ABSORPTION, EXCRETION AND METABOLISM OF CEPHACETRILE AS COMPARED WITH CEPHALOTHIN AND CEFAZOLIN
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Using a cross-over method, pharmacokinetic study of Cephacetrile (CEC) was carried out on 5 patients. The results were compared with those of Cephalothin (CET) and Cefazolin (CEZ).<BR>1. A solution of CEZ mixed with human serum and a solution of CEC diluted with a phosphate buffer achieved the highest blood levels, while with CET, the lowest levels were attained both with the mixture and the dilution. Regarding the time required for decrease in blood values, CET was the shortest, CEZ the longest, and CEC in between the two. <BR>2. The maximum urinary concentration was attained with CET, while CEZ showed the least. Urine collected 4-6 hours after the administration showed that the highest concentration was obtained with CEZ, CET was the lowest and CEC was in between.<BR>3. Presence of metabolites in the blood and urine was examined using a bioautogram. No metabolite was detected in the blood of patients administered CEC. Approximately 1.7% (average) of desacetyl compound was demonstrated in the urine, but the amount is not expected to affect the potency of CEC as measured by the cup method. CET group demonstrated approximately 40% desacetyl compound in the blood and 39% in the urine. In a patient about 76-86% desacetyl compound was demonstrated in the blood. In view of this data the desacetyl compound may affect the potency of CET as measured by the cup method. any metabolite of CEZ was not detected in both blood and urine of patients administered this drug.<BR>4. Total urinary excretion rates, including metabolites, were as high as 70-80% for all three brugs.<BR>Although CEC demonstrates similar pharmacokinetic behavior to that of CEZ, CEC seems to be evaluated between CET and CEZ.
- 公益社団法人 日本化学療法学会の論文
公益社団法人 日本化学療法学会 | 論文
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