Nakahara Y, Ochiai T, Kikura R
National Institute of Hygienic Sciences, Tokyo, Japan.
Arch Toxicol. 1992;66(6):446-9. doi: 10.1007/BF02035137.
We studied the incorporation of cocaine (COC), benzoylecgonine (BE) and ecgonine methyl ester (EME) into hair from blood. At first, the time courses of three drugs in rat plasma following i.p. administration of cocaine were investigated over 360 min. AUCs of COC, BE and EME in plasma were 14.2, 60.7 and 53.4 micrograms/ml/min, respectively. In contrast, the concentrations of the three compounds in hair were 16.4, 1.7 and 0.8 ng/mg. In spite of that, the AUC of COC in plasma was much lower than that of the other two compounds in plasma, the concentration of COC in hair was much higher than that of the other two compounds. The incorporation of COC into hair was much greater than that of BE and EME. If the incorporation of drugs from blood into hair is compared by [concentration in hair]/[AUC in plasma], that of COC, BE and EME is represented by 77:1.9:1. Our results suggest that the incorporation of drugs into hair from blood unexpectedly depends upon the physical properties of each drug.
我们研究了可卡因（COC）、苯甲酰爱康宁（BE）和芽子碱甲酯（EME）从血液进入毛发的情况。首先，在腹腔注射可卡因后360分钟内，研究了三种药物在大鼠血浆中的时间进程。血浆中COC、BE和EME的曲线下面积（AUC）分别为14.2、60.7和53.4微克/毫升/分钟。相比之下，毛发中这三种化合物的浓度分别为16.4、1.7和0.8纳克/毫克。尽管血浆中COC的AUC远低于其他两种化合物，但毛发中COC的浓度却远高于其他两种化合物。COC进入毛发的量远大于BE和EME。如果通过[毛发中的浓度]/[血浆中的AUC]来比较药物从血液进入毛发的情况，COC、BE和EME的该比值分别为77:1.9:1。我们的结果表明，药物从血液进入毛发的情况出乎意料地取决于每种药物的物理性质。
