Port R E, Edler L, Herrmann R, Feldmann U
Institute of Biochemistry, Deutsches Krebsforschungszentrum, Heidelberg, F.R.G.
Ther Drug Monit. 1991 Mar;13(2):96-102.
The correlation between single plasma concentration (CP) values of 5-fluorouracil (FU) after a 10-minute i.v. infusion and the total area under the plasma concentration-time curve (AUC) has been studied in 26 cancer patients. FU dose was either 320-550 mg/m2 (seven patients, 13 treatments) or 610-960 mg/m2 (19 patients, 30 treatments). Linear single CP-AUC relationships were found in both dose groups with the CPs at 1, 5, 10, 15, and 30 minutes after the end of infusion. Parameters of linear regression of AUC on single CP differed between the two dose groups. For the high-dose group, the single CPs at repeated treatments were tested as estimators of the total AUC at these treatments, using calibration lines relating total AUC to single CP, which were derived from the data of the first (or only) treatments of all patients. The "best" AUC estimators of the total AUC were the CPs at 10 and 15 minutes after the end of infusion, with a bias of only 2% and an imprecision of only 11% of the AUC values directly determined from the complete concentration-time profiles of the repeated treatments. Because of the close correlation between these single CPs and the total AUC, these CPs should be considered equivalent to the AUC as an overall index of individual FU kinetics after brief infusion of high doses.
在26例癌症患者中研究了静脉输注10分钟后5-氟尿嘧啶（FU）的单次血浆浓度（CP）值与血浆浓度-时间曲线下总面积（AUC）之间的相关性。FU剂量为320 - 550mg/m²（7例患者，13次治疗）或610 - 960mg/m²（19例患者，30次治疗）。在两个剂量组中均发现输注结束后1、5、10、15和30分钟时的CP与AUC呈线性关系。两个剂量组中AUC对单次CP的线性回归参数有所不同。对于高剂量组，使用将总AUC与单次CP相关联的校准线（这些校准线源自所有患者首次（或仅有的）治疗数据），将重复治疗时的单次CP作为这些治疗中总AUC的估计值进行测试。总AUC的“最佳”AUC估计值是输注结束后10和15分钟时的CP，其偏差仅为2%，不精密度仅为直接从重复治疗的完整浓度-时间曲线确定的AUC值的11%。由于这些单次CP与总AUC之间密切相关，在高剂量短暂输注后，这些CP应被视为等同于AUC，作为个体FU药代动力学的总体指标。
