国产马来酸伊索拉啶片剂人体生物等效性研究

Bioequivalence of Irsogladine Maleate Tablets in Healthy Volunteers

12名健康受试者随机交叉给药，分别口服单剂量国产马来酸伊索拉啶片剂及进口片剂8mg进行生物等效性的研究。采用高效液相紫外检测法测定血浆中马来酸伊索拉啶的浓度，经3p97中生物等效性程序计算处理，被试制剂和标准参比制剂的：Tpeak分别为8.67±2.15h和9.00±2.23h，Cmax分别为300.09±20.21μg·L-1和302.48±21.91μg·L-1，T1/2ke分别为127.18±16．83h和126．24±19．88h，经配对t检验，两者的AUC0-t，Teak,Cmax,T1/2Ke等主要药代动力学参数均无显著性差异（P＞0.05）。采用梯形法计算的两者的AUC0-t产值分别为37500.59±7605.32μg·h·L－1和38518．18±6934.74μ·h·L－1，经统计学分析，被试制剂和标准参比制剂具有生物等效性。被试制剂的相对生物利用度为97．3±5．9％。

The bioequivalence of domestic irsogladine maleate tablets was studied in 12healthy male volunteers. A dose of 8mg of domestic or imported irsogladine maleate (testand reference preparation) was given according to a randomized 2-way cross-over design.Blood samples were withdrawn up to 504 hours post administration, and plasmaconcentration of irsogladine maleate was determined by high performance liquidchromatography(HPLC) method. The concentration-time curves of the two preparationswere fitted to a two-compartment model. The peak plasma levels (Cmax) of irsogladinemaleate test drug and reference drug were 300.09±20.21 and 302.48±21.91μ g·L-1,respectively, the peak time (Tmax)were 8.67± 2.15h and 9.00±2.34h, respectively， T1/2Kewere 127. 18±16.83h and 126.24±19.88h, respectively, and AUC0-t, were 37500.59±7605.32 and 38518.18±6934.74 μg·h·L-1, respectively. The relative bioavailabilitydata obtained in the study provided definite proof of bioequivalence of both domesticirsogladine maleate tablets and imported irsogladine maleate tablets. The relativebioavailability of the test drug was 97.3±5.9%.