盐酸西替利嗪胶囊的人体生物利用度研究

Bioavailability of cetirizine hydrochloride capsules in healthy subjects

10名健康志愿者随机交叉给药,分别口服20mg国产盐酸西替利嗪胶囊和进口片剂进行药代动力学和相对生物利用度研究。采用高效液相色谱法,测定血浆中盐酸西替利嗪的浓度,经3p97生物利用度和生物等效性计算程序处理拟合,符合二室模型,并得国产胶囊和进口片剂的AUC分别为6842.10±962.24μg·h·L -1和7092.62±829.85μg·h·L -1,Tmax 分别为1.72±0.09h和1.54±0.09h,Cmax分别为954.29±76.88μg·L-1 和933.37±84.17μg·L-1,经配对t检验,两者的AUC,Tmax,Cmax 均无显著性差异(P>0.05)。采用梯形法计算的国产胶囊与进口片剂的AUC0 -t 分别为7077.02±1004.14μg·h·L-1 和7133.59±658.15μg·h·L-1,经方差分析和双单侧检验结果表明两者具有生物等效性。国产盐酸西替利嗪胶囊的相对生物利用度为99.0 %±7.2 %。

The relative bioavailability and pharmacokinetics of domestic cetirizine capsules were studied in 10 healthy male volunteers.A dose of 20 mg of domestic or imported cetirizine(test and reference preparation)was given according to a randomized 2-way cross-over design,blood samples were withdrawn up to 36 hours post administration,and plasma concentration of cetirizine was determined by high performance liquid chromatography(HPLC) method.The concentration-time curves of two preparations fitted to a two-compartment model.The peak plasma levels(Cmax)of cetirizine test drug and reference drug were 954.29±76.88 and 933.37±84.17 μg·L-1 respectively,the peak time (Tmax)were 1.72±0.09 h and 1.54±0.09 h respectively,and AUC0-t were 7077.02±1004.14 and 7133.59±658.15 μg·h·L-1,respectively.The pharmacokinetics and relative bioavailability data obtained in the study furnished definite proof of bioequivalence of both domestic cetirizine capsules and imported cetirizine tablets.