雷洛昔芬在肾功能正常和受损男性中的药代动力学。
Raloxifene pharmacokinetics in males with normal and impaired renal function.
作者信息
Czock David, Keller Frieder, Heringa Mette, Rasche Franz Maximilian
机构信息
University Hospital Ulm, Division of Nephrology, Ulm, Germany.
出版信息
Br J Clin Pharmacol. 2005 Apr;59(4):479-82. doi: 10.1111/j.1365-2125.2004.02326.x.
Abstract
AIMS
To compare raloxifene pharmacokinetics between renally impaired and healthy subjects.
METHODS
Raloxifene 120 mg was administered to 10 males with renal impairment (creatinine 2-4 mg dl(-1)) and to 10 healthy males. Data were analysed by two noncompartmental and one compartmental nonlinear regression methods.
RESULTS
The medians (95% confidence interval) of the area under the curves (AUC) were 35.1 (25.8, 74) and 20.5 (16.8, 28.0) h ng ml(-1) per mg kg(-1), P < 0.01, and of the clearances (CL/F) were 28.5 (13.5, 38.8) and 48.8 (35.8, 59.4) l h(-1) kg(-1), P < 0.01, in renally impaired and healthy subjects, respectively. 95% Confidence intervals on the differences for AUC and CL/F were 6.5-44.1 and -35.1 to -7.9, respectively.
CONCLUSION
Exposure to raloxifene was twice as high in males with renal impairment compared with healthy subjects.
摘要
目的
比较肾功能受损受试者与健康受试者之间雷洛昔芬的药代动力学。
方法
对10名肾功能受损男性（肌酐2 - 4mg dl⁻¹）和10名健康男性给予120mg雷洛昔芬。采用两种非房室和一种房室非线性回归方法分析数据。
结果
曲线下面积（AUC）的中位数（95%置信区间）在肾功能受损受试者和健康受试者中分别为35.1（25.8，74）和20.5（16.8，28.0）h ng ml⁻¹ per mg kg⁻¹，P < 0.01；清除率（CL/F）的中位数（95%置信区间）分别为28.5（13.5，38.8）和48.8（35.8，59.4）l h⁻¹ kg⁻¹，P < 0.01。AUC和CL/F差异的95%置信区间分别为6.5 - 44.1和 - 35.1至 - 7.9。
结论
与健康受试者相比，肾功能受损男性对雷洛昔芬的暴露量高两倍。
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