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目的观察部分药物对华法林在大鼠肝微粒体中代谢的影响。方法选择在临床上可能与华法林合用的药物,如瑞舒伐他汀、辛伐他汀、硝苯地平、甲苯磺丁脲、罗红霉素、雷尼替丁和左氧氟沙星。分别将其与华法林在大鼠肝微粒体系中共孵育,采用高效液相色谱法测定华法林的浓度。结果瑞舒伐他汀和辛伐他汀对华法林代谢有抑制作用,与对照组相比有显著差异(P<0.05)。瑞舒伐他汀和辛伐他汀对华法林抑制的IC50值分别为17.53和4.87μmol·L-1,且剂量依赖性抑制华法林的代谢,抑制率分别为6%～32%和18%～47%。其他药物对华法林代谢无显著影响。结论瑞舒伐他汀和辛伐他汀可能抑制华法林在大鼠肝微粒体中的代谢。
Objective To observe the effects of some drugs on the metabolism of warfarin in rat liver microsomes. METHODS: Drugs that may be clinically used in combination with warfarin, such as rosuvastatin, simvastatin, nifedipine, tolbutamide, roxithromycin, ranitidine and levofloxacin, were selected. Each was incubated with warfarin in rat liver particle system, and the concentration of warfarin was determined by high performance liquid chromatography. Results Rosuvastatin and simvastatin inhibited the metabolism of warfarin significantly compared with the control group (P <0.05). The IC50 values of rosuvastatin and rosuvastatin on simvastatin were 17.53 and 4.87μmol·L-1, respectively. The inhibition rates of warfarin and rosuvastatin were 6% -32% and 18% respectively, ~ 47%. Other drugs have no significant effect on warfarin metabolism. Conclusion Rosuvastatin and simvastatin may inhibit the metabolism of warfarin in rat liver microsomes.