1988 Volume 36 Issue 7 Pages 487-492
We studied the excretion of cefoperazone (CPZ) into choledochal bile to determine the appropriate dose and route of administration.
Choledochal bile was collected every 30 or 60 minutes from 6 patients with T-tube drainage. Each patient was examined 3 times in one week (cross-over method) after (1) bolus injection of 1g intravenously (1g i. v.), (2) bolus injection of 2g (2g i. v.) and (3) drip infusion of 2 g for 60 minutes (2g d. i. v.). The concentration of CPZ was measured by thin layer disc method.
The peak concentration, the peak time (time during which the concentration of the drug is higher than a half of the peak level) and the area under the curve of CPZ in bile were as follows (1) 1g i. v.: 748 μg/ml, 7.43 h, 5, 613 eμg·Eh/ml;(2) 2g i. v.: 1, 897μg/ml, 6.62h, 13, 536μg-h/ml and (3) 2g d. i. v.: 1, 855μg/ml, 6.15h, 11, 923μg·Eh/ml. The time-concentration curve of CPZ was gently-sloping, the concentration of CPZ at 10 h after administration being 380μg/ml (1g i. v.), 614μg/ml (2g i. v.) and 642μg/ml (2g d. i. v.).
In summary, excretion of CPZ into choledochal bile was excellent: the higher the dose, the higher the concentration of the drug in bile. The results of 2g i. v. and 2 g d. i. v. were similar. No prolongation of the peak time was achieved in the drip-infusion group.
From the above results, we consider CPZ a useful drug for the treatment of biliary tract infection. However, therapy with 0.5g or one injection per day should be examined.
