目的：研究西伐他汀对环孢素药物动力学的影响．方法：男性汉族健康志愿者７人随机交叉口服单剂量环孢素１００ｍｇ和同时口服西伐他汀１０ｍｇ后，采用特异性荧光偏振免疫法测定环孢素全血药物浓度．结果：血药浓度—时间曲线拟合表明该药体内过程符合二室开放模型，合用西伐他汀前后环孢素的主要药代动力学参数：Ｃｍａｘ（６４６±９４）和（６９８±３４０）μｇ·Ｌ－１；Ｔｍａｘ（１１２±０１３）和（１１３±０２１）ｈ；ＡＵＣ（２３±０４）和（２６±１２）ｍｇ·ｈ·Ｌ－１；Ｔ１２β（１２±６）和（２３±８）ｈ（Ｐ＜００５）．结论：环孢素与西伐他汀同时应用时，后者可延迟环孢素的代谢 Objective: To study the effect of simvastatin on the pharmacokinetics of cyclosporine. Methods: Seven randomized healthy volunteers of Han nationality were randomized to receive a single dose of cyclosporine 100 mg and simvastatin 10 mg at the same time. Cyclosporine whole blood concentration was determined by specific fluorescence polarization immunoassay. Results: The plasma concentration-time curve fitting showed that the in vivo process of the drug conformed to the two-compartment open model. The main pharmacokinetic parameters of ciclosporin before and after the combination of simvastatin: Cmax (646 ± 94) and (698 ± 340) μg · L-1; Tmax (112 ± 013) and (113 ± 021) h; AUC (23 ± 04) and (26 ± 12) mg · h · L-1; T12β (12 ± 6) and (23 ± 8) h (P <005). Conclusion: When cyclosporine and simvastatin are used in combination, the latter can delay cyclosporine metabolism