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血浆和尿液中罗索沙星及其N-氧化物代谢物的高效液相色谱分析。

High-performance liquid chromatographic analysis of rosoxacin and its N-oxide metabolite in plasma and urine.

作者信息

Kullberg M P, Koss R, O'Neil S, Edelson J

出版信息

J Chromatogr. 1979 May 11;173(1):155-63. doi: 10.1016/s0021-9673(01)80455-6.

Abstract

A high-pressure liquid chromatographic method for the analysis of rosoxacin and its pyridyl N-oxide metabolite in plasma and urine extracts is described. A statistical evaluation of the assay data has shown acceptable accuracy and precision for 0.5 to 25 microgram of rosoxacin or the metabolite per ml of plasma and for 2.5 to 60 microgram/ml of either compound in urine. The minimum quantifiable level for rosoxacin was 0.13 microgram/ml in plasma and 0.64 microgram/ml in urine; for the metabolite in plasma and urine, the corresponding values were 0.21 and 0.60 microgram/ml, respectively. The method was applied to plasma and urine from three dogs medicated orally with 5 mg/kg of rosoxacin. The pharmacokinetic parameters calculated for rosoxacin were: plasma halflife, 1.9 h; plasma clearance, 65 ml/min; volume of distribution, 11.31. The average total urinary excretion of rosoxacin as free and conjugated rosoxacin and its free N-oxide was 7.7 +/- 0.2% over the 48-h collection period.

摘要

本文描述了一种用于分析血浆和尿液提取物中罗索沙星及其吡啶基N-氧化物代谢物的高压液相色谱法。对测定数据的统计评估表明,对于每毫升血浆中0.5至25微克的罗索沙星或其代谢物,以及尿液中每毫升2.5至60微克的任何一种化合物,该方法具有可接受的准确度和精密度。罗索沙星在血浆中的最低可定量水平为0.13微克/毫升,在尿液中为0.64微克/毫升;对于血浆和尿液中的代谢物,相应的值分别为0.21和0.60微克/毫升。该方法应用于三只口服5毫克/千克罗索沙星的犬的血浆和尿液。计算得到的罗索沙星的药代动力学参数为:血浆半衰期1.9小时;血浆清除率65毫升/分钟;分布容积11.3升。在48小时的收集期内,罗索沙星以游离和结合形式及其游离N-氧化物形式的平均总尿排泄量为7.7±0.2%。

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