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Seventeen patients with various grades of kidney function were injected each with cefsulodin (CFS) 1 g dissolved in 20 ml of saline. Serum and urine concentrations of CFS were determined using high performance liquid chromatography up to 24 hours after administration. Pharmacokinetic analysis was done using a two-compartment model. The results were discussed by comparing creatinine clearance (Ccr) values divided into 4 groups: greater than or equal to 70 ml/min (group I), 50-less than 70 ml/min (group II), 30-less than 50 ml/min (group III), and less than 30 ml/min (group IV). A delay in the disappearance of CFS from the blood was observed with a decrease in Ccr. Half-lives of CFS in blood (T 1/2 beta) were 1.03 hours (group I), 2.09 hours (group II), 3.44 hours (group III), and 4.52 hours (group IV). Serum clearance (Cls) and Ccr were found to be related with an equation: Cls = 1.60 x Ccr + 7.70. The correlation coefficient (r) was 0.881. Ccr and T 1/2 beta were found to be related with an equation: T 1/2 beta = 31.27 x Ccr-0.688, and the area under the curve (AUC) was found to be related to Ccr with AUC = 4,226 x Ccr-0.81. Urinary excretion rates up to 24 hours after administration were 84.4% (group I), 69.1% (group II), 67.5% (group III), and 56.5% (group IV). This means that CFS is excreted in urine with a relatively high recovery even in the case of low Ccr less than 30 ml/min.

Hydrogen bromide adduct of neocarzinostatin chromophore: One of the stable derivatives of native neocarzinostatin chromophore.