In 12 fasting volunteers, the pharmacokinetics of ciprofloxacin (Bay o 9867; 1-cyclopropyl-6-fluor-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline carbonic acid) were determined after the administration of 50, 100, and 750 mg orally as well as 50 and 100 mg intravenously over 15 min. Serum

The pharmacokinetics of ciprofloxacin was studied in three groups of healthy volunteers comprising a total of 16 males and 16 females (age 21-35 years; body weight 52-80 kg). Single oral doses of 50, 100, 250, 500 and 750 mg were given to fasting subjects. The 250 mg dose was repeated after a breakfast. Intravenous doses of 50, 100 and 200 mg were given by short infusion in a randomized cross-over sequence. Concentrations of the drug in serum and urine were determined by high-performance liquid chromatography and by a microbiological assay. Mean peak concentrations between 0.37 +/- 0.49 mg/l (100 mg dose) and 1.97 +/- 0.50 (750 mg dose) were measured 60-75 min after oral administration. Twelve hours after 750 mg ciprofloxacin, serum concentrations were 0.15 +/- 0.05 mg/l. Taking a breakfast reduced absorption by 15-20% compared to the fasting state, as judged by peak concentrations, AUC and renal excretion. After 200 mg i.v. (20 min infusion period), initial serum concentrations of 4.0 +/- 1.2 mg/l were observed which declined 12 h later to 0.070 +/- 0.025 mg/l. Mean cumulated recovery of ciprofloxacin from urine over 24 h varied between 25.5% and 33.6% of oral doses and between 53.2% and 57.4% of intravenous doses. Two of the three metabolites seen in the chromatograms were identified as M1 and M3 (oxo-ciprofloxacin). Cumulated renal excretion after an oral 250 mg dose was 1.2 +/- 0.4% of M1 and 5.5 +/- 1.6% of M3.(ABSTRACT TRUNCATED AT 250 WORDS)

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Summary:Two column liquid Chromatographie (HPLC) methods for thexietermination of ciprofloxacin and three metabolites are described. Both use reversed phase chromatography, the stationary phase being Nucleosil 5C18. Method A separates ciprofloxacin, metabolite Ml and another metabolite of unknown structure using fluorometric detection. Method B allows the determinations of metabolite M3 (oxo-ciprofloxacin) in urine by UV absorption. Serum was deproteinised with acetonitrile. Urine was diluted with buffer solution. The detection limit of ciprofloxacin was 0.010 mg/1 serum and 0.2 mg/1 urine and for the metabolite M3, l mg/1 urine. Within-batch precision (coefficient of Variation) for ciprofloxacin in serum was 0.8 to 2.4% and between-batch precision 4.8 to 9.3%. In urine within-batch precision was 1.7 to 2.1% and between-batch precision 2.4 to 7.2%. Recovery rates of ciprofloxacin from three groups of spiked sera was 94.5 ± 2.6%, 97.2 + 1.1% and 95.0 ± 1.8% and from urine 99.6%. Results obtained by HPLC (method A) were compared with those from a Standard microbiological assay by means of bivariäte regression analysis. In 12 subsets of data the slope of the regression line varied from 1.042 to 1.556. Significantly higher results from the microbiological assay were probably due to the presence of microbiologically active metabolites. We conclude that HPLC is the more specific method of determination. The described methods were applied for pharmacokinetic studies and therapeutic drug monitoring. Flüssigkeitschromatographische Bestimmung von Ciprofloxacin in menschlichen Körperflüssigkeiten

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