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本文主要研究大鼠体内瑞舒伐他汀和瑞格列奈在药动学和肝脏分布方面的相互作用.发现健康Wistar大鼠连续7天灌服瑞格列奈(0.5 mg/kg,1 mg/kg and 2 mg/kg)后给予瑞舒伐他汀(10 mg/kg),与对照组相比,瑞舒伐他汀AUC0-24和Cmax显著提高(P＜0.01),CL/F显著降低(P＜0.01),Tmax.和t1/2变化不明显,肝脏浓度显著减低(P＜0.01).大鼠连续7天灌服瑞舒伐他汀(20 mg/kg)后给予瑞格列奈(1 mg/kg),与对照组相比,瑞格列奈AUC㈦2和Cmax显著提高(P＜0.05),CL/F显著降低(P＜0.01),肝脏浓度显著降低(P＜0.01).瑞格列奈可影响瑞舒伐他汀药动学和肝脏分布,瑞舒伐他汀也可影响瑞格列奈的药动学和肝脏分布.“,”In the present study,we aimed to investigate the interactions of pharmacokinetics and liver distributions between rosuvastatin and repaglinide in rats.Coadministration of repaglinide (0.5 mg/kg,1 mg/kg and 2 mg/kg) for 7 d significantly increased the AUC0-24 and Cmax of rosuvastatin (P＜0.01),but dramatically decreased the CL/F of rosuvastatin (P＜0.01) after a single dose of rosuvastatin (10 mg/kg).There were no obviously changes in the parameters of Tmax and t1/2.Coadministration of repaglinide also decreased the liver distribution of rosuvastatin (P＜0.01).Coadministration of rosuvastatin (20 mg/kg) for 7 days significantly increased the AUC0-12 and Cmax of repaglinide (P＜0.05),and decreased the CL/F of repaglinide (P＜0.01) after a single dose of repaglinide (1 mg/kg).The liver distribution of repaglinide was also decreased (P＜0.01).Our animal study indicated that repaglinide could significantly affect the phannacokinetics and liver distribution ofrosuvastatin in rats and vice versa.