关键词: 丙硫氧嘧啶, HPLC, 药代动力学, 生物利用度

Abstract: AIM: To study the pharmacokinetics and relative bioavailability of propylthiouracil tablet in Chinese healthy male volunteers.METHODS: The bioequivalence and relative bioavailability of a test domestic formulation of propylthiouracil in comparison with a reference imported formulation was investigated in a randomized 2-way cross-over study in 20 healthy volunteers following a single oral dose of 200 mg.The washout period was 1wk.Plasma concentrations of propylthiouracil were determined by a HPLC system equipped with a ultraviolet detector.RESULTS: The following pharmacokinetical parameters were derived from the individual plasma concentration time courses.The main parameters for test and reference formulations,C_max were(5.7±1.5)and(5.8±1.8)mg·L^-1;t_max were(1.4±0.8)and(1.4±0.7)h;t_1/2were 1.7±0.3 and(1.7±0.2)h;AUC_0-t were(18.0±4.4)and(17.8±4.6)mg·h·L^-1;AUC_0-∞were(18.1±4.5)and(17.9±4.7)mg·h·L^-1,respectively.Compared with reference formulation,the relative bioavailability(F)of test formulation was(101.9±13.2)%。The above parameters obtained from two formulations were compared by analysis of variance(ANOVA)and no significant difference was found.The bioequivalence of two formulations was found assessed by two one-side ways test(p<0.05).CONCLUSION: Therefore,from the results of this study it can be concluded that the test formulation is bioequivalent with the referenceformulation.

Key words: propylthiouracil, bioavailability, HPLC