单剂量口服他达拉非在中国健康男性受试者的药代动力学和安全性  

Pharmacokinetics and safety of tadalafil in Chinese male healthy subjects after a single dose oral administration

作　　者：周颖[1] 吴春颖[1] 孙培红[1] 赵侠[1] 刘玉旺[1] 赵东方[1] 刘玉成 戴欣 崔一民[1] 孙忠民[1] 

机构地区：[1]北京大学第一医院药剂科,北京100034 [2]礼来公司,上海200021

出　　处：《中国临床药理学杂志》2005年第6期431-434,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的 研究中国健康男性受试者单剂量口服他达拉非的药代动力学和安 全性。方法 用双盲随机安慰剂对照三交叉设计。在3个周期随机单次服用 他达拉非10,20 mg或安慰剂,采集静脉血,用液相色谱-质谱法测定血药浓度 并计算药代动力学参数。结果 单次服用他达拉非10,20 mg后的主要药代动 力学参数AUC0-t分别为3750和7180 ng·h·mL-1;AUC0-∞分别为3820和 7370 ng·h·mL-1;Cmax分别为172和274 ng·mL-1;tmax分别为3．00和4．00 h;CL／F分别为2．61和2．71 L·h-1;V／F分别为67．6和73．2 L。结论 他达 拉菲在10-20 mg,中国健康男性受试者较安全,且AUC与剂量呈正相关。Objective To study the single dose pharmacokinetics and safety of tadalafil in Chinese male healthy subjects. Methods This was a single centre, investigator and subject - blind, randomised, placebo controlled, three- way crossover study. The treatment included a single oral dose of 10, 20 mg tadalafil, or matching placebos on three separate occasions in a randomised fashion. Venous blood samples for the measurement of serum tadalafil concentrations were collected at scheduled time. The concentration of tadalafil in plasma was measured by LC/MS method. The serum concentration -time data were individually analysed. Results The results showed that AUC0-t, were 3750 and 7180 ng ·h·mL^-1 following oral administration of 10 and 20 mg tadalafil, AUC0-∞, were 3820 and 7370 ng ·h·mL^-1 , Cmax were 172 and 274 ng ·mL^-1 , CL/F were 2. 61 and 2.71 L ·h^-1 , V/F were 67.6 and 73.2 L, respectively. Conclusion Tadalafil 10 mg and 20 mg were safe in Chinese male healthy subjects.

关 键 词：他达拉非片 液相色谱-质谱 药代动力学 安全性 

分 类 号：R969.1[医药卫生—药理学] R979.9[医药卫生—药学]