普乐可复在国内首例亲体小肠移植患者的个体化用药  

Individual medication of FK506 in the recipient of the first case of living-related small bowel transplantation in China

作　　者：文爱东[1] 王为忠[2] 宋维亮[2] 赵磊[1] 吴国生[2] 赵京霞[2] 

机构地区：[1]第四军医大学西京医院药剂科,陕西西安710033 [2]第四军医大学西京医院胃肠外科,陕西西安710033

出　　处：《第四军医大学学报》2002年第6期540-542,共3页Journal of the Fourth Military Medical University

摘　　要：目的　了解普乐可复 (FK5 0 6 )在亲体小肠移植患者体内药代动力学的规律 ,为临床小肠移植患者制定个体化用药方案 .方法　在患者 FK5 0 6血药浓度达稳态条件下 ,于一个给药周期 (τ)内间隔采集患者全血 11次 ,以微粒子酶免分析法 (MEIA)测定 FK5 0 6全血浓度 ,以 3P97药动学程序拟合求算 FK5 0 6在患者体内的药动学参数 ,以该患者个体的药动学参数为依据 ,为其实施个体化用药 .结果　在患者 poFK5 0 6 (5 mg· 12 h- 1 )稳态时 ,FK5 0 6在该患者体内的处置为一室开放模型 ,其主要的药动学参数 :达峰时间 Tmax、最大全血浓度ρmax、消除相半衰期 t1 / 2 ke、曲线下面积 AUC分别为1.4h,2 5 .1μg· L- 1 ,8.8h和 35 5 .7μg· h- 1 ·L- 1 ,FK5 0 6全血浓度波动差值为 13.7μg· L- 1 .结论　为降低 FK5 0 6全血浓度波动范围 ,采用 8h1次 po FK5 0 6更为适宜 ,同时应加强 FK5 0 6血药浓度监测 。AIM To investigate the clinical pharmacokinetics of FK506 in the recipient of living-related small bowel trans-plantation and to provide gist for clinical individual dosage. METHODS When level of FK506 had achieved steady state, the blood of patient was collected 11 times in scheduled time between a τ. Whole blood concentration of FK506 was analyzed by microparticle enzyme immunoassay (MEIA) before and after using the medicine. Fit the concentration-time date with the computer software package 3P97, and the parameters of pharmacokinetics were calculated. The patient was given individual medication of FK506 according to the parameters of pharmacokinetics. RESULTS Compartmental analysis yielded a one-compartment open model in the steady state after oral administration of FK506 5 mg·12 h -1. Pharmacokinetics parameters of FK506 were as follows: The T max=1.4 h, ρ max=25.1 μg·L -1, t 1/2Ke=8.8 h, AUC=355.7 μg·h -1·L -1, respectively. The fluctuant range of whole blood concentration of FK506 was 11.4 to 25.1 μg·L -1. CONCLUSION In order to reduce the fluctuant range of whole blood concentration of FK506, it is better to administrate FK506 three times a day rather than two times. The whole blood concentration of FK506 should be monitored to ensure safety and efficacy.

关 键 词：他罗利姆 小肠移植 药代动力学 普乐可复 

分 类 号：R656.7[医药卫生—外科学]