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Estimating the influences of orally administrated naringin on the activity of hepatic cytochrome P4503A1/2 enzyme in rats using a probe substrate method
Author(s): 
Pages: 503-509
Year: Issue:  9
Journal: Qilu Pharmaceutical Affairs

Keyword:  柚皮苷CYP3A1/2探针底物法高效液相串联质谱大鼠;
Abstract: 目的 采用体内探针底物法评价柚皮苷连续灌胃给药7 d对大鼠肝脏CYP3A1/2酶代谢活性的影响.方法 选择咪达唑仑作为CYP3A1/2的特异性探针底物;将大鼠随机分成对照组和4个柚皮苷给药组,其中对照组灌胃给予等体积超纯水,柚皮苷4个剂量组分别按50、125、250和500 mg·kg-1剂量灌胃给药连续7 d;给药完成后,尾静脉注射咪达唑仑溶液,于不同时间点采集血样,采用高效液相串联质谱法测定大鼠血浆中咪达唑仑的浓度,利用DAS2.0软件计算咪达唑仑的药动学参数AUC0~t、AUC0~∞、MRT0~t、MRT0~∞、t1/2、V、Cl和Cmax,以评价柚皮苷对大鼠肝脏CYP3A1/2酶代谢活性的影响.结果 与对照组比较,柚皮苷四个剂量组中的咪达唑仑主要药代动力学参数AUC0~t、AUC0~ ∞、MRT0~t、MRT0~∞、t1/2、V、Cl和Cmax均无显著差异(P>0.05).结论 大鼠经连续7 d灌胃给予柚皮苷(50~500 mg·kg-1)后,肝脏CYP3A1/2酶代谢活性未受到显著影响.
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