1/2)有減少趨勢,但差異均不顯著;紅花組咖啡因和氯唑沙宗的CL有所降低,但差異不顯著,咪達(dá)唑侖的CL顯著降低(P<0.01),氯唑沙宗的AUC增加,但差異不顯著,咖啡因和咪達(dá)唑侖的AUC明顯增加(P<0.05、0.01);丹參+紅花組咖啡因和氯唑沙宗的CL明顯降低(P<0.05),曲線下面積(AUC)明顯增加(P<0.05),其t1/2有延長趨勢,但差異不顯著。結(jié)論 丹參、紅花配伍后對CYP450亞型CYP1A2和CYP2E1有抑制作用,這可能是丹參、紅花配伍協(xié)同增效的作用機(jī)制之一。;Objective To study the influence of Salviae Miltiorrhizae Radix et Rhizome (SMR) and Carthami Flos (CF) before and after compatibility on activitis of cytochrome P1A2 (CYP1A2), cytochrome P2E1 (CYP2E1), and cytochrome P3A4 (CYP3A4) from rat liver microsomes. Methods Using caffeine, chlorzoxazone, and midazolam as the probe drugs of CYP1A2, CYP2E1, and CYP3A4, the SD rats were randomized divided into four groups:control group, SMR (1.2 g crude drug/kg) group, CF (0.4 g crude drug/kg) group, and SMR (1.2 g crude drug/kg)+CF (0.4 g crude drug/kg) group. According to the above dose, rats were ig given drugs for 7 d. Rats were injected with caffeine, chlorzoxazone, and midazolam solution in tail vein 30 min after the last administration, and the blood was collected at different time points. Metronidazole as internal standard, method has been established to determine the levels of caffeine, chlorzoxazone, and midazolam to evaluate the activities of CYP1A2, CYP2E1, and CYP3A4 by HPLC. Results Compared with control group, SMR increased the clearance rates (CL) of caffeine, chlorzoxazone, and midazolam, reduced the AUC, and t1/2 was also show a decreasing trend, but the difference was not significant. In CF group, CL of caffeine and chlorzoxazone was decreased, but the difference is not significant. CL of midazolam significantly decreased (P<0.01). AUC of chlorzoxazone increased, but the difference was not significant. AUC of caffeine and midazolam increased significantly (P<0.05 and 0.01). In SMR+CF group, the CL of caffeine and chlorzoxazone decreased significantly (P<0.05), the AUC of caffeine and chlorzoxazone increased significantly (P<0.05), and t1/2 also showed a decreasing trend, but the difference is not significant. Conclusion Compatibility of SMR and CF has an inhibitive effect on CYP1A2 and CYP2E1 in rats, and it could be one of the mechanisms of interactive synergy."/>

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首頁 > 過刊瀏覽>2017年第40卷第3期 >2017,40(3):300-306. DOI:10.7501/j.issn.1674-6376.2017.03.003
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丹參-紅花藥對配伍前后對大鼠肝藥酶亞型CYP1A2、CYP2E1和CYP3A4活性的影響

Effect of Salviae Miltiorrhizae Radix et Rhizoma and Carthami Flos before and after compatibility on activities of CYP1A2, CYP2E1, and CYP3A4 from rat liver microsomes

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