单剂量口服奥美沙坦酯片在中国健康志愿者体内的药代动力学研究  

Pharmacokinetic Study of Olmesartan Medoxomil Tablets on Chinese Healthy Volunteers in Vivo after Single Dose Orally

作　　者：于洋[1] 胡玉钦[1] 刘建芳[1] 侯艳宁[1] 

机构地区：[1]解放军白求恩国际和平医院临床药理室,石家庄050082

出　　处：《解放军医药杂志》2014年第1期67-69,共3页Medical & Pharmaceutical Journal of Chinese People’s Liberation Army

基　　金：国家科技部"十二五重大新药创制"科技重大专项(2011ZXJ09202-12)

摘　　要：目的 研究奥美沙坦酯片单剂量口服给药在中国健康志愿者体内的药代动力学特征.方法 29名健康志愿者完成本次试验,随机分为低剂量组10名、中剂量组10名和高剂量组9名,分别单剂量口服奥美沙坦酯片20、40和80 mg,采用高效液相-质谱法测定不同时间血浆中奥美沙坦浓度,以药代动力学软件DAS Ver 2.0计算药代动力学参数.结果 奥美沙坦在体内过程符合二房室模型.血药浓度峰值和曲线下面积与剂量呈正相关（r=0.80,r=0.87,P〈0.01）,3个剂量组达峰时间、半衰期和平均驻留时间比较差异均无统计学意义（P〉0.05）,高剂量组表观清除率均高于低、中剂量组（P〈0.05）.结论 奥美沙坦酯片20~80 mg单剂量口服给药时在中国健康志愿者体内表现出良好的线性关系,安全性好.Objective To study the pharmacokinetic characteristics of olmesartan medoxomil tablets on Chinese healthy volunteers in vivo after single dose orally. Methods Twenty-nine healthy volunteers were randomly divided into low-dose group （n = 10） , middle-dose group （n = 10） and high-dose group （n = 9） with Olmesartan medoxomil tablets 20, 40 and 80 mg of oral dose for one time respectively. Plasma concentrations of olmesartan at different times were determined with high performance liquid chromatography-mass spectrography （HPLC-MS） method, and the pharmacokinetic parameters were calculated by DAS Ver 2. 0 software. Results The physiological dispositions of olmesartan were fitted in to a two-compartment model in vivo. Plasma drug level peaks and area under curve had a positive correlation with doses （ r = 0. 80 .r = 0. 87 ,P 〈 0. 01 ） , there were no significant differences in peak reach time, half life period and mean residence time among the three groups （P 〉 0.05） , and the aparent clearance of high-dose group was higher than those of low and medium dose groups （P 〈 0. 05）. Conclusion Satisfactory linear pharmacokinetic characteristics can be achieved by Olmesartan medoxomil tablets of 20 - 80 mg single dose orally in vivo of Chinese health volunteers.

关 键 词：奥美沙坦酯片 高效液相色谱 质谱法 血药浓度 药代动力学 

分 类 号：R969.1[医药卫生—药理学] R972.4[医药卫生—药学]