Uemura Koichi, Fujimiya Tatsuya, Ohbora Yumiko, Yasuhara Masahiro, Yoshida Ken-Ichi
Department of Forensic Medicine Graduate School of Medicine, University of Tokyo, 7-3-1 Hongo Bunkyo-ku, 113-0033, Tokyo, Japan,
Forensic Sci Med Pathol. 2005 Mar;1(1):27-30. doi: 10.1385/FSMP:1:1:027.
The individual differences in alcohol pharmacokinetics were studied using the one-compartment model with first-order absorption and zero-order elimination kinetics in humans. The blood alcohol concentrations (BACs) were simulated by obtained parameters, absorption rate constant (ka), and climination rate constant (β). The 81 healthy young Japanese volunteers, who had been divided into those without alcohol-induced facial flushing (nonflushers) and those with facial flushing (flushers) according to alcohol patch test results and a questionnaire beforehand, ingested 0.50 g/kg ethanol within 1 minute. Breath alcohol concentrations (BrACs) were measured during absorption and during the elimination period. BACs were obtained based on BrACs. Fifteen percent of subjects exhibited low BAC profile (below 0.4 mg/mL) (first-pass effect [FPE] group), although the majority showed normal BAC profile (normal group). The ka was approximately 5 to 8 (h(-1)) in the normal group without significant difference between nonflushers and flushers, whereas that in the FPE group was significantly smaller than in the normal group. For the normal group, peak BACs were well simulated by the one-compartment model with first-order absorption and zero-order elimination kinetics. A considerable portion of subjects exhibited FPE. Absorption of alcohol from the intestine plays an important role in alcohol pharmacokinetics in humans.
利用具有一级吸收和零级消除动力学的单室模型对人体酒精药代动力学的个体差异进行了研究。通过获得的参数、吸收速率常数(ka)和消除速率常数(β)对血醇浓度(BAC)进行模拟。81名健康的日本年轻志愿者,根据酒精贴片试验结果和事先的问卷调查,被分为无酒精性面部潮红者(非潮红者)和有面部潮红者(潮红者),在1分钟内摄入0.50 g/kg乙醇。在吸收期和消除期测量呼气酒精浓度(BrAC)。基于BrAC获得BAC。15%的受试者表现出低BAC曲线(低于0.4 mg/mL)(首过效应[FPE]组),尽管大多数受试者表现出正常的BAC曲线(正常组)。正常组的ka约为5至8(h-1),非潮红者和潮红者之间无显著差异,而FPE组的ka显著小于正常组。对于正常组,具有一级吸收和零级消除动力学的单室模型能很好地模拟BAC峰值。相当一部分受试者表现出首过效应。肠道对酒精的吸收在人体酒精药代动力学中起着重要作用。