Ambre J, Ruo T I, Nelson J, Belknap S
Department of Medicine, Northwestern University Medical School, Chicago, Illinois 60611.
J Anal Toxicol. 1988 Nov-Dec;12(6):301-6. doi: 10.1093/jat/12.6.301.
The excretion kinetics of cocaine (C) and its two major metabolites, benzoylecgonine (BZ) and ecgonine methyl ester (EME), were determined by collecting all urine for 30 h from 5 cocaine users (subjects C, D, E, F, and G) given bolus doses followed by exponential cocaine infusions that delivered doses of 253 (subject C), 444 (subjects D, E, and F), and 700 mg (subject G). Plasma cocaine, urine cocaine, BZ, and EME were measured by gas chromatography, with a nitrogen detector. Elimination half-times for EME and BZ, estimated from semilog plots of excretion rates vs. time, averaged 3.1 and 4.5 h respectively, in agreement with our previous report. Urinary recovery in D, E, and F was 27-41% of the dose, with 14-17% as BZ, 12-21% as EME, and 2% as cocaine. Subject C excreted very little EME--5-6-fold less than the mean for the other subjects and amounting to only 3% of the dose. Cocaine disposition in subject G, who received the largest dose and attained plasma levels of 3000 ng/mL, showed some characteristics of a nonlinear process.
通过收集5名可卡因使用者（受试者C、D、E、F和G）在给予单次推注剂量后以指数方式输注可卡因（剂量分别为253mg（受试者C）、444mg（受试者D、E和F）和700mg（受试者G））后30小时内的所有尿液，来测定可卡因（C）及其两种主要代谢物苯甲酰芽子碱（BZ）和芽子碱甲酯（EME）的排泄动力学。采用带氮检测器的气相色谱法测定血浆可卡因、尿液可卡因、BZ和EME。根据排泄率与时间的半对数图估算，EME和BZ的消除半衰期分别平均为3.1小时和4.5小时，与我们之前的报告一致。受试者D、E和F的尿液回收率为剂量的27%-41%，其中14%-17%为BZ，12%-21%为EME，2%为可卡因。受试者C排泄的EME极少，比其他受试者的平均值少5-6倍，仅占剂量的3%。接受最大剂量且血浆水平达到3000ng/mL的受试者G的可卡因处置表现出一些非线性过程的特征。
