Okonkwo P O, Ogbuokiri J E, Ofoegbu E, Klotz U
Department of Pharmacology, University of Nigeria College of Medicine, Enugu.
Clin Pharmacol Ther. 1993 Apr;53(4):426-30. doi: 10.1038/clpt.1993.46.
We measured ivermectin in plasma, urine, and saliva of nine patients with onchocerciasis. The aim was to establish pharmacokinetic parameters and to assess the most facile medium for use in monitoring compliance. Binding of ivermectin to plasma proteins in vitro was also investigated. The mean (+/- SEM) plasma values for the nine subjects were as follows: weight, 66.3 +/- 2.8 kg; dose, 11.11 +/- 0.4 mg; half-life, 56.50 +/- 7.01 hours; clearance, 142.5 +/- 22.6 L/kg; volume of distribution, 9.91 +/- 2.67 L/kg; area under the plasma concentration-time curve, 1545.3 +/- 190.5 ng/ml.hr; time to reach maximum concentration, 4.7 +/- 0.5 hours; and maximum concentration, 38.2 +/- 5.8 ng/ml. Ivermectin was not detected in the urine of any of the nine subjects. Low levels were found in saliva. Blood specimens remain the only reliable biologic fluid for assessment of compliance after ivermectin oral administration. Ivermectin binds specifically to human serum albumin.
我们检测了9名盘尾丝虫病患者血浆、尿液和唾液中的伊维菌素。目的是确定药代动力学参数，并评估用于监测依从性的最便捷介质。还研究了伊维菌素在体外与血浆蛋白的结合情况。9名受试者的平均（±标准误）血浆值如下：体重66.3±2.8kg；剂量11.11±0.4mg；半衰期56.50±7.01小时；清除率142.5±22.6L/kg；分布容积9.91±2.67L/kg；血浆浓度-时间曲线下面积1545.3±190.5ng/ml·小时；达峰时间4.7±0.5小时；最大浓度38.2±5.8ng/ml。9名受试者的尿液中均未检测到伊维菌素。唾液中发现的水平较低。血液标本仍然是口服伊维菌素后评估依从性的唯一可靠生物流体。伊维菌素特异性结合人血清白蛋白。
