Ndovi Themba T, Choi Leena, Caffo Brian, Parsons Teresa, Baker Sharon, Zhao Ming, Rohde Charles, Hendrix Craig W
Department of Medicine, Division of Clinical Pharmacology, School of Medicine, Johns Hopkins University, Baltimore, MD, USA.
Clin Pharmacol Ther. 2006 Aug;80(2):146-58. doi: 10.1016/j.clpt.2006.04.013.
The male genital tract is a complex collection of anatomically and biochemically distinct compartments that contribute to the ejaculate. Understanding the pharmacokinetics in these compartments should inform rational therapeutics involving these glands.
Nineteen men were administered a single dose of 600 mg chloroquine (base) and 975 mg aspirin before providing a semen sample by masturbation with fractionation into a 5-compartment collection device. Fractions were assayed for fructose (unique seminal vesicle marker), prostate-specific antigen (unique prostate marker), salicylate, and chloroquine. Seminal vesicle and prostate concentrations of salicylate and chloroquine were estimated via a novel analytic method involving a multilevel latent-variable model implemented by use of Bayesian methods.
The geometric mean chloroquine semen/blood ratio was 4.02 (95% confidence interval [CI], 2.36-6.86); for salicylate, the primary metabolite of aspirin, the semen/blood ratio was 0.10 (95% CI, 0.08-0.14). The estimated mean prostate/seminal vesicle ratio for salicylate, 0.38 (95% CI by Bayesian methods, 0.12-0.73), was consistent with our hypothesis that salicylate would achieve higher concentrations in the seminal vesicle than in the prostate. Chloroquine, however, did not demonstrate a statistically significant seminal vesicle/prostate difference (4.41; 95% CI by Bayesian methods, 0.14-30.52).
We successfully demonstrated the quantitative, noninvasive estimation of drug concentrations in the prostate gland fluid distinct from the seminal vesicle fluid using our optimized method of split-ejaculate collection and a novel mixed-effects model with Bayesian estimation. Our methods can be applied to gland-specific quantitation of drugs and other substances of interest, thus enabling pharmacokinetic, pharmacodynamic, and pathophysiologic studies to inform rational therapeutics within different glands of the male genital tract.
男性生殖道是由在解剖学和生物化学上不同的腔室组成的复杂集合,这些腔室对射精有贡献。了解这些腔室内的药代动力学情况应为涉及这些腺体的合理治疗提供依据。
19名男性在通过手淫提供精液样本并将其分馏到一个五腔收集装置之前,单次服用600毫克氯喹(碱)和975毫克阿司匹林。对各馏分进行果糖(精囊特异性标志物)、前列腺特异性抗原(前列腺特异性标志物)、水杨酸盐和氯喹的检测。通过一种涉及使用贝叶斯方法实施的多级潜在变量模型的新型分析方法,估算精囊和前列腺中水杨酸盐和氯喹的浓度。
氯喹的几何平均精液/血液比值为4.02(95%置信区间[CI],2.36 - 6.86);对于阿司匹林的主要代谢产物水杨酸盐,精液/血液比值为0.10(95%CI,0.08 - 0.14)。水杨酸盐的估计平均前列腺/精囊比值为0.38(贝叶斯方法的95%CI,0.12 - 0.73),这与我们的假设一致,即水杨酸盐在精囊中的浓度会高于前列腺。然而,氯喹在精囊/前列腺中的差异无统计学意义(4.41;贝叶斯方法的95%CI,0.14 - 30.52)。
我们通过优化的射精分离收集方法和具有贝叶斯估计的新型混合效应模型,成功地证明了对前列腺液中与精囊液不同的药物浓度进行定量、无创估计。我们的方法可应用于药物和其他感兴趣物质的腺体特异性定量,从而使药代动力学、药效学和病理生理学研究能够为男性生殖道不同腺体的合理治疗提供依据。