Gupta S K, Legg B, Solomon L R, Johnson R W, Rowland M
Department of Pharmacy, University of Manchester.
Br J Clin Pharmacol. 1987 Oct;24(4):519-26. doi: 10.1111/j.1365-2125.1987.tb03206.x.
1 The pharmacokinetics of cyclosporin were studied in 12 renal transplant patients. Five patients received a constant rate (7 mg kg-1 day-1) intravenous infusion over 72 h and the remainder received rates of 7, 4 and 10 mg kg-1 day-1, consecutively each for at least 24 h. 2 Plasma, separated at 37 degrees C, was analysed by h.p.l.c. 3 The data were best described by a biexponential model. 4 Following the 72 h infusion, a plateau was reached by 24 h and clearance was 0.60 l h-1 kg-1. 5 Clearance associated with the 10 mg kg-1 day-1 infusion rate (0.43 l h-1 kg-1) was estimated to be lower than that following the 4 and 7 mg kg-1 day-1 rates (0.52 and 0.54 l h-1 kg-1 respectively) but the difference is unlikely to be of clinical significance.
对12名肾移植患者的环孢素药代动力学进行了研究。5名患者在72小时内接受了恒定速率(7毫克/千克/天)的静脉输注,其余患者分别接受了7、4和10毫克/千克/天的速率,每种速率至少持续24小时。
在37摄氏度下分离的血浆通过高效液相色谱法进行分析。
数据用双指数模型能得到最佳描述。
在72小时输注后,24小时达到平台期,清除率为0.60升/小时/千克。
估计与10毫克/千克/天输注速率相关的清除率(0.43升/小时/千克)低于4毫克/千克/天和7毫克/千克/天速率后的清除率(分别为0.52和0.54升/小时/千克),但这种差异不太可能具有临床意义。