Studies on Absorption, Distribution, Metabolism and Excretion of a New Macrolide Antibiotic SF-837. I. Absorption, Metabolism and Excretion of SF-837

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The comparative absorption, metabolism, and excretion of SF-837 substance, a new macrolide antibiotic, was studied in rat, dog and man. Blood, urine and bile analysis were performed on these animals collected at several times after either oral ingestion or intravenous administration of a dose. SF-837 was found to be rapidly absorbed in rats and once in the body, was metabolized to M1 substance and M2 substance in rats, dogs and men. By densitometric analysis of thin-layer chromatograms, the urinary antimicrobial activities were analyzed falling in with 2.0%of unchanged SF-837,18.0% of M1 and 1.7%of M2,and the biliary were analyzed falling in with 0.02% of unchanged SF-837,5.8% of M1 and 47.3% of M2,within 24 hours after intravenous administration of SF-837 (50 mg/kg). Namely the main metabolite in the urine was M1 substance and that in the bile was M2 substance. The antimicrobial activity in the blood was derived mostly from M1 substance, not only by intravenous administration but also oral in rats. Similar results were obtained also from dogs and men. These results inficated that SF-837 was metabolised mainly to M1 substance and then M2 substance in rats, dogs and men.
社団法人日本薬学会の論文
1973-08-25