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 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：t_max（1.08±0.44）和（1.35±0.76）h，C_max（5.40±0.60）和（5.37±0.72）μg·ml^-1，t_1/2(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，MRT（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。

Pharmacokinetics and Bioequivalence of Fluconazole Tablets in Healthy Volunteers

Objective： To study the relative bioavailability and bioequivalenee 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 ehromatog- raphy-UV, and the pharmacokinetic parameters and bioequivaience of the tablets were analyzed through DAS 2.0 software. Result： The pharmacokinetic parameters of the test and reference tablets in plasma were as follows： tmax of（ 1.08 ± 0.44）and （1.35 ± 0.76）h, Cmax of（5.40 ±0.60）and（5.37 ±0.72）μg ·h ·ml^-1,t1/2 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,AUC〈0-∞ of （204.0 ±17.5） and（202.4±18.1）μg ·h ·ml^-1,MRTof（34.7±1.7）and（34.0±l.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.