Forty patients with chronic cholecystitis or cholelithiasis were prosp
ectively randomized for therapy with either ciprofloxacin or fleroxaci
n to study the penetration of these two agents into gallbladder tissue
, plasma, and bile. Patients received a 3-day course of ciprofloxacin
(500 mg twice a day) or fleroxacin (400 mg once daily) and were subdiv
ided into four groups reflecting intraoperative sample collection at 4
, 7, 14, and 25 to 26 h following the last quinolone dose. Mean concen
trations in plasma for ciprofloxacin and fleroxacin at 4 and 25 to 26
h postdose were 2.5 and 10 mu g/ml and 0.3 and 1.8 mu g/ml, respective
ly. The concentrations of ciprofloxacin and fleroxacin in bile and gal
lbladder wall tissue at 25 to 26 h postdose were 4.5 and 8.6 mu g/ml a
nd 1.2 and 4.4 mu g/ml, respectively. Both agents demonstrate rapid ti
ssue penetration with persistence at levels appropriate for treatment
of biliary pathogens.