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目的:研究伏立康唑对家兔体内环孢素A(CsA)药动学的影响。方法:测定6只家兔单用CsA及合用伏立康唑后CsA的血药浓度,并进行药动学参数的计算与比较结果:与合用前比较,合用伏立康唑后CsA的t_(1/2)显著延长[(16.31±9.80)和(46.77±19.36)h,(P<0.05)],AUC_(0-24h)显著增加[(18.25±4.67)和(25.48±2.39)mg·h·L~(-1),(P<0.01)],CL显著降低[(2.29±0.62)和(1.43±0.17)L·h~(-1)·kg~(-1),(P<0.01)],其余药动学参数无显著变化。结论:合用伏立康唑后CsA的半衰期延长,临床上两者合用需调整CsA的剂量并监测血药浓度,以保证治疗的安全有效。
Objective: To study the effect of voriconazole on cyclosporine A (CsA) pharmacokinetics in rabbits. Methods: The plasma concentration of CsA in 6 rabbits and CsA combined with voriconazole were determined and the pharmacokinetic parameters were calculated and compared. The t_ (1/2) of CsA after voriconazole combination was significantly prolonged (18.25 ± 4.67) and (25.48 ± 2.39) mg · h · L -1 (-1) in AUC_ (0-24h) group were significantly higher than those in control group [(16.31 ± 9.80) and (46.77 ± 19.36) (P <0.01), CL significantly decreased (2.29 ± 0.62 vs 1.43 ± 0.17 L · h -1 · kg -1, P <0.01) No significant changes in learning parameters. CONCLUSION: The half-life of CsA is prolonged when voriconazole is combined. Clinically, the dosage of CsA should be adjusted and the plasma concentration monitored to ensure the safe and effective treatment.