Yolles S, Leafe T D, Woodland J H, Meyer F J
J Pharm Sci. 1975 Feb;64(2):348-9. doi: 10.1002/jps.2600640239.
Parallel in vitro and in vivo release rates of tritiated naltrexone from poly(lactic acid) composites were studied. The in vitro release of naltrexone was 67% of the dose over a 35-day test period, while the in vivo release was only 24% within 70 days. Apparently, an exchange of the tritium for the hydrogen of the body water takes place, indicating that urinary excretion radioactivity is not a reliable measure for estimating the naltrexone released. Naltrexone-poly(lactic acid) composites showed effective blocking action to morphine in rats (24 days), dogs (29 days), monkeys (20 days), and mice (21 days).
研究了氚标记的纳曲酮从聚乳酸复合材料中的体外和体内平行释放率。在35天的测试期内，纳曲酮的体外释放量为剂量的67%，而在70天内的体内释放量仅为24%。显然，氚与体内水分中的氢发生了交换，这表明尿排泄放射性不是估计释放的纳曲酮的可靠指标。纳曲酮-聚乳酸复合材料对大鼠（24天）、狗（29天）、猴子（20天）和小鼠（21天）的吗啡显示出有效的阻断作用。
