Pharmacokinetics of testosterone and estradiol gel preparations in healthy young men
Pharmacokinetics of testosterone and estradiol gel preparations in healthy young men
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DOI：
10.1016/j.psyneuen.2012.05.018
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发表时间：
2013-02-01
影响因子：
3.7
通讯作者：
von Eckardstein, Sigrid
中科院分区：
文献类型：
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作者：
Eisenegger, Christoph;von Eckardstein, Arnold;von Eckardstein, Sigrid
睾酮凝胶制剂的药代动力学数据的缺乏以及健康年轻男性中雌二醇给药的此类数据的缺乏构成了行为内分泌学研究的基本知识空白。我们在一项双盲安慰剂对照研究中解决了这个问题，其中我们对 28 名健康年轻男性使用了含有 150 毫克睾酮 (N = 10)、2 毫克雌二醇 (N = 8) 或相应安慰剂 (N = 10) 的局部凝胶。然后，我们在给药后一小时至七小时内评估雌二醇和睾酮的血清浓度，在基线时以及凝胶给药后三、四和六小时测量一次 LH、SHBG 和皮质醇水平。睾酮凝胶治疗在给药三小时后产生最大总血清睾酮浓度，并且在任何时间点都不会抑制 LH、皮质醇和 SHBG 水平。雌二醇凝胶的施用导致施用后两小时达到最大雌二醇血清浓度。皮质醇、SHBG 和绝对 LH 水平没有受到抑制。我们在此首次报告高剂量睾酮和雌二醇凝胶在健康年轻男性中应用的药代动力学数据。所提出的模型将有助于设计未来的研究，旨在建立睾酮和雌二醇凝胶给药与行为以及神经生理学效应之间的因果关系。 (C) 2012 Elsevier Ltd. 保留所有权利。
The paucity of pharmacokinetic data on testosterone gel formulations and absence of such data on estradiol administration in healthy young men constitutes a fundamental gap of knowledge in behavioral endocrinological research. We addressed this issue in a double-blind and placebo controlled study in which we applied a topical gel containing either 150 mg of testosterone (N = 10), 2 mg of estradiol (N = 8) or a respective placebo (N = 10) to 28 healthy young men. We then assessed serum concentrations of estradiol and testosterone in one hour intervals up to seven hours after drug application, measured LH, SHBG and cortisol levels once at baseline and three, four as well as six hours after gel administration. Treatment with testosterone gel resulted in maximum total serum testosterone concentration three hours after administration and did not suppress LH, cortisol and SHBG levels at any time point. Administration of estradiol gel led to maximum estradiol serum concentration two hours after administration. There was no suppression of cortisol, SHBG and absolute LH levels. We report here, for the first time, pharmacokinetic data on both high dose testosterone and estradiol gel application in healthy young males. The proposed model will assist in the design of future studies that seek to establish causality between testosterone and estradiol gel administration and behavioral as well as neurophysiological effects. (C) 2012 Elsevier Ltd. All rights reserved.