尼美舒利颗粒在中国健康人体的生物等效性

目的评价2种国产尼美舒利颗粒在中国健康人体的生物等效性。方法20名健康男性受试者随机交叉单剂量口服试验药物或对照药物,各100 mg。用高效液相色谱法测定血浆中尼美舒利浓度;用DAS 2.1软件计算主要药代动力学参数,并对2种药物进行生物等效性评价。结果试验药物和对照药物的主要药代动力学参数:Cmax分别为(6.67±1.80)和(6.50±1.72)μg.mL-1;Tmax分别为(1.88±0.81)和(2.25±0.66)h;t1/2分别为(2.99±0.72)和(2.70±0.58)h;AUC0-24分别为(33.67±12.16)和(33.93±12.99)μg.h.mL-1。AUC0-24、AUC0-∞、Cmax的90%可信区间分别为86.2%～116.3%,86.6%～116.7%和86.8%～120.7%。试验药物相对于对照药物的生物利用度F为(106.9±40.2)%。结论试验药物和对照药物生物等效。

Bioequivalence of nimesulide granules in Chinese healthy volunteers

Objective To evaluate the bioequivalence of two kinds of domestic nimesulide granules in healthy volunteers.Methods In self-control and two-way crossover design,20 healthy male volunteers were divided into two groups at random.Each subject was given 100 mg of the test tablet and reference tablet of nimesulide granules respectively at single dose.The concentrations of nimesulide in plasma were determined by HPLC.The pharmacokinetic parameters were calculated and compared statistically to evaluate the bioequivalence between the two kinds granules by DAS 2.1 software.Results The main pharmacokinetic parameters of test and reference preparation were as follows: Cmax were(6.67±1.80),(6.50±1.72) μg·mL-1;Tmax were(1.88±0.81),(2.25±0.66) h;t1/2 were(2.99±0.72),(2.70±0.58) h;AUC0-24 were(33.67±12.16),(33.93±12.99) μg·h·mL-1,respectively.The 90% confidential interval of AUC0-24、AUC0-∞ and Cmax of tested formulation were 86.2%-116.3%,86.6%-116.7% and 86.8%-120.7%,respectively.The relative bioavailability was(106.9±40.2)%.Conclusion The results demonstrated that the two preparations of nimesulide granules were bioequivalent.