高脂饮食对非洛地平在中国健康受试者体内药动学的影响

目的研究高脂饮食对非洛地平在健康中国人体内的药动学影响。方法 10名健康男性受试者随机分成2组,分别于空腹或进食高脂餐后口服非洛地平缓释片1片(10 mg/片),采用液相色谱-串联质谱(LC-MS/MS)法测定血浆中非洛地平的浓度,用DAS 2.1.1软件计算主要药动学参数,用SPSS 19.0软件对主要药动学参数进行统计学分析。结果受试者于空腹和进食高脂餐后口服非洛地平缓释片的主要药动学参数ρmax、tmax、AUC0-36 h分别为(5.78±3.22)μg·L-1和(9.29±3.47)μg·L-1、(3.11±1.27)h和(5.33±1.80)h、(46.6±24.2)μg·h·L-1和(58.7±18.6)μg·h·L-1;对空腹与进食高脂餐后给药的主要药动学参数采用配对t检验进行统计分析,ρmax和tmax具有显著性差异(P<0.05)。结论高脂饮食可显著降低非洛地平的吸收速度,并显著提高峰浓度。

Effect of high-fat meal on the pharmacokinetics of felodipine in healthy Chinese volunteers

Objective To investigate the effect of high-fat food on the pharmacokinetics of felodipine in healthy Chinese volunteers after single oral dose of felodipine tablet. Methods 10 healthy volunteers w ere randomly divided into 2 groups w ith each group of 5 persons. One group received felodipine extended released tablet( 10 mg per tablet) after fasting 10 hours. Another group received felodipine extended released tablet( 10 mg per tablet) after taking high-fat meal. The concentrations of felodipine in plasma w ere determined by LC-MS / MS. The main pharmacokinetic parameters w ere calculated w ith DAS 2. 1. 1 softw are. The statistical analysis w as carried w ith SPSS 19. 0 softw are. Results Under the condition of high-fat meal vs fasting,the main pharmacokinetic parameters of felodipine w ere as follow s: ρmax( 5. 78 ± 3. 22) μg·L-1vs( 9. 29 ±3. 47); t1 /2( 11. 53 ± 5. 29) h vs( 8. 56 ± 3. 57) h; tmax( 3. 11 ± 1. 27) h vs( 5. 33 ± 1. 80) h; AUC0-36 h( 46. 6 ±24. 2) μg·h·L-1vs( 58. 7 ± 18. 6) μg·h·L-1,respectively. Paired t-test was applied for the determination of statistical difference in pharmacokinetic parameters betw een fasting and high-fat meal groups. Significant differences betw een the tw o groups for ρmaxand tmaxw ere observed. Conclusions High-fat meal could significantly decrease the absorption rate but increase the peak plasma concentration of felodipine.