单次及多次口服奥美沙坦酯在中国健康受试者体内药代动力学的研究.docVIP

单次及多次口服奥美沙坦酯在中国健康受试者体内药代动力学的研究 　　[摘要] 目的 分析中国健康受试者单剂量或多次口服奥美沙坦酯后体内药代动力学的特征。 方法 单剂量实验：12名筛选合格的受试者，采用开放、随机、单剂量、三周期、3×3拉丁方设计方法将试验分为3组，每组4名，每周期分别服用相对应剂量的药物，且每周期服药前经过7 d的洗脱期。多次给药试验：12名健康受试者每天服用20 mg奥美沙坦酯，连续4 d。采集服药前0 h及服药后48 h内的血样，分析体内药物各PK参数。 结果 单剂量服用奥美沙坦 　　[关键词] 奥美沙坦酯；药代动力学；中国人 　　[中图分类号] R969.1 [文献标识码] A [文章编号] 1674-4721（2014）08（a）-0013-04 　　Pharmacokinetic study of olmesartan medoxomil in healthy Chinese subjects after single and multiple administrations 　　LI Kun-yan QIU Yu JIANG Yun LUO Cheng-hui YANG Nong LIN Xiao-ping ZHOU Chun-hua WANG Jing 　　GCP Center，Hunan Cancer Hospital；the Affiliated Cancer Hospital of Xiangya School of Medicine，Central South University，Changsha 410006，China 　　[Abstract] Objective To investigate pharmacokinetic characters of olmesartan medoxomil in healthy Chinese subjects after single and multiple administrations. Methods A single dose experiment：12 screening qualified subjects，the test wass divided into three groups by randomized-sequence，single-dose，3-treatment，3-period crossover design，each group of 4 peoples，each cycle respectively corresponding to the dose of drugs，and each cycle after 7 d washout period before taking the medicine.Multiple dosing test：12 healthy subjects were given 20 mg olmesartan medoxomil every day，continuous 4 d.Collected 0 h before taking the medicine and medication after blood analysis within 48 h of drugs in vivo PK parameters. Results Single dose olmesartan medoxomil （20，40，80 mg） after the maximum concentration in plasma （Cmax） were respectively （1016±349），（1503±266），（2516±1196） ng/ml，1/2 level elimination half-life （t1/2） for （5.2±1.2），（5.6±1.6），（6.2±0.9） h，after multiple dose olmesartan medoxomil，the Cmax and t1/2 was （894±301） ng/ml，（6.4±1.2） h respectively，single dose and t1/2 level differences between multiple dosing has no statistical significance.A single dose experiment，when within 20 to 80 mg dose，AUC0-∞，AUC0-48 and Cmax PK parameters with a linear relationship between dose of drug. Conclusion