Absorption, distribution, excretion and metabolism of cefmetazole in cynomolgus monkeys.

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Abstract
The pharmacokinetics and metabolic fate of cefmetazole (CS-1170, CMZ) were studied in cynomolgus monkeys by means of combination of radio- and bioassay techniques and that of 3 radioactive drugs labeled at the different moiety of the molecule. The plasma level of radioactivity after i.m. injection of cefmetazole[methoxy-14C] (50 mg/kg) reached the maximum levels (185 .mu.g/ml) after 10 min and declined with a half-life of .apprx. 48 min. In the TLC of the plasma extracts, a single radioactive spot was detected corresponding to unchanged cefmetazole. Repeated i.v. administration for 1 and 2 wk showed no effect on the plasma levels and half-lives. More than 75% of the i.v. or i.m. dose was recovered in the urine by radio- and bioassay, the most part being excreted during the first 3 h period. On the TLC of urine, 93-97% was detected as unchanged cefmetazole. In the bile, the most part (> 80%) was detected as unchanged cefmetazole. In the feces, .apprx. 15% of the dose was recovered, in which 30-40% was detected as intact cefmetazole. The metabolic fate of [3-35S] and [7-35S]cefmetazole was described and discussed. The whole-body autoradiography in the monkeys was also presented.