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绿茶教理素降低了raloxifene的In Vitro溶解度及其在小鼠中的全身暴露

Victoria O Oyanna¹, Baron J Bechtold¹, Katherine D Lynch¹

¹Department of Pharmaceutical Sciences, College of Pharmacy and Pharmaceutical Sciences, Washington State University, 412 E. Spokane Falls Blvd, Spokane, WA, 99202, USA.

Pharmaceutical research

|February 1, 2024

概括

绿茶绿茶是一种绿茶.

科学领域:

药理学和药物新陈代谢
自然产品化学化学

背景情况:

绿茶是一种流行的饮料,已知与药物代谢的相互作用.
一项先前的临床研究表明,绿茶可以将系统性暴露在拉洛西芬中减少34-43%.

研究的目的:

调查拉洛西芬溶解度的变化是否是绿茶消费后系统性暴露减少的机制.
评估绿茶成分对在模拟肠道液体中的拉洛西芬溶解度的影响.

主要方法:

评估了绿茶提取物,EGCG和EGC对禁食 (FaSSIF) 和食 (FeSSIF) 状态模拟肠液中的拉洛西芬溶解性的影响.
在FaSSIF和FeSSIF中评估了小胞体大小的变化.
进行了一项小鼠研究,以确定绿茶提取物和EGCG对拉洛西芬全身暴露 (Cmax和AUC) 的影响.

主要成果:

(-) - 乙甲基酸盐 (EGCG) 在FaSSIF中显著降低了78%的拉洛西芬溶解度,从而增加了小胞体大小.
(-) - 乙甲基素 (EGC) 显示溶解度略有降低 (13%) 没有影响小体大小.
在FeSSIF中,拉洛西芬的溶解度是FeSSIF的3.4倍,并不受绿茶提取物或EGCG的影响.
在小鼠中,绿茶提取物降低了44%的拉洛西芬Cmax,而EGCG对Cmax或AUC没有显著影响.

结论:

像EGCG一样,flavan-3-gallate catechins可以降低水溶性较差的药物的可溶性,例如raloxifene.
这种降低的溶解度,特别是在禁食状态下,可能解释了临床研究中观察到的全身暴露的减少.
这些发现强调了在制药研究和临床实践中考虑饮料药物相互作用的重要性.

关键词:

吸收吸收吸收吸收绿茶绿茶是一种绿茶.我们的肠道是肠道.药物动力学药物动力学溶解度溶解度溶解度溶解度

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