洛索洛芬钠片在健康志愿者体内的生物等效性

Bioequivalence of loxoprofen tablet in healthy volunteers

目的 研究洛索洛芬钠片的人体生物等效性。方法 健康志愿者2 0名,用随机双交叉试验方法,单剂量(6 0mg)口服洛索洛芬钠的试验或参比制剂,洗净期为2wk ;分别于服药后10h内不同时间点抽取静脉血。用HPLC法测定血浆中洛索洛芬浓度。用3P97程序进行生物等效性评价。结果 单剂口服试验或参比制剂的cmax分别为(3.6 72±1.0 4 1)、(3.35 4±0 .6 93)mg·L-1;tmax分别为(0 .6 6 7±0 .16 7)、(0 .75 0±0 .183)h ;T1/2 分别为(1.4 4 3±0 .2 0 4 )、(1.5 82±0 .30 5 )h ;AUC0→10 分别为(8.5 15±1.84 5 )、(8.0 2 4±1.36 9)mg·h·L-1;AUC0→∞分别为(8.6 19±1.85 1)、(8.14 9±1.4 4 0 )mg·h·L-1。AUC0→∞、AUC0→10 、cmax的90 %置信区间分别为93.3%～115 .8%、99.2 %～114 .8%、10 2 .4 %～12 3.3% ;相对生物利用度为(10 6 .5±16 .9) %。

AIM To study the bioequivalence of loxoprofen sodium tablet. METHODS A single oral dose of loxoprofen sodium tablet (60 mg of test or reference formulation) were given to 20 healthy volunteers in a randomized crossover study. The concentrations of loxoprofen in plasma were determined by HPLC. The pharmacokinetic parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by 3P97 program. RESULTS After a single dose, the pharmacokinetic parameters for loxoprofen were as follows:c max were (3.672±1.041) and (3.354±0.693)mg·L -1;t max were (0.667±0.167) and (0.750±0.183)h; T 1/2 were (1.443±0.204) and (1.582±0.305)h; AUC 0→10 were (8.515±1.845) and (8.024±1.369)mg·h·L -1; AUC 0→∞ were (8.619±1.851) and (8.149±1.440)mg·h·L -1 for test and reference formulation respectively. The 90% confidential interval of AUC 0→∞,AUC 0→10 and c max were 93.3%-115.8%,99.2%-114.8%,102.4%-123.3% respectively. The relative bioavailability was (106.5±16.9)%. CONCLUSION The test and reference formulation are bioequivalent.