这两个物种中，放射性物质的可测量排泄持续超过50天，并且在豚鼠中实现了剂量的完全回收。两个物种的放射性排泄速率-时间曲线不同，豚鼠的排泄速率持续下降，而猴子在第5天出现峰值。在经过薄层层析的选定猴子尿液样本（第4、17 - 20和49 - 52天）中，获得了纳曲酮、β-纳曲醇和2-羟基-3-O-甲基-β-纳曲醇存在的证据，它们大多以葡萄糖醛酸和/或硫酸盐共轭物的形式存在。薄层层析数据还表明，在猴子中，在52天的释放期内，一种纳曲酮代谢物相对于纳曲酮有所积累。
