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目的评价香港Christo公司生产与进口阿替洛尔片的药动学特征和相对生物利用度。方法 18名男性健康受试者按照3×3交叉设计单剂量口服(100mg)阿替洛尔试验制剂A、B及参比制剂R后,用RP-HPLC-FLD检测不同时间点阿替洛尔的血药浓度。借助DAS软件进行药物动力学基本参数的计算与统计分析。结果受试制剂A、B及参比制剂R主要药物动力学参数如下:Cmax分别为(376.7±122.3)、(389.9±115.5)和(398.0±118.0)ng.mL-1;tmax分别为(2.8±0.8)、(2.8±1.0)和(2.7±0.7)h;AUC0→24分别为(3 193.3±993.5)、(3 069.0±915.7)和(3 218.6±994.9)ng.h.mL-1。AUC0→∞分别为(3 530.9±1 119.2)、(3 333.1±1 047.7)和(3 545.5±1 260.3)ng.h.mL-1。试验制剂A、B对参比制剂R的相对生物利用度分别为(101±19)%和(97±14)%。结论 2种阿替洛尔受试制剂与参比制剂相比均具有生物等效性。
Objective To evaluate the pharmacokinetics and relative bioavailability of atenolol tablets produced and imported by Hong Kong Christo Company. Methods A total of 18 male healthy subjects were randomized into three groups according to a single oral dose (3 × 3) of atenolol (100 mg) for atenolol to test preparations A, B and reference formulation R. RP-HPLC-FLD was used to detect atenolol Blood concentration. Calculate and analyze the basic parameters of pharmacokinetics with DAS software. Results The main pharmacokinetic parameters of test preparation A, B and reference preparation R were as follows: Cmax were (376.7 ± 122.3), (389.9 ± 115.5) and (398.0 ± 118.0) ng.mL-1, respectively; ± 0.8, 2.8 ± 1.0 and 2.7 ± 0.7 h, respectively; AUC0 → 24 were (3 193.3 ± 993.5), (3 069 ± 915.7) and (3 218.6 ± 994.9) ng.h.mL-1, respectively. AUC0 → ∞ were (3 530.9 ± 1 119.2), (3 333.1 ± 1 047.7) and (3 545.5 ± 1 260.3) ng.h.mL-1, respectively. The relative bioavailabilities of Test Formulations A, B to Reference Formulation R were (101 ± 19)% and (97 ± 14)%, respectively. Conclusions The two atenolol test preparations are bioequivalent compared with the reference preparations.