Czejka M J, Jäger W, Schüller J, Fogl U, Schernthaner G
Institut für Pharmazeutische Chemie, Universität Wien.
Arzneimittelforschung. 1991 Aug;41(8):860-3.
The plasma levels of fluorouracil (5-fluorouracil, 5FU; CAS 51-21-8) after intravenous administration have been monitored without, under influence of interferon-alpha-2b (IFN) and under influence of IFN combined with folic acid (FA). IFN causes a highly significant change of the pharmacokinetic parameters of 5FU (p less than 0.001) compared to 5FU administration without IFN. The bioavailability of 5FU (compared as the AUC0-60 values) is elevated to 80%. In contrary, the combination of IFN with FA leads to a non-significant change of the 5FU pharmacokinetics, although the bioavailability is increased to 18%. The higher plasma levels of 5FU under the influence of IFN might be causes by a changed renal clearance, which is indicated by the reduction of the total plasma clearance at about 53%. The combination IFN/FA did not show a similar effect. Yet, in both cases an improvement of the tumor response and of the clinical picture could be observed.
在静脉注射后,对氟尿嘧啶(5-氟尿嘧啶,5FU;化学物质登记号51-21-8)的血浆水平进行了监测,监测情况分别为未使用干扰素-α-2b(IFN)、使用IFN以及使用IFN联合叶酸(FA)。与未使用IFN的5FU给药相比,IFN导致5FU的药代动力学参数发生极显著变化(p<0.001)。5FU的生物利用度(以AUC0-60值比较)提高到了80%。相反,IFN与FA联合使用导致5FU药代动力学无显著变化,尽管生物利用度提高到了18%。IFN影响下5FU的血浆水平较高可能是由于肾脏清除率改变所致,这表现为总血浆清除率降低约53%。IFN/FA联合使用未显示出类似效果。然而,在这两种情况下均观察到肿瘤反应和临床表现有所改善。