氟氯西林镁颗粒的人体生物等效性研究

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。

Study on Bioequivalence of Flucloxacillin Magnesium Granules in Healthy Volunteers

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.