CAJ | 학술논문

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(20、40、80 mg)后体内血浆最大浓度(Cmax)分别为(1016±349)、(1503±266)、(2516±1196) ng/ml；消除半衰期(t1/2)为(5.2±1.2)、(5.6±1.6)、(6.2±0.9)h；多次服用奥美沙坦20 mg后Cmax和t1/2分别为(894±301)ng/ml、(6.4±1.2) h,单次给药和多次给药间t1/2差异无统计学意义。单剂量试验中,当服药剂量在20~80 mg范围,AUC0-肄、AUC0-48、Cmax等PK参数与药物剂量呈线性关系。结论奥美沙坦酯20 mg,1 d/次的给药方案在体内不会造成蓄积作用。
목적：분석중국건강수시자단제량혹다차구복오미사탄지후체내약대동역학적특정。방법단제량실험：12명사선합격적수시자,채용개방、수궤、단제량、삼주기、3×3랍정방설계방법장시험분위3조,매조4명,매주기분별복용상대응제량적약물,차매주기복약전경과7 d적세탈기。다차급약시험：12명건강수시자매천복용20 mg오미사탄지,련속4 d。채집복약전0 h급복약후48 h내적혈양,분석체내약물각PK삼수。결과단제량복용오미사탄(20、40、80 mg)후체내혈장최대농도(Cmax)분별위(1016±349)、(1503±266)、(2516±1196) ng/ml；소제반쇠기(t1/2)위(5.2±1.2)、(5.6±1.6)、(6.2±0.9)h；다차복용오미사탄20 mg후Cmax화t1/2분별위(894±301)ng/ml、(6.4±1.2) h,단차급약화다차급약간t1/2차이무통계학의의。단제량시험중,당복약제량재20~80 mg범위,AUC0-이、AUC0-48、Cmax등PK삼수여약물제량정선성관계。결론오미사탄지20 mg,1 d/차적급약방안재체내불회조성축적작용。
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,contin-uous 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,sin-gle 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. Con-clusion Olmesartan medoxomil has no accumulation in healthy Chinese subjects after 20 mg multiple-dose.