[Clinical studies with cefoperazone in the biliary disease]

The concentration of cefoperazone (CPZ) in serum and bile was estimated after intravenous drip infusion of 1 g of the drug in 11 patients, who have performed cholecystectomy, choledocholithotomy and T-tube drainage for gallstone diseases. Administration of cefazolin (CEZ) 1 g was compared by the cross over method. After 1 g intravenous drip infusion of CPZ, the mean serum concentration was 88.3 +/- 24 micrograms/ml at 1 hour, 52 +/- 11.7 micrograms/ml at 2 hours and 36.5 +/- 10 micrograms/ml at 4 hours. The maintenance period of serum concentration was inclined to be longer in CPZ than in CEZ. After 1 g intravenous drip infusion of CPZ, the mean bile concentration reached to 810 +/- 459 micrograms/ml in 2 hours and it was maintained as high as 562 +/- 319 micrograms/ml even after 4 hours. On the other hand, after 1 g intravenous drip infusion of CEZ, the mean bile concentration was only 28.7 +/- 26 micrograms/ml in 1 hour and was low level in the progress. As compared with the highest concentration of CPZ and CEZ in same patient, the mean bile concentration of CPZ (942 +/- 525 micrograms/ml) was about 30 times higher than that of CEZ (28.6 +/- 26.3 micrograms/ml). There was no difference in the group of Gram-positive cocci between minimum inhibitory concentration (MIC) of CPZ and that of CEZ. While MIC of CEZ in the group of Gram-negative bacilli was from 0.78 to over 400 micrograms/ml, MIC of CPZ in that group was from 0.10 to 50 micrograms/ml. The value in CPZ was lower than that in CEZ at all strains. No side effects was seen in all patients.