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To characterize the effect of the binding of antibiotics to tissue protein on urinary excretion, we examined the extent of the binding of 9 penicillins and 9 cephems to 100,000 X g supernatant fluid of human liver homogenates. The correlation analysis revealed a significant simple correlation between the binding to 100,000 X g supernatant fluid of liver homogenates and urinary excretion. Drugs with lesser binding were mainly excreted in the urine, conversely, urinary excretion of highly bound drugs exhibited lower values. The prediction with regard to urinary excretion of healthy subjects was done by multiple regression analysis using the binding to 100,000 X g supernatant fluid and other physicochemical factors. The values predicted for urinary excretion coincided well with the observed values.

journal of antibiotics

Studies on protein binding of antibiotics. V. Effect of the binding of drug to 100,000*g supernatant fluid of human liver homogenates on urinary excretion.