氟康唑片在健康人体的药物动力学和生物等效性研究

摘要

Objective: To study the relative bioavailability and bioequivalence of fluconazole tablets in healthy volunteers. Method : Twenty healthy male volunteers were involved in a double periodic self-cross randomized trial with a single dose of 200 mg of test and reference tablets. The fluconazole concentrations in plasma were determined by reversed-phase high-performance liquid chromatog-raphy-UV, and the pharmacokinetic parameters and bioequivalence of the tablets were analyzed through DAS 2.0 software. Resu The pharmacokinetic parameters of the test and reference tablets in plasma were as follows; tmas of(1. 08 ±0.44) and( 1. 35 ± 0. 76) h, C?*of(5.40±0.60)and(5.37±0.72)μg ·ml-1 ,ti/2 of (29.1 ±3.4) and (29.0 ±3.5)h,AUC(0_t) of(191. 3 ± 13. 8)and (190.4 ±15.7) μg ·h ·ml-1,A[/C(ll..) of (204.0±17.5) and(202.4 ± 18.1) μg -h -ml"1 ,MRT of(34.7 ± 1.7)and(34.0 ± 1.9)h, respectively. The relative bioavailability of the test preparation was 100.9% ±6.8%. Conclusion; The test tablets are bioequivalent to the reference tablets in the clinical research.%目的:研究氟康唑片在健康人体的药物动力学并评价其生物等效性.方法:采用双周期自身随机交叉试验设计.20名健康男性志愿者分别单剂量口服受试制剂和参比制剂200 mg,以非那西丁为内标,采用HPLC法测定血药浓度.用DAS软件计算药动学参数和进行统计分析.结果:单次口服受试制剂和参比制剂200 mg后的主要药动学参数:tmax(1.08±0.44)和(1.35±0.76)h,Cmax (5.40±0.60)和(5.37±0.72) μg ·ml-1,t1/2 (29.1±3.4)和(29.0±3.5)h,AUC(0-t)(191.3±13.8)和( 190.4±15.7) μg·h·ml-1,AUC(0-∞)(204.0±17.5)和(202.4±18.1)μg·h·ml-1,M RT( 34.7±1.7)和(34.0±1.9)h,以AUC(0-t)计算,受试制剂的相对生物利用度为100.9％±6.8％.结论:两种氟康唑片剂具有生物等效性.