[A clinical study on cefotiam with special reference to excretion in bile and concentration in gallbladder tissue]

Following 1 hour intravenous drip infusion of 1.0 g of cefotiam (CTM), 38 patients with cholelithiasis were operated at scheduled intervals. The CTM concentrations in serum, common duct bile, gallbladder bile and gallbladder tissue were measured. The mean level of CTM concentration in serum showed a peak of 53.1 micrograms/ml at 1 hour, and decreased in the level of 1.0 microgram/ml at 5 hours after administration. CTM concentrations in common duct bile revealed a mean level of 162 micrograms/ml at 1 hour and similarly high concentrations from 1 to 5 times of the peak level in serum were maintained for 3.5 hours. In patients with impaired liver function, the levels of CTM concentration were lower than those without them. CTM concentrations in gallbladder bile showed a high value at 2-3.5 hours after administration . In many cases the levels were relatively lower than those in common duct bile, particularly ion patients with cystic duct obstruction and/or with marked chronic cholecystitis. As for gallbladder tissue levels, CTM concentrations showed low levels less than 50 micrograms/g in patients with pathological changes of gallbladder, as well as in gallbladder bile. While, favorable concentrations of 50-100 micrograms/g were obtained in patients without them. There was a positive correlation between CTM concentrations in common duct bile and gallbladder bile, and also between the concentrations in gallbladder bile and those in gallbladder tissue in patients without cystic duct obstruction or marked chronic cholecystitis. Then, in the situation, CTM transfer into gallbladder bile or gallbladder tissue might be mainly dependent on biliary excretion of CTM.(ABSTRACT TRUNCATED AT 250 WORDS)