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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 study the effects of high-fat and high-calorie diet on the pharmacokinetics of oral atorvastatin calcium capsules in Chinese healthy volunteers. Methods Twenty-four healthy volunteers were randomly divided into two groups. Randomized, crossover and self-controlled design were used. Two groups were given orally 20 mg atorvastatin calcium capsules after fasting and eating high-fat and high-calorie food for two different test periods . The blood samples were collected before administration and at different time points after administration. The concentrations of atorvastatin in plasma were determined by HPLC-MS / MS, and the corresponding pharmacokinetic parameters were calculated. The fasting and eating Differences of pharmacokinetic parameters after administration of high fat and hot food. Results The main pharmacokinetic parameters of 24 mg orally taken 20 mg atorvastatin capsules in 24 subjects were (4.71 ± 2.36) ng · mL-1, (12.35 ± 6.85) ng · mL -1 and tmax were (2.49 ± 2.06) h and (0.49 ± 0.24) h, respectively; t 1/2 was (13.85 ± 4.23) h and (15.84 ± 12.48) h respectively; AUC0-t was (47.74 ± 18.23) ng · ML-1, (51.50 ± 17.58) ng · mL-1. Conclusion High-fat and high-calorie foods have a great effect on the absorption rate of atorvastatin, but have little effect on the elimination rate and the degree of absorption.