Cephacetrileの基礎および臨床研究

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タイトル別名
  • LABORATORY AND CLINICAL INVESTIGATION ON CEPHACETRILE
  • Cephacetrile ノ キソ オヨビ リンショウ ケンキュウ

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The laboratory and clinical investigations were carried out on a new derivative of cephalosporin-Cephacetrile (CEC). and the following results were obtained.<BR>1) In susceptibility test using clinically isolated bacteria, MICs of both CEC and CEZ on 20/21 strains of Staph. aureus were found less than 1.6 μg/ml, and those of 13/14 of E. coli were less than 12.5 and 3.2 μg/ml respectively, whereas most of Klebsiella-Enterobacter and Pseud. aeruginosa were not inhibited at the concentration of 100 μg/ml of these drugs.<BR>2) The activity of desacetylated metabolite of CEC both on Staph. aureus and E. coli decreased to 1/2-1/4 of parent substance. Desacetyl-lactone form did not show the activity practically.<BR>3) In i. m. absorption and excretion study in human subjects using cup plate method, B. subtitis as the test organism, mean blood level attained to peak of 21.3 μg/ml at 1 hour. Calculated half life, in the blood was found to be about 1.8 hours. Twenty-60% of dose was recovered in 8 hours as active substance in urine.<BR>4) In study of protein binding, the bound ratios of CEC and CED were about 38.5-50 and 11-20% respectively by the cellophane bag dialysis.<BR>5) In the study of metabolism using TLC, CEC and its desacetylated metabolites were found in urines of a patient following multiple i. m. administration.<BR>6) In clinical investigation, 25 cases including 9 cases with R. T. I. and 13 cases with U. T. I. were treated daily 2-39 i. m. or i. v. administration of CEC. Twenty-two cases responded well but relapses have occurred in 3 cases. Two cases with biliary tract infection and one with septicemia due to Klebsiella resistant to cephalosporins did not respond. Laboratory values before and after the treatment showed no abnormal fluctuation except for 3 cases with decrease in RBC after the treatment.

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