Plasma concentrations of heroin and morphine-related metabolites after intranasal and intramuscular administration
Plasma concentrations of heroin and morphine-related metabolites after intranasal and intramuscular administration
复制标题
DOI：
10.1093/jat/21.2.105
复制
发表时间：
1997-03-01
影响因子：
2.5
通讯作者：
Aderjan, R
中科院分区：
文献类型：
--
作者：
Skopp, G;Ganssmann, B;Aderjan, R
本文研究了4名健康男性志愿者鼻腔内注射6和12 mg盐酸海洛因后海洛因及其代谢产物的处置。此外，两种剂量的盐酸海洛因6 mg肌肉注射，以比较药代动力学参数。采用固相萃取-气相色谱-质谱法对血清样品中的海洛因、6-乙酰吗啡和吗啡进行分析。吗啡葡萄糖醛酸苷的浓度通过基于缀合物的天然荧光的高效液相色谱法测定。主要发现是迅速上升和下降的终端阶段海洛因和6-乙酰吗啡和缓慢下降阶段的吗啡和代谢物后，两种途径的管理。吗啡-3-葡糖苷酸的曲线下面积值取决于剂量，但不取决于给药途径。吗啡-3-葡萄糖醛酸苷的表观终末半衰期范围为2.2至5.2小时，鼻内给予海洛因，分别为3.0和1.7小时，肌肉注射药物。平均吗啡-3-葡萄糖醛酸-海洛因：鼻内给药的曲线下面积比为93，而肌内给药的曲线下面积比为38，这表明相同剂量鼻内给药后，海洛因的循环量约为一半。
The disposition of heroin and its metabolites was investigated in four healthy male volunteers following intranasal administration of 6 and 12 mg heroin hydrochloride. In addition, two doses of 6 mg heroin hydrochloride were injected intramuscularly for comparison of pharmacokinetic parameters. Serum samples were analyzed for heroin, 6-acetylmorphine, and morphine by solid-phase extraction-gas chromatography-mass spectrometry. The concentration of morphine glucuronides was determined by high-performance liquid chromatography based on the native fluorescence of the conjugates. Major findings were rapidly rising and declining terminal phases for heroin and 6-acetylmorphine and slowly declining phases of morphine and metabolites after both routes of administration. The area under the curve values of morphine-3-glucuronide depended on dose but not on route of administration. The apparent terminal half-lives of morphine-3-glucuronide ranged from 2.2 to 5.2 h for intranasally administered heroin and were 3.0 and 1.7 h for the intramuscularly applied drug. A mean morphine-3-glucuronide-heroin:area-under-curve ratio of 93 for the intranasal route as compared with 38 for the intramuscular route demonstrated that circulating amounts of heroin were about half the size after intranasal administration of the same dose.