高脂高热量饮食对中国健康受试者口服阿托伐他汀药代动力学的影响  

Effect of High-Fat and High-Calorie Diets on Pharmacokinetics of Atorvastatin in Chinese Healthy Subjects

作　　者：刘名义[1] 夏春华[1] 靳高凤 陈亚军[1] 陈琳[1] 高瑞[1] 张红[1] 刘大仁[2] 熊玉卿[1] 

机构地区：[1]南昌大学临床药理研究所江西省临床药物代谢动力学重点实验室,南昌330006 [2]南昌大学期刊社,南昌330006

出　　处：《南昌大学学报（医学版）》2015年第5期14-18,共5页Journal of Nanchang University：Medical Sciences

基　　金：国家自然科学基金(81260508);赣鄱英才555工程人选计划

摘　　要：目的研究高脂高热量饮食对中国健康受试者口服阿托伐他汀钙胶囊药代动力学的影响。方法采用随机、交叉、自身对照设计方法,将24名健康受试者随机分成2组,分别在两个不同试验周期空腹和进食高脂高热量食物30min后口服20 mg的阿托伐他汀钙胶囊。受试者在给药前和给药后不同时间点采集血样,用建立的HPLC-MS/MS方法测定血浆中阿托伐他汀的浓度,计算相应的药代动力学参数,比较分析空腹和进食高脂高热食物给药后药动学参数的差异。结果 24名受试者在进食和空腹状态下口服阿托伐他汀钙胶囊20mg的主要药代动力学参数:Cmax分别为(4.71±2.36)ng·mL-1、(12.35±6.85)ng·mL-1;tmax分别为(2.49±2.06)h、(0.49±0.24)h;t1/2分别为(13.85±4.23)h、(15.84±12.48)h;AUC0-t分别为(47.74±18.23)ng·mL-1、(51.50±17.58)ng·mL-1。结论进食高脂高热量食物对阿托伐他汀吸收速度影响较大,而对消除速度和吸收程度影响较小。Objective To investigate the effect of high-fat and high-calorie diets on pharmaco-kinetics of atorvastatin in Chinese healthy subjects.Methods Twenty-four healthy subjects were selected using a randomized,self-controlled and two-period crossover design.These subjects were orally given 20 mg atorvastatin calcium capsules in fasted state and fed state,respectively.Blood samples were collected before and after administration,and plasma concentrations of atorvastatin were determined by HPLC-MS/MS.The pharmacokinetic parameters were calculated and com-pared between the two states.Results The C max ,t max ,t 1/2 and AUC0-t were,respectively,（4.71± 2.36）ng·mL-1 ,（2.49±2.06）h,（13.85±4.23）h and（47.74±18.23）ng·mL-1 in subjects tak-ing atorvastatin calcium capsules in fed state,and（12.35 ± 6.85）ng· mL-1 ,（0.49 ± 0.24）h, （15.84±12.48）h and（51.50±17.58）ng·mL-1 in subjects taking atorvastatin calcium capsules in fasted state.Conclusion High-fat and high-calorie diets exert a greater influence on absorption＆amp;nbsp;rate of atorvastatin,but have less influence on elimination rate and absorption degree of atorvasta-tin.

关 键 词：阿托伐他汀 药代动力学 高脂高热量饮食 

分 类 号：R969.1[医药卫生—药理学] R972.6[医药卫生—药学]