国产辛伐他汀片剂人体生物利用度研究

RELATIVE BIOAVAILITY OF SIMVASTAIN TABLET IN HEALTHY VOULUNTEERS

8名健康男性受试者随机自身交叉给药,分别口服单剂量40mg国产辛伐他汀片剂和进口片剂进行相对生物利用度研究。采用气相色谱/质谱联用测定血浆中辛伐他汀的体内水解物 β-羟基酸代谢物浓度,经3p97生物利用度计算程序处理拟合,符合一室模型,并得国产和进口辛伐他汀片剂的试验结果如下:AUC0 -∞ 分别为19.016±2.255μg·h·L-1 和20.444±2.830μg·h·L -1,Tpeak 分别为2.71±0.19h和2.69±0.20h,Cmax 分别为1.82±0.23μg·L -1和1.93±0.31μg·L-1 ,经配对t-检验,两者的主要药代动力学参数均无显著性差异(P>0.05)。经方差分析和双单侧检验结果表明两者具有生物等效性。国产辛伐他汀片剂的相对生物利用度为94.9 %±6.0 %。

A single oral dose of 40mg domestic and imported simvatatin was given to 8 healthy volunteers in a randomized crossover study, simvatatin's active metabolite concentration in plasma were determined by GC/MS method . The pharmacokinetics and bioavailability were studied . The results showed that the plasma concentration_time curves of the two products were all fitted to one-compartment model. Tpeak of domestics and imported tablets were 2.71±0.19 h and 2.69±0.20 h, AUC0-∞ were 19.016±2.255 μg·h· L-1 and 20.444±2.830 μg·h·L-1, Cmax were 1.82±0.23 μg· L-1 and 1.93±0.31 μg· L-1,the relative bioavailability of domestics to imported tablets was 94.9±6.0%. There were no statistically singnificant difference between the two parameters(P>0.05). The results demonstrated that two preparations were bioquivalent.