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通过成像方法开发使用肠道器官进行药物流量运输分析的评估系统
Chihiro Koseki1, Takehiko Ishikawa1, Yuki Sato2
1School of Pharmaceutical Sciences and Pharmacy, Hokkaido University, Kita-12-jo, Nishi-6-chome, Kita-ku, Sapporo 060-0812, Japan.
Journal of pharmaceutical sciences
|June 13, 2024
概括
从肠道中提取的类固醇可以很容易地用于评估药物分泌方向,特别是P-glycoprotein (P-gp) 基质. 结和传递不会影响肠膜功能,使可靠的P-gp基质评估成为可能.
科学领域:
- 药理动力学 药理动力学
- 毒品运输是毒品的运输.
- 肠道有机物 肠道有机物
背景情况:
- 在体外评估药物分泌方向是具有挑战性的.
- 体是用于研究的肠道器官,但冷保存和传递对传送器功能的影响尚不清楚.
研究的目的:
- 为了研究通过和冷保存对体功能的影响,特别是P-glycoprotein (P-gp) 介导的药物运输.
- 建立一个简单和定量方法,用体来评估P-gp基质.
主要方法:
- 体受到了通过和冷保存.
- 罗达胺123 (Rh123) 转移到肠膜的速率与或没有P-gp抑制剂被测量.
- 分析了载体的mRNA表达水平.
主要成果:
- 过渡和冷保存并没有显著改变载体的mRNA表达水平.
- 类药物显示Rh123的P-gp介导的排泄到膜中.
- P-gp抑制剂显著降低了Rh123的分泌,导致细胞内积累.
- 在体操纵之前和之后,Rh123的转移率保持一致.
结论:
- 体是评估P-gp基质的可靠模型.
- 在P-gp运输研究中,冷保存和传递不会损害肠功能.
- 这种方法提供了一种简单而定量的方式来评估化合物的P-gp基质潜力.
相关概念视频
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