【摘要】 目的:研究五味子酯甲对免疫抑制剂他克莫司在大鼠体内吸收的促进作用。方法:大鼠分别灌胃五味子酯甲(5、10、20mg/kg)、南五味子提取物(145 mg/kg)或空白溶剂后再灌胃他克莫司,分别于不同时间点取血,采用液相色谱-串联质谱法测定全血中的他克莫司浓度。结果:5、10、20 mg/kg的五味子酯甲使他克莫司的峰浓度提高了0.51、2.87、2.96倍,使浓度-时间曲线下面积提高了1.22、4.08、6.40倍。10 mg/kg的五味子酯甲与145 mg/kg的南五味子提取物对他克莫司的吸收促进作用相似。结论:五味子酯甲可大幅促进他克莫司在大鼠体内的吸收,有望被开发成他克莫司的吸收促进剂。更多还原

【Abstract】 OBJECTIVE:To study the promotion effects of schisantherin A on the absorption of tacrolimus in rats.METHODS:Tacrolimus was intragastrically administered to rats after intragastrical administration of schisantherin A(5,10,20 mg/kg),Schisandra sphenanthera extract(145 mg/kg),or blank solvent.The blood sample was collected at different time points,and the blood concentration of tacrolimus was assayed by LC-MS.RESULTS:By the dose of 5 mg/kg,10 mg/kg and 20 mg/kg schisantherin A,the Cmax of tacrolimus was enhanced by 0.51、2.87 and 2.96 folds,respectively,and the AUC of tacrolimus was enhanced by 1.22 folds,4.08 folds and 6.40 folds,respectively.Schisantherin A(10 mg/kg) possessed the similar activity with S.sphenanthera extract on the absorption of tacrolimus(145 mg/kg).CONCLUSIONS:Schisantherin A can enhance the absorption of tacrolimus rapidly and it is a promising absorption promoter of tacrolimus.更多还原