Distribution of doubly radiolabelled amphotericin B methyl ester and amphotericin B in the non-human primate, Macaca mulatta.
Distribution of doubly radiolabelled amphotericin B methyl ester and amphotericin B in the non-human primate, Macaca mulatta.
复制标题
双放射性标记的两性霉素 B 甲酯和两性霉素 B 在非人类灵长类动物猕猴中的分布。
DOI：
10.1093/jac/6.2.241
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发表时间：
1980
期刊：
影响因子：
--
通讯作者：
Carl P. Schaffner
中科院分区：
文献类型：
--
作者：
Ruth M. Lawrence;Paul D. Hoeprich;Franklyn A. Jagdis;Nobuo Monji;A. C. Huston;Carl P. Schaffner
将双放射性标记的两性霉素 B 甲酯盐酸盐 (AME) 或两性霉素 B 脱氧胆酸盐 (AMB) 作为单次静脉注射剂量注入恒河猴 (Macaca mulatta) 中。 24小时后，放血处死动物，获取组织和液体用于放射性和生物活性药物的测量。AME不脱酯。 AMB 脱氧胆酸复合物解离，各成分在体内的处理方式不同。胆汁中发现两种药物的浓度最高。 5 mg/kg 体重剂量下的 AME 在肺中的累积量是 1 mg/kg 体重剂量下 AMB 的 12 至 46（平均：23）倍。在肾脏中，AME 超过 AMB 3 至 10（平均：6）倍，并且达到的浓度比尿液中 AMB 高 12 至 22 倍。这两种药物均不会在大脑或脑脊液中积聚。
Either doubly radiolabelled amphotericin B methyl ester hydrochloride (AME) or amphotericin B deoxycholate (AMB) was infused as a single intravenous dose into rhesus monkeys (Macaca mulatta). Twenty-four hours later, the animals were killed by exsanguination, and tissues and liquids were obtained for measurements of radioactivity and bioactive drugs.AME was not de-esterified. The AMB deoxycholate complex dissociated and the components were handled differently in the body. The highest concentrations of both drugs were found in the bile. AME in a dose of 5 mg/kg body weight accumulated in the lung in amounts 12 to 46 (mean: 23) times greater than AMB in a dose of 1 mg/kg body weight. In the kidneys, AME exceeded AMB 3 to 10 (mean: 6) times, and attained concentrations 12 to 22 times greater than AMB in the urine. Neither drug accumulated in brain or cerebrospinal fluid.