在大鼠体内联苯双酯对环孢素A药代动力学的影响

目的：探讨联苯双酯（bifendate，BDD）与环孢素A（cyclosporin，CsA）在大鼠体内合用后，联苯双酯对环孢素A药动学过程的影响。方法：随机分成治疗组和安慰剂组进行随机平行对照实验。用HPLC法测定大鼠全血中环孢素A浓度，采用非隔室模型方法计算药动学参数，并进行统计学比较。结果：环孢素A与联苯双酯合用后，前者在大鼠体内的血药浓度普遍降低，相对清除率（CL/F）显著增大（P〈0．05），生物半衰期（t1/2）显著缩短（P〈0．05），其余参数差异无统计学意义（P〉0．05）。结论：联苯双酯可明显降低环孢素A的血药浓度。联苯双酯与环孢素A合用时必须监测环孢素A的血药浓度。

Effects of Bifendate on the Pharmacokinetics of Cyclosporin A in Rats

Objective: To study the effects of bifendate (BDD) on the pharmacokinetics of cyclosporin A (CsA) in rats. Methods: Rats were randomly divided into treated group and control group and underwent randomized parallel study. The whole blood concentration of CsA was determined by HPLC, pharmacokinetic parameters were analyzed by non-compartment model and statistics study was performed. Results: The whole blood concentration of CsA decreased in both groups, the clearance/bioavailability (CL/F) increased significantly (P < 0.05), the half-life (t1/2) decreased significantly (P < 0.05) and no significant difference was observed in other parameters between 2 groups (P > 0.05) after the combination of CsA and BDD. Conclusion: The blood concentration of CsA decreases by the effect of BDD and should be monitored when it is combined with BDD.