氟氯西林钠胶囊在中国人体的药动学和生物等效性评价

 目的建立人血浆中氟氯西林浓度的测定方法,进行氟氯西林的人体药动学研究和生物等效性评价。方法20名健康志愿者随机交叉、单剂量po 500mg受试和参比氟氯西林钠胶囊剂,用高效液相色谱法测定血浆中氟氯西林浓度,计算氟氯西林的人体药动学参数,并进行生物等效性评价。结果受试和参比氟氯西林钠胶囊剂的药-时曲线均符合二房室模型,药动学参数为:t_lag(0.1±0.2)和(0.2±0.1)h,t_max(0.8±0.2)和(0.9±0.3)h,ρ_max(34.83±7.90)和(30.53±10.73)mg·L^-1,K_a(4.869±2.135)和(3.682±1.681)h^-1,t^1/2(1.51±0.39)和(1.45±0.36)h,CL/F(9.268±2.165)和(9.876±2.657)L·h^-1,Vd/F(23.58±11.26)和(22.34±12.35)L,AUC_0-8h(69.05±13.26)和(62.22±15.51)mg·h·L^-1,AUC_0-∞(70.55±13.47)和(63.69±15.69)mg·h·L^-1,相对生物利用度为(114.9±25.1)%。结论氟氯西林钠胶囊口服在中国人体中吸收迅速,消除快;两种胶囊剂在人体内生物等效。

Pharmacokinetics and Bioequivalence of Flucloxacillin Capsules in Chinese Healthy Subjects

OBJECTIVE To study the pharmacokinetics and bioequivalence of flucloxacillin capsules in 20 Chinese healthy subjects.METHODS A single oral dose of 500 mg test or reference of flucloxacillin sodium capsules was given to each subject according to an open randomized crossover design.The concentrations of flucloxacillin in plasma were determined by HPLC method.The pharmacokinetic parameters were calculated and the bioequivalence was evaluated.RESULTS The concentration-time curves of flucloxacillin were fitted into a two-compartment model.The pharmacokinetic parameters of test and reference of flucloxacillin sodium capsules were as follows:t_lag(0.1±0.2)and(0.2±0.1)h,t_max(0.8±0.2)and(0.9±0.3)h,ρ_max(34.83±7.90)and(30.53 ±10.73)mg·L^-1,K_a(4.869±2.135)and(3.682±1.681)h^-1,t_1/2(1.51±0.39)and(1.45±0.36)h,CL/F(9.268±2.165)and(9.876±2.657)L·h^-1,Vd/F(23.58±11.26)and(22.34±12.35)L,AUC_{0-8 h}(69.05±13.26)and(62.22±15.51)mg·h·L^-1,AUC_0-∞(70.55±13.47)and(63.69±15.69)mg·h·L^-1.The relative bioavailability of the test formulation was(114.9±25.1)%.CONCLUSION The flucloxacillin sodium capsules had a rapid absorption and elimination profile in Chinese volunteers.The two flucloxacillin formulations were bioequivalent.