氟康唑在健康人体的药代动力学及生物等效性

Pharmacokinetics and bioequivalence of fluconazol in healthy volunteers

目的评价单剂量口服3种氟康唑制剂(抗真菌药)在健康受试者体内的生物等效性。方法采用三交叉全排列组合设计,18名健康男性受试者随机分为3组,自身交叉口服单剂量试验制剂氟康唑片、氟康唑胶囊和参比氟康唑胶囊600mg,采用液制联用法测定人血浆中氟康唑浓度。结果由DASS2.0软件计算的主要药代动力学参数:Cmax分别为(9.3±1.5)、(9.5±1.4)、(8.9±1.6)μg·mL-1;tmax分别为(1.9±0.7)、(1.9±0.6)、(2.0±0.7)h;t1/2分别为(32.4±6.1)、(34.5±5.8)、(32.6±6.4)h;AUC0-t分别为(358.7±75.0)、(359.5±76.1)、(346.0±78.4)μg.h·mL-1;AUC0-∞分别为(415.3±81.6)、(419.5±82.4)、(401.6±80.6)μg·h·mL-1。结论2种氟康唑受试制剂与参比制剂具有相同的生物效应。

Objective To evaluate the bioequivalence in 18 healthy volunteers after a single oral dose of three kinds of fluconazol preparations. Methods Eighteen healthy human volunteers were divided randomly into three groups, and 600 mg reference and test fluconazol preparations were given to them in a 3 - way cross - over study. Plasma concentrations were determined by LC/MS method. Results The main pharmarcokinetic parameters calculated by DASS2.0 software were as follows： Cmax were （9.3±1.5）,（9.5±1.4） and （8.9 ±1.6）μg·mL;^-1 tmax were （1.9±0.7）,（1.9±0.6） and （2.0±0.7）h; t1/2 were （32.4±6. 1）, （34.5±5.8） and （32.6±6.4）h; AUC0-t were （358.7±75.0）, （359.5±76. 1） and （346.0±78.4）μg·h·mL^-1;AUC0-∞ were （415.3±81.6）, （419.5±＋82.4） and （401.6±80.6）μg·h·mL^-1 respectively by using trapezoid method. Conclusion The results shown that the 3 preparations are bioeqivalent.