【作者】 于洋； 胡玉钦； 侯艳宁； 王金； 赵维； 刘建芳；

【Author】 YU Yang, HU Yu-qin, HOU Yan-ning , WANG Jin, ZHAO Wei, LIU Jian-fang Department of Clinical pharmacology, Bethune International Peace Hospital, Hebei Shijiazhuang 050082, China

【机构】 白求恩国际和平医院临床药理室；

【摘要】 目的研究中国健康受试者口服不同剂量奥美沙坦酯片的药动学。方法 29名健康受试者(男性15名,女性14名) 分性别按体重指数随机分为三组,分别单剂量口服低(20mg)、中(40mg)、高(80mg)三个剂量的奥美沙坦酯片,于不同时间分别从受试者肘静脉取血5 mL,离心分离血浆,采用高效液相色谱-质谱法测定血浆中奥美沙坦酯的活性代谢物——奥美沙坦浓度,采用DAS Ver1．0药动学软件进行房室模型判断并计算药动学参数。结果奥美沙坦的体内经时过程符合有滞后时间的一室模型,低、中、高三个剂量组单剂量口服给药后血浆中奥美沙坦的Tmax分别为(2．7±1．4),(2．6±0．8)和(2．8±0．8)h; Cmax分别为(546．2±138．8),(1049±418．2)和(1521±259．7)μg·L-1:AUC0-∞分别为(4051±784．0),(7659±2028)和(11781±2232) μg·L-1·h;t1／2别为(7．0±0．9),(7．1±1．4)和(7．1±2．0)h。结论健康人单剂量口服奥美沙坦酯片后,体内奥美沙坦的药动学符合有滞后时间的一房室模型,Cmax与AUC与服药剂量呈线性相关。不同性别受试者单剂量口服奥美沙坦酯片后的药动学参数无统计学显著差异,表明男、女性受试者口服奥美沙坦酯片后的体内药动学过程基本相同。更多还原

【Abstract】 OBJECTIVE To investigate the pharmacokinetics of olmesartan in Chinese healthy volunteers. METHODS A single oral dose (20, 40, 80 mg) of olmesartan medoxomil tablet was given 29 healthy volunteers (15 male, 14 female), who were divided into three groups randomly. Plasma samples were collected from elbow vein at certain sampling times. Plasma concentration of olmesartan, the active metabolite of the pre-drug, olmesartan medoxomil, was determined by HPLC-MS method, and the pharmacokinetic parameters were calculated by DAS software. RESULTS The plasma concentration-time curves of olmesartan were fitted to a one-compartment model after a oral olmesartan medoxomil tablet in single dose(20, 40, 80 mg). The main pharmacokinetic parameters of olmesartan were as follows: Tmax were (2.7±1.4), (2.6±0.8) and (2.8±0.8) h: Cmax were (546.2 ± 138.8), (1049±418.2) and (1521±259.7) μg·L-1; AUC0-∞ were (4051 ± 784.0), (7659 ± 2028) and (11781±2232) μg·L-1·h;t1/2 were (7.0±0.9), (7.1 ± 1.4) and (7.1±2.0) h, respectively. CONCLUSION The plasma concentration-time curves of olmesartan were fitted to a one-compartment model in 29 healthy volunteers after a oral olmesartan medoxomil tablet in single dose (20, 40, 80 mg), and the Cmax, AUC were dose dependent. There was no significant difference in the pharmacokinetic parameters between female and male volunteers.更多还原