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用HPLC法研究10名健康男性受试者单剂量口服500mg氟他胺胶囊和片后,血浆中羟基氟他胺浓度及其药代动力学指标。并以片剂为参比制剂,对胶囊的生物利用度及其生物等效性进行评价。结果显示受试者服药后,血浆中原型药物浓度低,且变异性大,并快速转化为羟基代谢物。测得的胶囊T_(max)2.7h,C_(max)2.22μg·ml~(-1),片剂的T_(max)3.3h,C_(max)2.00μg·ml~(-1)。两制剂的t1/2约为5.7h。AUC~(24)分别为20.93±4.01和19.43±5.35μg·ml~1。相对生物利用度为110.22±14.82％。经方差分析和双向单侧t检验显示两种剂型的AUC~(24)和AUC生物等效。
The plasma concentrations of hydroxyflutamide and its pharmacokinetic parameters in 10 healthy male volunteers after oral administration of 500 mg flutamide capsules and tablets were studied by HPLC. The bioavailability and bioequivalence of the capsules were evaluated using the tablet as reference preparation. The results showed that after taking the drug, the plasma concentration of the prototype drug is low, and the variability is large, and quickly converted to hydroxy metabolites. The measured capsule T max 2.7h, C max 2.22μg · ml -1, tablet T max 3.3h, C max 2.00μg · ml -1. The t1 / 2 of both formulations was approximately 5.7 h. AUC ~ (24) were 20.93 ± 4.01 and 19.43 ± 5.35μg · ml ~ 1, respectively. The relative bioavailability was 110.22 ± 14.82%. ANOVA and two-way one-sided t-test showed that the AUC 24 and AUC of the two formulations were bioequivalent.