Abstract

Cefoperazone is a third generation cephalosporin antibiotic with a broad spectrum against gram-positive and gram-negative bacteria. It is clinically effective in the treatment of the biliary tract infections. In the present study, we utilized microdialysis sampling technique with shunt linear probe for continuous monitoring levels of cefoperazone from rat biliary ducts. The effects of berberine (a potential P-glycoprotein enhancer) pretreatment were also evaluated. Analysis of cefoperazone in the dialysates was achieved using a reversed phase RP-18 column (250mm×4.6mm i.d.; particle size 5μm) maintained at ambient temperature. The mobile phase comprised 100mM monosodium phosphate (pH 5.5)–methanol (70:30, v/v), and the flow rate of the mobile phase was 1ml/min. The UV detector wavelength was set at 254nm. The area under the concentration–time curve and elimination half-life of cefoperazone were about 242.3±13.4minmg/ml and 64.1±28.2min, respectively. No significant effect was showed on the pharmacokinetics of cefoperazone with berberine pretreatment. This study represents a successful application of biliary microdialysis sampling technique, which is feasible for pharmacokinetic and biliary drug excretion studies.

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