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 AUC_0→t, T_max, 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.