[Transfer of cadrofloxacin, a novel fluoroquinolone antibacterial, into the gallbladder tissue and bile].

Clinical pharmacological studies of a novel fluoroquinolone antibacterial drug, cadrofloxacin, were performed in 12 surgical patients by investigating the transfer of cadrofloxacin into the gallbladder tissue and bile. They were scheduled for cholecystectomy (n = 6) or had undergone a percutaneous transhepatic biliary drainage (n = 5) or gallbladder drainage (n = 1) at the Second Department of Surgery, Wakayama Medical University. A single dose of cadrofloxacin was orally administered to all patients at a dose of 200 mg. The results were as follows: 1) Serum and gallbladder tissue levels of cadrofloxacin after 2.9-5.7 hours were 0.6-2.5 micrograms/ml and 0.6-8.6 micrograms/ml, respectively. The gallbladder/serum ratios of drug concentration were 0.6-3.4. 2) Levels of cadrofloxacin in bile reached a peak of 2.5-12.9 micrograms/ml after individually different period of time. Cumulative bile recoverlies of cadrofloxacin (unchanged compound + glucuronide conjugate) within the first 6 hours were 0.02-0.49%, and 0.08-0.75% within 0-12 hours. The mean value of [glucuronide conjugate/unchanged compound] in bile was 37%, although the values depended on the patients.