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目的:评价2种双醋瑞因制剂在人体内的生物等效性。方法:20例男性健康志愿者随机交叉单剂量口服试验制剂和参比制剂,利用液相-质谱联用法(LC-MS/MS)法测定大黄酸体内的血药浓度。结果:试验制剂和参比制剂的主要药动学参数如下:AUC_(0-t)分别为(25 205.6±15 694.9)μg·h·L~(-1)和(24 927.7±15 869.8)μg·h·L~(-1);AUC_(0-∞)分别为(26 266.3±17021.4)μg·h·L~(-1)和(25 961.7±16 592.5)μg·h·L~(-1);C_(max)分别为(4 276.8±2 391.8)μg·L~(-1)和(4 352.8±2 415.4)μg·L~(-1);t_(max)分别为(2.3±0.7)h和(2.3±0.8)h;t_(1/2)分别为(4.5±1.4)h和(4.4±0.9)h;经方差分析和双单侧t检验显示,主要药动学参数无显著差异,以AUC_(0-t)计算大黄酸的相对生物利用度为(105.2±22.6)%。结论:试验制剂与参比制剂具有生物等效性。
OBJECTIVE: To evaluate the bioequivalence of two diacerein preparations in humans. Methods: Twenty healthy male volunteers were randomized to crossover single dose oral test formulation and reference formulation. The plasma concentration of rhein was determined by liquid chromatography-mass spectrometry (LC-MS / MS). RESULTS: The main pharmacokinetic parameters of the test and reference preparations were as follows: AUC_ (0-t) were (25 205.6 ± 15 694.9) μg · h · L -1 and (24 927.7 ± 15 869.8) μg · H · L -1 and AUC 0 -∞ were 26 266.3 ± 17021.4 μg · h · L -1 and 25 961.7 ± 16 592.5 μg · h · L -1, 1 and Cmax were (4 276.8 ± 2 391.8) μg · L -1 and (4 352.8 ± 2 415.4) μg · L -1, respectively; t max were 2.3 ± (4.5 ± 1.4) h and (± 4.4 ± 0.9) h, respectively. The variance analysis and double unilateral t-test showed that the main pharmacokinetic parameters were as follows: Significant difference, the relative bioavailability of rhein calculated by AUC_ (0-t) was (105.2 ± 22.6)%. Conclusion: The test preparation and the reference preparation are bioequivalent.