安吡昔康片在健康受试者单次给药的药代动力学

Pharmacokinetics of single dose ampiroxicam tablet in Chinese healthy subjects

目的评价安吡昔康片在中国健康受试者单次给药的药代动力学。方法用随机、开放、单剂量、口服给药、三交叉拉丁方设计的方法,12名受试者随机分为3组,先后单次口服安吡昔康片13.5,27.0,40.5 mg,给药间隔14 d,在不同时间点收集血、尿样本,用HPLC法测定浓度。结果受试者口服安吡昔康片后10名受试者进行了药代动力学统计分析,13.5,27.0,40.5 mg 3个剂量组主要药代动力学参数如下:Cmax分别为(0.90±0.42),(1.55±0.35),(2.17±0.49)mg.L-1;t1/2β分别为(54.03±30.13),(45.65±14.84),(44.01±11.75)h;tmax分别为(7.30±4.47),(12.20±8.80),(11.50±7.59)h;AUC0-t分别为(56.09±20.78),(105.55±29.18),(161.80±46.44)mg.h.L-1。3个剂量组0～192 h原型药物尿中累积排泄百分率分别为(0.01±0.02)%,(0.11±0.14)%,(0.17±0.13)%。结论不同给药剂量的安吡昔康片主要药代动力学参数呈线性分布特性,药物尿液排泄量很少。

Objective To evaluate the pharmacokinetics of single dose of ampiroxicam tablet in Chinese healthy subjects.Methods A randomized,three period cross-over study was conducted.Twelve subjects randomized for administration of a single dose of 13.5,27.0 and 40.5 mg of ampiroxicam tablet.The concentrations of ampiroxicam in serum and urine were determinated by HPLC method.Results The main pharmacokinetics parameters of three doses（13.5 mg,27 mg and 40.5 mg） in ten subjects were as follows：Cmax were（0.90 ± 0.42）,（1.55 ± 0.35） and（2.17 ± 0.49） mg.L-1;t1/2β were（54.03 ± 30.13）,（45.65 ± 14.84） and（44.01 ± 11.75） h;tmax were（7.30 ± 4.47）,（12.20 ± 8.80） and（11.50 ± 7.59） h;AUC0-t were（56.09 ± 20.78）,（105.55 ±29.18） and（161.80 ±46.44） mg.h.L-1,respectively.Urinary recovery rates were（0.01 ± 0.02） %,（0.11 ± 0.14） % and（0.17 ±0.13） %,respectively.Conclusion The main pharmacokinetics parameters of ampiroxicam in different doses were nearly fit linear dynamic feature,and the drug was little excreted through kidney.