口服依西美坦后尿中内源性甾体排放规律  

The Endogenous Steroid Profile after Oral Administration of Exemestane

作　　者：刘欣[1] 杨声[1] 王静竹[1] 邢延一[1] 杨志勇[1] 徐友宣[1] 

机构地区：[1]国家体育总局反兴奋剂中心,北京100029

出　　处：《中国运动医学杂志》2011年第3期275-278,共4页Chinese Journal of Sports Medicine

摘　　要：依西美坦(exemestane)作为芳香酶抑制剂,因其能够抑制人体内的雄激素向雌激素转变,提高雄激素水平,而被世界反兴奋剂机构(WADA)禁用。本研究通过对一名健康男性志愿者口服单次治疗剂量依西美坦1片(25 mg/片)后,留取15天尿样,采用气相色谱/质谱联用技术,分析其中的内源性甾体激素并逐一定量,分析口服依西美坦后尿中内源性甾体激素的排放规律。结果显示,尿中睾酮等内源性雄性甾体激素浓度有一定增加,几种相关内源性雄性甾体激素比值无明显变化,而睾酮与雌酮浓度比值发生明显变化。采用气相色谱/同位素比质谱技术测定尿中雄酮和本胆烷醇酮的13C/12C比值,未显示外源性来源。结果提示口服单次治疗剂量依西美坦对尿中内源性甾体激素的排放有一定影响。Exemestane as the aromatase inhibitor is prohibited by WADA.Because exemestane inhibits the transformation of androgens to estrogens,and thus increases the androgens concentrations in human body.A healthy male voluntarily was administrated per os a single dose of exemestane（25 mg）.Urinary steroids were analyzed by gas chromatography-mass spectrometry（GC/MS）.Results showed that the concentrations of endogenous steroid increased,and their ratios varied insignificantly.The ratio of testosterone to estrone was raised quickly after exemestane administration.The 13C/12C ratios of androsterone and etiocholanolone in urine（determined by GC/C/IRMS） demonstrated that no other exogenous substance was found.It was shown that exemestane can affect the urinary steroid profile.

关 键 词：依西美坦 气相色谱/质谱 气相色谱/同位素比质谱 甾体激素排放规律 兴奋剂 

分 类 号：R96[医药卫生—药理学]