Nooter K, Schultz F, Sonneveld P
Res Commun Chem Pathol Pharmacol. 1984 Mar;43(3):407-15.
Cyclosporin-A (Cy-A) was administered to rats intravenously (i.v.) at different dosages (20, 40 and 80 mg/kg body weight). At the lower dose (20 mg/kg), the blood levels decreased biphasically and could be described by an open linear two-compartment model with excretion from the central compartment only. The t 1/2 values for the alpha-distribution and beta-elimination phases were about 6 min and 16.5 h, respectively. At higher dose levels (40 and 80 mg/kg), the involvement of an additional compartment became apparent. The blood concentration/time data sets obtained with 40 and 80 mg/kg doses were best described by an open linear three-compartment model. The 24-h urine and bile excretions were in the order of 10 and 20% of the total administered dose. The values for the normalized areas under the plasma concentration/time curves obtained at different Cy-A doses (20, 40 and 80 mg/kg) were about 1, 3 and 25, respectively.
将环孢素 A（Cy - A）以不同剂量（20、40 和 80 毫克/千克体重）静脉注射给大鼠。在较低剂量（20 毫克/千克）时，血药浓度呈双相下降，可用仅从中央室排泄的开放线性二室模型描述。α分布相和β消除相的 t1/2 值分别约为 6 分钟和 16.5 小时。在较高剂量水平（40 和 80 毫克/千克）时，另一个房室的参与变得明显。40 和 80 毫克/千克剂量获得的血药浓度/时间数据集最好用开放线性三室模型描述。24 小时尿液和胆汁排泄量约为总给药剂量的 10%和 20%。在不同 Cy - A 剂量（20、40 和 80 毫克/千克）下获得的血浆浓度/时间曲线下归一化面积值分别约为 1、3 和 25。
