Abstract: 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.

Key words: Thiamphenicol, Thiamphenicol glycinate, HPLC, Pharmacokinetics