白藜芦醇影响氨氯地平在健康志愿者体内的药代动力学研究

Effect of resveratrol on the pharmacokinetics of amlodipine in healthy volunteers

目的探讨白藜芦醇对氨氯地平体内药代动力学的影响。方法用自身对照研究,选取13名男性健康志愿者,单剂量口服氨氯地平5 mg,洗脱5 d后,口服白藜芦醇每次1000 mg,qd,连续服药14 d,再口服氨氯地平5 mg。采集不同时间的血样,用超高效液相色谱-串联质谱(UPLC-MS/MS)法检测氨氯地平的血药浓度,并计算药代动力学参数。结果单剂量口服氨氯地平5 mg后,tmax为(10.62±11.44)h,t1/2为(49.81±14.46)h,Cmax为(0.42±0.11)μg·mL-1,AUC0-96 h为(2.23±0.16)ng·mL-1·h。单剂量口服与白藜芦醇达到稳态后氨氯地平的Cmax,AUC0-96 h和AUC0-∞的几何均值比值分别为92.78%,104.96%和104.15%,差异均无统计学意义(均P>0.05)。白藜芦醇给药前后氨氯地平药代动力学参数比值的90%的参考区间均不超过等效范围,两药联合对氨氯地平的代谢无明显影响。结论白藜芦醇对氨氯地平体内药代动力学无明显影响。

Objective To investigate the effect of resveratrol on the pharmacokinetics of amlodipine in vivo.Methods We conducted a self-controlled study in which recruited 13 healthy male volunteers.All the volunteers were given a single dose of amlodipine 5 mg.And after eluting for 5 days, followed by continuously taking resveratrol 1000 mg, qd, for 14 days, they were given amlodipine 5 mg for the second time.Blood samples were collected at different times, and the blood drug concentration of amlodipine was detected by ultra performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS), and the pharmacokinetic parameters were calculated.Results After taking a single dose of amlodipine 5 mg, tmax was(10.62±11.44) h, t1/2 was(49.81±14.46) h, Cmax was(0.42±0.11) μg·mL-1, and AUC0-96 h was(2.23±0.16) ng·mL-1·h.The geometric mean ratios of amlodipine Cmax, AUC0-96 h and AUC0-∞ before and after resveratrol reached steady state were 92.78%, 104.96% and 104.15%(all P>0.05).Conclusion Resveratrol has no significant effect on the pharmacokinetics of amlodipine in vivo.