天然维生素E对P-糖蛋白活性影响的体内研究  

Effects of regular consumption of RRR-α-tocopherol on the activity of P-gp in vivo

作　　者：张松波[1,2] 段娟 周宏灏[2] 

机构地区：[1]岳阳职业技术学院 [2]中南大学临床药理研究所 [3]湖南省血防所附属医院

出　　处：《中国临床药理学与治疗学》2011年第5期545-548,共4页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的:阐明天然维生素E在体内对P-糖蛋白活性的影响。方法:12名健康志愿者,随机分两组,采用两阶段双周期交叉设计,一组口服天然维生素E 600 mg/d,另一组不服药,连续14 d,在第15天两组均口服他林洛尔100 mg,在0、0.25、0.5、0.75、1、1.5、2、2.5、3、4、6、8、12、24 h采外周静脉血5 mL,洗脱4周交叉进行下阶段实验。采血后0.5 h内进行离心和分离血浆,运用HPLC测定他林洛尔血浆中药物浓度,分析比较不同服药组间药代动力学参数的差异。结果:天然维生素E明显降低了他林洛尔的血药浓度。天然维生素E服用组与对照组之间他林洛尔曲线下面积AUC(0-24 h)分别为(2104±670)和(2914±1061)ng·h·mL-1,P<0.05;峰浓度Cmax分别为(249±69)ng/mL和(406±214)ng/mL,P<0.05。结论:口服天然维生素E 600 mg,连续14 d,明显诱导了P-糖蛋白的活性。AIM： To investigate the effect of regular consumption of RRR-α-tocopherol on the activity of P-gp in vivo. METHODS： In a two-stage doubly periodic cross-over study,12 healthy volunteers,who were randomly divided into two groups,ingested RRR-α-tocopherol 600 mg each day or placebo（control） for 14 d.On day 15,a single 100 mg dose of talinolol was administered by all the volunteers and 5 mL peripheral vein blood of each one was taken at 0,0.25,0.5,0.75,1,1.5,2,2.5,3,4,6,8,12,24 h.Plasma concentrations of talinolol were determined by HPLC after centrifugation and blood plasma separation.The difference of pharmacokinetic parameters of every groups were compared and analyzed.RESULTS：Co-administration of RRR-α-tocopherol obviously decreased the area under the curve AUC（0-24h） of talinolol [（2104±670） ng·h·mL-1 vs（2914±1061） ng·h·mL-1],P〈0.05,and significantly decreased Cmax of talinolol [（249±69） ng/mL vs（406±214） ng/mL],P〈0.05.CONCLUSION： Regular consumption of RRR-α-tocopherol 600 mg each day for 14 d,significantly induces the activity of P-gp.

关 键 词：天然维生素E 他林洛尔 孕烷X受体 P-糖蛋白 

分 类 号：R969.1[医药卫生—药理学]