【摘要】 目的 评价非布司他片受试制剂与参比制剂在中国健康受试者中的生物等效性。方法 采用单次给药、开放、随机、两周期、两制剂、双交叉试验设计，空腹组和餐后组分别入组50例和42例受试者，每周期分别口服40 mg受试制剂或参比制剂，用液相色谱-串联质谱法测定血浆中非布司他的浓度，用PhoenixWinNonlin 7.0和SAS 9.4软件分析生物等效性。结果 空腹单次给药非布司他片受试制剂和参比制剂的C_max分别为（2 087.86±710.89）和（2 057.88±601.91）ng·mL^-1,AUC0-t分别为（5 802.30±1 620.08）和（5 771.11±1 491.04）h·ng·mL^-1,AUC0-∞（5 958.56±1 639.40）和（5 925.41±1 515.15）h·ng·mL^-1。餐后单次给药非布司他片受试制剂和参比制剂的C_max分别为（1 645.79±701.71）和（1 832.86±714.04）ng·mL^-1,AUC0-t分别为（4 797.92±1 379.01）和（4 851.88±1 306.75）h·ng·mL^-1,AUC0-∞（4 951.55±1 357.99）和（5 007.03±1 308.32）h·ng·mL^-1。2种制剂空腹和餐后的C_max、AUC0-t和AUC0-∞几何均值比值及其90%置信区间均在80.00%～125.00%之间。结论 空腹和餐后条件下，2种非布司他片在中国健康受试者中具有生物等效性。更多还原

【Abstract】 OBJECTIVE To evaluation the bioequivalence of febuxostat tablets between test formulation and reference formulation in Chinese healthy subjects. METHODS A single-dose,random,open-label,two-formulation,two-period,double crossover study design was used. 50 Chinese healthy subjects were assigned to the postprandial group and 42 to the fasting group. A single dose of test and reference febuxostat tablets was given to Chinese healthy subjects in each period. The plasma concentration of febuxostat was determined by HPLC-MS/MS,and bioequivalence was analyzed using Phoenix Win Nonlin 7.0 and SAS 9.4 software. RESULTS The pharmacokinetic parameters of febuxostat tablets after oral adminstration were as follows. Fasting group C_max were（2 087.86±710.89） and（2 057.88±601.91） ng·m L^-1. AUC0-t were（5 802.30±1 620.08） and（5 771.11±1 491.04） h·ng·m L^-1. AUC0-∞ were（5 958.56 ± 1 639.40） and（5 925.41 ± 1 515.15） h·ng·m L^-1. Postprandial group C_max were（1 645.79 ± 701.71） and（1 832.86±714.04） ng·m L^-1,AUC0-t were（4 797.92±1 379.01） and（4 851.88±1 306.75） h·ng·m L^-1,AUC0-∞ were（4 951.55±1 357.99） and（5 007.03±1 308.32） h·ng·m L^-1. The 90% confidence intervals of the geometic mean ratios of C_max,AUC0-t and AUC0-∞ for the test and reference formulations were between 80.00% and 125.00% under fasting and postprandial conditions. CONCLUSION The test and reference febuxostat tablet are bioequivalent in Chinese healthy subjects under fasting and postprandial conditions.更多还原