氟氯西林镁颗粒的人体生物等效性研究

Study on Bioequivalence of Flucloxacillin Magnesium Granules in Healthy Volunteers

目的:比较氟氯西林镁颗粒与氟氯西林钠胶囊的人体生物等效性。方法:24名健康受试者随机分为两组,采用双周期自身交叉方法,单剂量口服受试制剂氟氯西林镁颗粒或参比制剂氟氯西林钠胶囊0.5 g。用液-质联用(LC-MS/MS)法测定氟氯西林的血浆浓度,并计算其药动学参数,比较二者的人体生物等效性。结果:受试制剂与参比制剂的药动学参数分别为:t1/2(1.53±0.29)、(1.55±0.25)h,cmax(34.56±8.13)、(34.67±8.89)mg/L,tmax(0.72±0.25)、(0.74±0.25)h,AUC0-24 h(69.51±15.34)、(70.47±16.19)mg·h/L,受试制剂的相对生物利用度为(99.29±10.34)%。结论:氟氯西林镁颗粒与氟氯西林钠胶囊在吸收程度上具有生物等效性。

OBJECTIVE： To study the pharmacokinetics of Flucloxacillin magnesium granules and Flucloxacillin sodium capsules in healthy volunteers. METHODS： 24 subjects were randomized into 2 groups and enrolled in bi-periodic crossover test. They were given test preparation Flucloxacillin magnesium granules or reference preparation Flucloxacillin sodium capsules of 0.5 g. Plasma concentrations of flucloxacillin were determined by LC-MS/MS. The main pharmacokinetic parameters were calculated, and bioequiavailability of them were compared. RESULTS： The main pharmacokinetic parameters of test preparation vs. reference preparation were as follows： t1/2（1.53±0.29）h vs.（1.55±0.25）h; Cmax（34.56 ± 8.13）mg/L vs.（34.67±8.89）mg/L;tmax（0.72±0.25） h vs. （0.74±0.25） h; AUC0-24 h（69.51 ＋ 15.34） mg. b./L vs. （70.47±16.19）mg. h/L. The relative bioavailability of test preparation was （99.29±10.34） %. CONCLUSIONS： The results demonstrate that the two preparations are bioequivalent.