新セファマイシン系抗生物質CS-1170の各種動物における吸収, 分布, 代謝ならびに排泄

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  • ABSORPTION, DISTRIBUTION, EXCRETION AND METABOLISM OF A NEW CEPHAMYCIN ANTIBIOTIC, CS-1170, IN VARIOUS ANIMAL SPECIES
  • セファマイシンケイ コウセイ ブッシツ CS 1170 ノ カクシュ ドウブツ

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Pharmacokinetics and metabolic fate of CS-1170 were studied in mice, rats, rabbits, dogs and monkeys. It was found that there is a large species variation in the blood levels and urinary excretion and that monkey is the most suitable model for human pharmacokinetics.<BR>After subcutaneous or intramuscular administration (50mg/kg), the urinary recovery was lowest in rats (22%) followed by mice and dogs (60%) and rabbits (64%), while highest in monkeys (77%).<BR>The peak plasma concentration was also lowest in rats (27gg/ml) and highest in monkeys (150gg/ml).<BR>The species difference was found to be mainly due to that in the participation of biliary excretion and the excretion in cannulated animals was in the order: rabbits (1.3%) < dogs (15%) < rats (60%).<BR>The concentration in the bile was significantly higher in CS-1170 as compared to cefazolin in all animals tested.<BR>The distribution studies in rats and mice showed that the concentration of CS-1170 was high in the liver and kidney, followed by the plasma and lung, while low in the muscles, pancreas and spleen and none in the brain.<BR>The fate of CS-1170 in monkeys was studied in detail by bio-and radioassay with 7α-rnethoxyl-14C-labeled drug. The plasma level of radioactivity after intramuscular injection reached the maximum after 10 min and declined afterward with half-life of 48 min. In the plasma extracts, a single radioactive spot corresponding to CS-1170 was detected on TLC. Over 75% of the intravenous or intramuscular dose was recovered in the urine by both radio-and bioassay, the most part being excreted during the first 3 hr. In the TLC autoradiogram of urine, the main radioactive spot was observed corresponding to CS-1170. The counting experiment revealed that over 97% of the urinary radioactivity in the 3 hr urine is intact CS-1170. In the feces, about 15% of the radioactive dose was recovered in which 30-40% was detected as intact CS-1170. In the respiratory air, only about 1% of the dose was excreted as 14CO2, indicating that 7-methoxyl moiety is stable in the body.

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