[Clinical study on transfer into lung tissue and postoperative prophylactic effect of new cephamycin antibiotics,...

The following findings were obtained in our clinical study on the transfer of cefotetan (CTT) and cefbuperazone (CBPZ), new antibiotics of cephamycin series, into the lung tissue and on their postoperative prophylactic effect. 1. The mean serum concentration 30 minutes after the start of an intravenous drip infusion of 1 g of CTT over a period of 30 minutes was 99.4 micrograms/ml, and it decreased gradually thereafter with the half-life of 2.45 hours. After an intravenous drip infusion of 1 g of CTT over a period of 1 hour, the mean peak concentration of 104.1 micrograms/ml appeared 1 hour after the start of the infusion, and mean concentrations at 2, 4 and 6 hours after the infusion were 63.4, 34.3 and 27.0 micrograms/ml, respectively, with the half-life of 2.35 hours during phase beta. 2. Following 30 minutes of an intravenous drip infusion of CTT, the tissue CTT level in normal lung tissues was Tmax 1.82 hours and Cmax 19.8 micrograms/g. After 1 hour of an intravenous drip infusion the mean concentration in the tissues was at the peak of 39.7 micrograms/g in 2 hours after the start of an administration, while mean levels at 3, 4 and 6 hours after an administration were 32.2, 22.2 and 8.76 micrograms/g, respectively, with Tmax of 1.82 hours and Cmax of 30.5 micrograms/g. 3. Following an intravenous drip infusion of 1 g of CBPZ over a period of 1 hour, the mean serum drug concentration 1 hour after the start of infusion was at its peak, 83.3 micrograms/ml, while mean values at 2, 4 and 6 hours after the start of an administration were, respectively, 40.4, 19.8 and 9.62 micrograms/ml, with the beta-phase half-life of 2.03 hours. 4. By 1 hour after the start of intravenous drip infusion of CBPZ, the mean tissue level in normal lung tissues was at the peak of 31.6 micrograms/g, while mean levels at 3, 4 and 8 hours after an administration were 16.2, 11.0 and 4.56 micrograms/g, respectively, with Tmax of 1.67 hours and Cmax of 21.9 micrograms/g. 5. Infused CBPZ was transferred into bronchiole tissues. Drug concentrations in these tissues at 3 and 5 hours after the start of the infusion were 7.87 and 4.85 micrograms/g, respectively, with their ratios to the peak serum level were 9.4 and 5.8%, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)