Simultaneous determination of thiamphenicol and its prodrug thiamphenicol glycinate in human plasma and its pharmacokinetics study

AIM:To develop a simple and sensitive HPLC method for simultaneous determination of thiamphenicol(TAP) and its prodrug thiamphenicol glycinate(TG) in human plasma.METHODS:A single(0.5,1.0,and 1.5 g) intravenous drip doses of thiamphenicol glycinate was performed on 24 Chinese healthy volunteers randomly.The plasma was treated with ethyl acetate.The chromatographic condition was as follows:a column of Hypersil ODS2(5 μm,4.6 mm×200 mm),a mobile phase consisting of acetonitrile-water containing 0.003 mol/L tetrabutyl ammonium bromide and 0.056 mol/L ammonium acetate(13∶87,pH=6.6) at a flow rate of 1 mL/min with UV detection at 224 nm.RESULTS:The calibration curves of TAP and TG were all linear ranging from 0.78 to 100 μg/mL in plasma and the intra-day and inter-day relative standard deviations were all less than 15%.TAP was stable in plasma samples after extraction or in two freeze-thaw cycles or in 4 h at ambient temperature or at-70 ℃.CONCLUSION:The method is sensitive,accurate,simple,fast and is suitable for the pharmacokinetics study of TAP and TG.