Frey F J, Horber F F, Frey B M
Medizinische Poliklinik, University of Berne, Switzerland.
Clin Pharmacol Ther. 1988 Jan;43(1):55-62. doi: 10.1038/clpt.1988.11.
We determined the AUC of cyclosporine (24 hours) nonspecifically by RIA and specifically by HPLC after an oral and an intravenous dose of cyclosporine in 58 patients undergoing renal transplantation. The RIA/HPLC concentration ratio of cyclosporine changed continuously during the first 12 hours after administration. The ratio was higher after oral than after intravenous administration and varied from patient to patient. The predictive value of trough levels for the corresponding AUCs was better when trough levels were assessed 24 than 12 hours after administration. Trough levels assessed by RIA poorly predicted AUCs measured specifically by HPLC. Therefore if, in the future, therapeutic cyclosporine monitoring has to be improved, trough levels should be assessed 24 hours after the last dose by means of a specific HPLC method.
我们通过放射免疫分析法(RIA)非特异性地测定了58例肾移植患者口服和静脉注射环孢素后环孢素(24小时)的曲线下面积(AUC),并通过高效液相色谱法(HPLC)特异性地进行了测定。给药后最初12小时内,环孢素的RIA/HPLC浓度比值持续变化。口服给药后的该比值高于静脉给药后,且因患者而异。给药后24小时评估谷浓度时,其对相应AUC的预测价值优于给药后12小时。通过RIA评估的谷浓度对通过HPLC特异性测定的AUC预测效果较差。因此,如果未来要改善环孢素治疗监测,应在最后一剂后24小时通过特定的HPLC方法评估谷浓度。