Pharmacokinetic comparison of cefroxadin (CGP 9000) and cephalexin by simultaneous administration to humans

Abstract

The pharnacokinetic parameters of cefroxadin and cephalexin were compared after simultaneous oral administration of the two cephalosporins to 21 subjects.The influence of the dose, the formulation, and food intake on these parameters was investigated. Both drugs were equally well absorbed from all of the tested fornulations; identical percentages of the dose were recovered in the urine in all cases. The elimination half-life of cefroxadin and, consequently, the area under the plasma concentration-time curve were about 10% less than those ofcephalexin. Plasma concentrations and cumulative excretion curves of the two drugs were almost superimposable. Food intake had the same effect on both drugs; absorption was slowed, but the amounts absorbed were almost the same as those in fasted subjects.

Pharmacokinetics of β-Lactam Antibiotics

“…Serum levels are proportional to dose, and administering the drug with food has only a slight effect on the rate and extent of drug absorption. Multiple oral dose administration (0.75, 1.0, or 2.0 g every 6 h or 1.0 g every 4 h) resulted in no drug accumulation in serum (GOWER and DASH 1969;BERGAN et al 1970;LoDE et al 1979;GRIFFITII and BLACK 1971;CHOW et al 1979;LECAILLON et al 1980;HENNESS et al 1978;FINKELSTEIN et al 1978). However, some accumulation may occur on a regimen of 1.5 g every 6 h (JOLLY et al 1977).…”

“…Oral doses of solution or tablets ranging from 125-1,500 mg given to healthy volunteers, produced peak plasma levels of drug in 30-90 min. Plasma levels are proportional to dose and 88%-96% of the dose is recovered unchanged in urine in 12 h. Renal clearance ranged from 240-340 ml/min in the different groups studied (WIRZ et al 1979;LoDE et al 1979;LECAILLON et al 1980;BERGAN 1980). Ingesting an oral dose of cefroxadine with food delays the time of peak plasma levels of drug and reduces absorption by 5%-10% .…”

A specific and rapid HPLC assay for the determination of cefroxadine in human plasma and its application to pharmacokinetic study in Korean

“…The sample preparation method reported by Lecaillon et al [5] was modified in this study. To 200 L of plasma, 10 L of internal standard solution and 20 L of 60% trichloroacetic acid were added.…”

“…For the determination of the pharmacokinetic parameters of cefroxadine in biological samples, microbial assays or high pressure liquid chromatography (HPLC) has been used in a number of studies [4][5][6][7][8][9][10][11]. Most of the HPLC methods reported previously are mainly based on the method developed by Lecaillon et al [5,8,9,11,12]. Although the HPLC method was more accurate and precise than microbiological determination, the peaks were not well resolved and had slow retention times.…”

“…1A) is one of the frequently prescribed oral cephalosporins with a broad antibacterial spectrum [1][2][3]. For the determination of the pharmacokinetic parameters of cefroxadine in biological samples, microbial assays or high pressure liquid chromatography (HPLC) has been used in a number of studies [4][5][6][7][8][9][10][11]. Most of the HPLC methods reported previously are mainly based on the method developed by Lecaillon et al [5,8,9,11,12].…”