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目的研究健康受试者单剂量与多剂量口服复方苯磺酸氨氯地平/盐酸贝那普利片后的药动学。方法LC-MS/MS测定单剂量与多剂量给药后氨氯地平与贝那普利及贝那普利拉血药浓度并利用DAS软件计算药动学参数。结果单剂量给药氨氯地平与贝那普利及贝那普利拉的主要药动学参数分别是:t1/2为(47.3±10.6),(1.3±0.4)和(4.5±0.6)h,Cmax为(6.4±1.5),(136.5±40.2)和(158.3±46.7)μg·L-1,AUC0-t为(267.7±88.4),(144.3±46.7)和(891.4±265.4)μg·h·L-1;多剂量给药氨氯地平与贝那普利的主要药动学参数分别是:t1/2为(45.1±8.7),(1.4±0.4)和(5.3±0.8)h,Cmax为(8.2±1.8),(142.4±47.5)和(165.2±40.8)μg·L-1,AUC0-t为(413.5±102.4),(155.7±52.8)和(915.7±316.9)μg·h·L-1,R为(1.6±0.6)、(1.0±0.1)和(1.2±0.1)。结论复方苯磺酸氨氯地平/盐酸贝那普利片2组分及活性代谢产物在健康受试者体内的吸收速率和消除速度不随连续给药变化,但连续给药后苯磺酸氨氯地平在体内有轻微蓄积。
Objective To study the pharmacokinetics of single-dose and multiple-dose oral compound amilodipine besylate / benazepril hydrochloride tablets in healthy subjects. Methods LC-MS / MS was used to determine plasma concentrations of amlodipine and benazepril and benazepril following single and multi-dose administration and pharmacokinetic parameters were calculated using DAS software. Results The main pharmacokinetic parameters of amlodipine, benazepril and benazeprilat were (47.3 ± 10.6), (1.3 ± 0.4) and (4.5 ± 0.6) h Cmax were (6.4 ± 1.5), (136.5 ± 40.2) and (158.3 ± 46.7) μg · L-1, respectively. The AUC0-t was (267.7 ± 88.4), (144.3 ± 46.7) and (891.4 ± 265.4) μg · h · L-1; The main pharmacokinetic parameters of amlodipine and benazepril for multidose administration were: t1 / 2 (45.1 ± 8.7), (1.4 ± 0.4) and (5.3 ± 0.8) AUC0-t was (413.5 ± 102.4), (155.7 ± 52.8) and (915.7 ± 316.9) μg · h · L-1 for the patients with (8.2 ± 1.8), (142.4 ± 47.5) and (165.2 ± 40.8) -1, R was (1.6 ± 0.6), (1.0 ± 0.1) and (1.2 ± 0.1). Conclusion Amlodipine besylate / benazepril hydrochloride tablets 2 components and active metabolites absorption rate and elimination rate in healthy subjects do not change with continuous administration, but after continuous administration of ammonia chloride benzene sulfonate The earth has a slight accumulation in the body.