Teicoplanin is a glycopeptide antibiotic comprising six closely related major components whose activities against specific microbial species differ. In order to clarify the significance of monitoring these components separately for determining the therapeutic effectiveness of teicoplanin, we measured the total and unbound concentrations of the main teicoplanin components in plasma and the unbound fractions in patients. Teicoplanin components in plasma were determined separately by high-performance liquid chromatography following a co-extractive clean-up procedure. The concentrations of unbound teicoplanin components were estimated after plasma ultrafiltration. The plasma concentrations of the main components of teicoplanin were strongly correlated with each other. The apparent elimination rate constants of total bound and unbound teicoplanin calculated by population pharmacokinetic parameters were almost same among the components. Furthermore, the mean population unbound clearance corrected by the unbound fraction was almost the same among the components. These results suggest that monitoring the individual components of teicoplanin has no clinical significance based on the pharmacokinetics of teicoplanin.
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