Rui J Z, Zhuo H T, Jiang G H, Chen G
Department of Clinical Pharmacology, General Hospital of Nanjing Armed Forces.
Yao Xue Xue Bao. 1995;30(4):241-7.
NONMEM program was applied for estimating population pharmacokinetic parameters of cyclosporin A (CsA). The influence of body weight, age, sex and drug administration history on clearance were investigated. There were 281 CsA concentrations in whole blood from 60 clinical renal transplantation patients. Samples were analysed by HPLC and FPIA (TDx, Abbott, monoclonal antibody). One compartment open model with first-order absorption and elimination was used to analyse the data. Population mean values of CL(L.h-1), Vd(L), and Ka(h-1) were 59.8, 227, and 1.28 respectively. The interindividual variations of CL, Vd, and Ka were 30.27%, 29.01%, and 75.10% respectively. The residual error was 31.19%. The adjustment value of weight to clearance was 0.03 times with additional model. CL increased 4.31 in male patients, and decreased 12.7 when patients were treated with CsA for a long time.
使用NONMEM程序估算环孢素A（CsA）的群体药代动力学参数。研究了体重、年龄、性别和用药史对清除率的影响。收集了60例临床肾移植患者全血中的281个CsA浓度样本。采用高效液相色谱法（HPLC）和荧光偏振免疫分析法（FPIA，TDx，雅培公司，单克隆抗体）对样本进行分析。采用一级吸收和消除的一室开放模型对数据进行分析。清除率（CL，L·h-1）、分布容积（Vd，L）和吸收速率常数（Ka，h-1）的群体均值分别为59.8、227和1.28。CL、Vd和Ka的个体间变异分别为30.27%、29.01%和75.10%。残差误差为31.19%。在附加模型中，体重对清除率的校正值为0.03倍。男性患者的CL增加4.31，长期使用CsA治疗的患者CL降低12.7。
