单剂量与多剂量口服复方奥美沙坦酯片的药动学研究

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目的:研究健康受试者口服复方奥美沙坦酯片后的药动学。方法:采用高效液相色谱法测定单剂量与多剂量口服复方奥美沙坦酯片后氢氯噻嗪与奥美沙坦的血药浓度,并利用DAS药动学软件计算药动学参数。结果:单剂量给药后氢氯噻嗪与奥美沙坦的主要药动学参数分别为:t1/2(9.7±3.4)、(6.3±2.0)h,Cmax(69.7±19.8)、(635.1±237.7)μg.L-1,AUC0~48(737.8±110.6)、(4 438.4±1 058.1)μg.h.L-1,AUC0~∞(760.4±128.2)、(4 467.0±1 115.6)μg.h.L-1;多剂量给药后氢氯噻嗪与奥美沙坦的主要药动学参数分别为:t1/2(11.4±2.8)、(5.8±2.0)h,Cmax(82.3±26.4)、(694.3±251.2)μg.L-1,AUC0~48(753.2±147.4)、(4 701.3±1 196.6)μg.h.L-1,AUC0~∞(789.3±172.2)、(4 735.0±1 235.1)μg.h.L-1。结论:复方奥美沙坦酯片2组分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,连续给药后药物在体内蓄积不明显。 Objective: To study the pharmacokinetics of omeprazartan ester tablets in healthy volunteers. Methods: The plasma concentrations of hydrochlorothiazide and olmesartan were determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters were calculated by DAS pharmacokinetic software. RESULTS: The main pharmacokinetic parameters of hydrochlorothiazide and olmesartan after single-dose administration were t1 / 2 (9.7 ± 3.4), (6.3 ± 2.0) h, Cmax (69.7 ± 19.8), (635.1 ± 237.7) μg .AUC0 ~ ∞ (760.4 ± 128.2), (4 467.0 ± 1 115.6) μg.hL-1, AUC0 ~ 48 (737.8 ± 110.6), (4 438.4 ± 1 058.1) μg.hL- The main pharmacokinetic parameters of hydrochlorothiazide and olmesartan after dosing were t1 / 2 (11.4 ± 2.8), (5.8 ± 2.0) h, Cmax (82.3 ± 26.4), (694.3 ± 251.2) μg.L- 1, AUC0 ~ 48 (753.2 ± 147.4), (4 701.3 ± 1 196.6) μg.hL-1, AUC0 ~ ∞ (789.3 ± 172.2), (4735.0 ± 1 235.1) μg.hL-1. CONCLUSION: The absorption rate and elimination rate of the two components of olmesartan is not changed with continuous administration. The drug accumulation in the body is not obvious after continuous administration.
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