国产与进口盐酸沙格雷酯片在健康人体的生物等效性

Bioequivalence of domestic and imported sarpogrelate hydrochloride tablets in healthy volunteers

目的研究国产与进口盐酸沙格雷酯片(抗血栓药)的相对生物利用度,评价2者的生物等效性。方法采用双周期自身交叉试验设计,单剂量口服给药。24名健康男性受试者分别单剂量口服受试制剂和参比制剂,血浆样品采用高效液相色谱-串联质谱法检测。结果受试制剂及参比制剂盐酸沙格雷酯片的主要药代动力学参数:Cmax分别为(710.25±305.79),(653.33±311.06)μg·L-1;tm ax分别为(0.39±0.23),(0.38±0.19)h;t1/2分别为(0.72±0.10),(0.67±0.10)h;AUC0-tn分别为(473.80±216.83),(440.17±440.17)μg·h·L-1;AUC0-∞分别为(479.88±224.77),(443.79±144.70)μg·h·L-1;受试制剂盐酸沙格雷酯片的相对生物利用度F0-tn、F0-∞分别为(110.24±38.24)%,(110.64±39.07)%。结论受试制剂和参比制剂具有生物等效性。

Objective To study the bioavailability of domestic and imported sarpogrelate hydrochloride and evaluate the bioequivalence between two preparations. Methods A single oral dose of sarpogrelate hydrochloride was given respectively to 24 healthy male volunteers in a two -way cross over test and serum drug concentrations were determined by HPLC - MS/MS. Results The main pharmaeokinetie parameters of the test preparation and reference preparation were as follows： Cmax were （710. 25 ±305.79）and（653.33 ±311.06）μg·L^-1; tmax were （0. 39 ± 0. 23）and（0. 38 ±0. 19）h; t1/2 were（0. 72 ±0. 10）and（0. 67 ±0. 10）h ;AUC0-tn were（473.80 ±216. 83） and（440. 17 ±440. 17）μg·h·L^-1; AUC0-∞ of were （479. 88 ±224.77） and （443.79 ±144. 70） μg·h·L^-1; F0-tn, F0-∞ of test preparation were （ 110. 24 ±38.24）% and （ 110. 64 ±39.07 ） %. Conclusion The test preparation was bioequivalent to the reference preparation.