大黄素对环孢素A在大鼠体内的药代动力学  

The effect of emodin on the pharmacokinetics of intragastrically administered cyclosporine A in rats

作　　者：陈侨[1] 李慧[1] 罗红军[1] 罗文鸿[1] 

机构地区：[1]汕头大学医学院分析测试实验室,广东汕头515041

出　　处：《中国临床药理学杂志》2012年第6期444-447,共4页The Chinese Journal of Clinical Pharmacology

基　　金：广东省自然科学基金团队资助项目(9351507102000001)

摘　　要：目的评价中药成分大黄素对大鼠灌服环孢素A(CsA)的药代动力学。方法 60只雄性SD大鼠按体重进行随机分为5组,分别灌服CsA+60 mg.kg-1高剂量蒸馏水;CsA+30 mg.kg-1低剂量酮康唑;CsA+大黄素(60 mg.kg-1);CsA+大黄素(30 mg.kg-1);1～3 d大黄素,第4 d灌服CsA+大黄素。用HPLC-MS法测定全血中CsA的浓度,kinetica软件计算主要药代动力学参数,用SPSS17.00进行统计学分析。结果阳性对照组与空白对照组药代动力学参数除吸收速率外均有显著性差异;高剂量大黄素组使其较快达到峰浓度(P<0.05);低剂量大黄素组药代动力学参数与空白对照组比较无显著性差异;服用3 d大黄素后,最后1 d灌服CsA+大黄素组的吸收速率和峰浓度与空白对照组比较有显著性差异(P<0.05)。结论大黄素对CsA的生物利用度和代谢无明显影响。Objective To investigate the effect of emodin,an active ingredient of a commonly used Chinese herb,on the pharmacokinetics of cyclosporine A（CsA） by intragastric administration in rats.Methods Sixty male Sprague-Dawley rats were equally divided into five groups by randomized block design according to weight.Group Ⅰ： CsA plus distilled water;group Ⅱ： CsA plus KCZ（150 mg·kg-1）;group Ⅲ： CsA plus emodin（60 mg·kg-1）;group Ⅳ： CsA＋emodin（30 mg·kg-1）;group Ⅴ： After administrated emodin for three days,CsA coadministrated with emodin on the fourth day.Whole blood CsA concentration was measured by HPLC-MS.The data of time-blood concentrations of CsA were analyzed by kinetica practical pharmacokinetics program and SPSS 17.0.Results The results implied that AUC,Cmax,Tmax,T1/2 and CL of CsA had significant difference between the CsA coadministration of water and coadministration of ketoconazole（P0.05 and P0.01）,while the Tmax had significant difference between the CsA coadministration of water and coadministration of high dose emodin（P0.05）.The Ka and Tmax had significant difference between the CsA coadministration of water and coadministration of three-day low dose emodin（P0.05）.There was not significant difference between the CsA coadministration of water and coadministration low dose emodin.Conclusion The emodin had no obvious influence on the absorption of CsA and the metabolism of CsA.

关 键 词：环孢素A 大黄素 药代动力学 液质联用 

分 类 号：R969.1[医药卫生—药理学] R979.5[医药卫生—药学]