铝镁匹林片单剂量和多剂量人体药动学研究  

Pharmacokinetics of aspirin after single and multiple doses in healthy subjects

作　　者：田蕾[1] 黄一玲[1] 华潞[1] 成小如[1] 李飞鸥[1] 李一石[1] 

机构地区：[1]中国医学科学院阜外心血管病医院临床药理中心,卫生部心血管药物临床研究重点实验室,北京100037

出　　处：《中国新药杂志》2006年第16期1393-1396,共4页Chinese Journal of New Drugs

基　　金：863国家攻关项目<临床试验关键技术及平台研究>(2002AA2Z341A;2004AA2Z3760)

摘　　要：目的:研究单剂量和多剂量铝镁匹林片(每片含阿司匹林81 mg,甘羟铝11 mg,重质碳酸镁22 mg)的人体药动学特征。方法:27名健康受试者随机等分成81,162和324 mg·d^(-1)三组,每日口服规定剂量的铝镁匹林片,连续7 d。采用HPLC-MS-MS法测定血浆阿司匹林和水杨酸浓度。结果:阿司匹林的T_(max)约30 min,t_(1/2)为17．4～29．8 min;水杨酸的t_(1/2)为3～4 h,T_(max)为30～60 min;各剂量组的C_(max)AUC,T_(max),t_(1/2)和Cl/F在给药后d1和d7均无显著性差异,t_(1/2)和Cl/F在三组间无显著性差异。结论:在本研究剂量范围内,阿司匹林和水杨酸呈线性动力学,连续服药未见体内蓄积。Objective： To evaluate the pharmacokinetic profiles of aluminium, magnesium and aspirin tablets in healthy Chinese subjects. Methods： 27 healthy volunteers were randomly administered with oral doses of aluminium, magnesium and aspirin tablets 81 , 162 or 324 mg for 7 days. The plasma concentrations of aspirin and salicylic acid from the volunteers were determined by HPLC-MS-MS. The pharmacokinetic parameters were calculated by WinNonlin software. Results： The PK parameters of aspirin and salicylic acid were Tmax 30 min versus 30 - 60 min, t1/2 17.4 - 29.8 min versus 3 - 4 h, respectively. No significant difference in C AUC, T t1/2 and CI/F between day 1 and day 7 and in t1/2 and CI/F were found among three dosing groups. Conclusion： The linearity of aspirin and salicylic acid concentrations were shown in the dosing setting （81 -324 mg） and without drug accumulation in vivo in the continuous administration manner.

关 键 词：铝镁匹林 阿司匹林 水杨酸 药动学 高效液相色谱-串联质谱法 

分 类 号：R969.1[医药卫生—药理学] R971.1[医药卫生—药学]