依普利酮在健康受试者体内的尿药排泄特征  

Study on urinary excretion characteristics of eplerenone in healthy volunteers

作　　者：钱文娟[1] 丁黎[1] 文爱东[2] 徐贵丽[3] 贺建昌[3] 龚斌[1] 云昌宏[1] 冷晔[1] 杨林[2] 

机构地区：[1]中国药科大学药物分析教研室,江苏南京210009 [2]中国人民解放军第四军医大学西京医院国家药品临床试验机构,陕西西安710032 [3]中国人民解放军成都军区昆明总医院药学部,云南昆明650032

出　　处：《中国新药与临床杂志》2009年第4期258-262,共5页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的建立人尿样中依普利酮浓度的HPLC-MS测定法,并研究依普利酮在健康人体内的尿药排泄特征。方法20名健康受试者分别单次口服依普利酮25、50和100mg,测定尿药浓度,计算尿药排泄参数,并进行统计比较。结果在给药后36h内低、中、高3个剂量下人体尿液中的累积排泄量分别为(594±s302)μg,(1085±185)μg和(2558±854)μg,排泄率为2.17%～2.56%。男性受试者的累积排泄量和最大排泄速率高于女性受试者。结论在25～100mg剂量范围内,依普利酮尿排泄量及最大排泄速率与剂量呈线性关系,不同剂量组之间排泄率无差异,依普利酮尿药排泄参数存在性别差异。AIM To establish a HPLC-MS method for the determination of eplerenone in urine sample and to investigate the urinary excretion characteristics of eplerenone in healthy Chinese volunteers. METHODS Twenty healthy volunteers were given splitting single doses of eplerenone 25, 50, and 100 mg orally, followed by determination and calculation of the concentrations of eplerenone in urine and finally compared by statistical analysis. RESULTS The accumulation amounts of eplerenone excreted in urine after 36 h of administration were （594 ± s 302）, （1 085 ± 185）, and （2 558 ±854） μg for the 25, 50, and 100 mg dosages, respectively. The excretion rates for the dosage range of 25 - 100 mg were 2.17% - 2.56%. The accumulation amounts of eplerenone excreted and the maximum excretion rates in urine of the male were higher than those of the female. CONCLUSION The accumulation amounts of eplerenone excreted and the maximum excretion rates in urine increased with linear correlation to the doses of eplerenone ranging from 25 mg to 100 mg and no significant difference in between them; but only different in gender.

关 键 词：抗高血压药 色谱法 高压液相 光谱法 质量 电喷雾电离 药动学 依普利酮 尿药排泄 

分 类 号：R972.4[医药卫生—药品] R969.1[医药卫生—药学]