McCoy L F, Crawmer B P, Benziger D P
Antimicrob Agents Chemother. 1985 May;27(5):769-73. doi: 10.1128/AAC.27.5.769.
An analytical method for the quantitation of amifloxacin, 6-fluoro-1,4-dihydro-1-(methylamino)-7-(4-methyl-1-piperazinyl)-4-oxo-3- quinolinecarboxylic acid, in plasma and urine has been developed. The method involves extraction with chloroform, back-extraction into 0.1 M sodium hydroxide, and subsequent analysis by reverse-phase high-pressure liquid chromatography with UV detection. The precision of the assay calculated as the overall standard deviation was +/- 4.9% in plasma and +/- 1.1% in urine. The range of mean percent differences from the nominal values was used as an estimate of accuracy and was 93.6 to 103% of the nominal values in plasma and 95.2 to 107% of the nominal values in urine. The minimum quantifiable levels were 0.032 micrograms/ml in plasma and 2.7 micrograms/ml in urine. The methods were employed in a pharmacokinetic analysis of amifloxacin after intravenous administration to rhesus monkeys. The decline in drug plasma levels was described by a biexponential process with mean rates of 8.4 h-1 and 0.32 h-1 with corresponding half-lives of ca. 5 min and 2.2 h. Amifloxacin was rapidly excreted, with ca. 53% of the dose appearing in the urine within 48 h after medication. The mean renal clearance +/- standard deviation was 4.4 +/- 1.0 ml X kg-1 X min-1 and is compatible with passive glomerular filtration in this species.
已开发出一种用于定量测定血浆和尿液中阿米氟沙星（6-氟-1,4-二氢-1-(甲氨基)-7-(4-甲基-1-哌嗪基)-4-氧代-3-喹啉羧酸）的分析方法。该方法包括用氯仿萃取，再反萃取到0.1 M氢氧化钠中，随后通过反相高效液相色谱法和紫外检测进行分析。以总标准偏差计算的测定精密度在血浆中为±4.9%，在尿液中为±1.1%。平均百分比差异与标称值的范围用作准确度的估计值，在血浆中为标称值的93.6%至103%，在尿液中为标称值的95.2%至107%。最低可定量水平在血浆中为0.032微克/毫升，在尿液中为2.7微克/毫升。这些方法用于对恒河猴静脉注射阿米氟沙星后的药代动力学分析。药物血浆水平的下降由双指数过程描述，平均速率分别为8.4 h-1和0.32 h-1，相应的半衰期约为5分钟和2.2小时。阿米氟沙星排泄迅速，给药后48小时内约53%的剂量出现在尿液中。平均肾清除率±标准偏差为4.4±1.0毫升·千克-1·分钟-1，与该物种的被动肾小球滤过情况相符。
