Almeida Ana, Almeida Susana, Filipe Augusto, Gagnon Stéphanie, Mirapeix Aitor, Girard Benoît, Tanguay Mario
Medical Department, Grupo Tecnimede, Prior Velho (Portugal).
Arzneimittelforschung. 2005;55(4):218-22. doi: 10.1055/s-0031-1296848.
This study was conducted in order to assess the bioequivalence of two different coated tablet formulations containing 5 mg finasteride (CAS 98319-26-7). Twenty-six healthy volunteers were enrolled in an open, randomised, crossover single dose study with 2 periods x 2 sequences and a minimum washout period of 7 days. Plasma samples were obtained over 24 h (at baseline, +0.5 h, +1 h, +1.5 h, +2 h, +2.5 h, +3 h, 3.5 h, +4 h, +4.5 h, +5 h, +6 h, +8 h, +10 h, +12 h, +16 h and +24 h after administration). Finasteride levels were determined by high-pressure liquid chromatography with tandem mass detection, HPLC-MS/ MS, (LOQ 0.50 ng/mL). Pharmacokinetic parameters used for bioequivalence assessment (AUClast and Cmax were main evaluation criteria, however, AUCinf was also analysed) were determined from the finasteride concentration data using non-compartmental analysis. The 90 % confidence intervals (obtained by ANOVA) were 86.31-98.69 for Cmax, 95.40-104.88 for AUClast and 96.20-105.81 for AUCinf that is, they were all within the predefined ranges. It may be therefore concluded that the evaluated formulations are bioequivalent in terms of rate and extent of absorption.
本研究旨在评估两种含5mg非那雄胺（CAS 98319-26-7）的不同包衣片剂制剂的生物等效性。26名健康志愿者参加了一项开放、随机、交叉单剂量研究，该研究有2个周期×2个序列，最短洗脱期为7天。在24小时内（给药后基线、+0.5小时、+1小时、+1.5小时、+2小时、+2.5小时、+3小时、3.5小时、+4小时、+4.5小时、+5小时、+6小时、+8小时、+10小时、+12小时、+16小时和+24小时）采集血浆样本。非那雄胺水平通过高压液相色谱-串联质谱检测法（HPLC-MS/MS）测定（定量下限为0.50ng/mL）。用于生物等效性评估的药代动力学参数（AUC末次和Cmax是主要评估标准，但也分析了AUC无穷大）通过非房室分析从非那雄胺浓度数据中确定。通过方差分析获得的90%置信区间，Cmax为86.31-98.69，AUC末次为95.40-104.88，AUC无穷大为96.20-105.81，也就是说，它们均在预定义范围内。因此可以得出结论，所评估的制剂在吸收速率和程度方面具有生物等效性。
