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研究阿替洛尔硝苯地平复方缓释片在家犬体内单剂量和多剂量口服给药的药物动力学。6只家犬随机交叉试验,以阿替洛尔片和硝苯地平缓释胶囊为参比制剂,用液相色谱-质谱法测定单剂量与多剂量口服参比与受试制剂的经时过程血药浓度。单剂量试验中,阿替洛尔的参比制剂和受试制剂t1/2为(7.26±1.09)和(7.48±1.02)h,AUC0-t为(5 737±423)和(5 957±430)ng.ml-1.h,受试制剂中阿替洛尔的相对生物利用度为(102.55±2.55)%;硝苯地平的参比制剂和受试制剂t1/2为(7.53±0.27)和(7.33±0.29)h,AUC0-t为(37.92±2.59)和(36.58±1.99)ng.ml-1.h。受试制剂中硝苯地平的相对生物利用度为(95.77±5.65)%。多剂量试验中,阿替洛尔的参比制剂和受试制剂的稳态血药浓度css为(296±18.1)和(306±17.7)ng.ml-1;硝苯地平的参比制剂和受试制剂的稳态血药浓度css为(1.89±0.14)和(1.87±0.18)ng.ml-1。
To study the pharmacokinetics of atenolol nifedipine compound sustained-release tablets in oral and multi-dose oral administration in dogs. Six dogs were randomized to cross-over test. Atenolol tablets and nifedipine sustained-release capsules were used as reference preparations. The single-dose and multi-dose oral reference preparations and the time-course of the test preparations were determined by liquid chromatography-mass spectrometry Blood concentration. In the single-dose trial, t1 / 2 for atenolol reference formulation and test formulation were (7.26 ± 1.09) and (7.48 ± 1.02) h, AUC0-t was (5737 ± 423) and ) ng.ml-1.h, the relative bioavailability of atenolol in the test preparations was (102.55 ± 2.55)%; the reference preparation of nifedipine and the test preparation t1 / 2 were (7.53 ± 0.27) And (7.33 ± 0.29) h, AUC0-t was (37.92 ± 2.59) and (36.58 ± 1.99) ng.ml-1.h. The relative bioavailability of nifedipine in the test preparation was (95.77 ± 5.65)%. In the multi-dose trial, steady-state plasma concentrations cot of atenolol’s reference formulation and the test formulation were (296 ± 18.1) and (306 ± 17.7) ng.ml-1; nifedipine’s reference formulation and The steady-state plasma concentrations css of the test preparations were (1.89 ± 0.14) and (1.87 ± 0.18) ng.ml-1.