五酯胶囊对他克莫司药代动力学的影响  

Effect of Wuzhi capsules on pharmacokinetics of tacrolimus

作　　者：米丽[1] 位华[2] 李敬超 秦士新[4] 茅建辉 

机构地区：[1]武警上海总队医院药剂科,201103 [2]第二军医大学长征医院药剂科,上海200041 [3]武警海南总队医院医务处,海口570203 [4]武警上海总队医院医务处,201103

出　　处：《武警医学》2016年第3期240-242,共3页Medical Journal of the Chinese People's Armed Police Force

摘　　要：目的观察不同剂量五酯胶囊对他克莫司药代动力学的影响。方法 40名健康志愿者,随机分为5组,在口服给药2 mg他克莫司5 min后,分别给予0、1、2、6及8粒五酯胶囊,于给药前、给药后不同时间点静脉取血,置于抗凝管中,保存至分析测定。结果他克莫司的药物动力学参数AUC0→t、Tmax随着五酯胶囊剂量的增大而增大,最大时分别可达到(459.3±114.2)ng/(h·ml)和(3.125±1.356)h,而Cmax则在五酯胶囊服用2粒时最大,达(43.539±10.656)ng/ml。口服清除率(CL/F ratio),1粒五酯胶囊时,就降至到51.67%,当服用8粒时,降至到27.09%。结论合用五酯胶囊后,他克莫司在体内代谢速度减慢,清除率降低,血药浓度升高。Objective To evaluate the effect of different doses of Wuzhi capsules on the pharmacokinatics of Tacrolimus in healthy human body. Methods 40 healthy volunteers were divided into 5 groups,and 0,1,2,6,8 capsules of Wuzhi capsules were given to each group accordingly after 2 mg of tacrolimus was given systematically. Venous blood was collected before and at different time points after drug administration. Blood samples were collected in anti-coagulation tubes and stored till analysis. Results The dose of tacrolimus was increased with the increase of the dose of Wuzhi capsules AUC0→t,Tmax,and the largest were（ 459. 3 ± 114. 2）ng·h / ml and（ 3. 125 ± 1. 356） h,respectively,and Cmax was the largest after taking two capsules（ 43. 539 ± 10. 656） ng / ml. The CL / F ratio decreased from 51. 67% to 27. 09% when the dose of Wuzhi capsules increased from 1 capsule to 8 capsules.Conclusions The metabolic rate of tacrolimus decreases,the clearance rate decreases and the blood concentration increases when Wuzhi capsules are administered together with tacrolimus.

关 键 词：他克莫司 五酯胶囊 药动学 高效液相色谱法 

分 类 号：R978[医药卫生—药品] R657.3[医药卫生—药学]