Distribution of doubly radiolabelled amphotericin B methyl ester and amphotericin B in the non-human primate, Macaca mulatta

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Abstract
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.