在两种剂量水平下对阿姆洛迪平的肠道透性的多段评估
Müge Ateş1, Agata Bogacz Stelmasińska1, Michał Stelmasińska1
1Department of Pharmaceutical Technology, Faculty of Pharmacy, İnönü University, Malatya, Turkey.
氨基氨酸 (AML) 的肠道透性因地区和剂量而异. 通过高剂量降低了膜和结膜的透性,但在结肠中保持稳定.
科学领域:
- 药理动力学 药理动力学
- 药物吸收 药物的吸收
- 胃肠道生理学 胃肠道生理学
背景情况:
- 肠道透性显著影响口服药物的生物可用性.
- 胃肠道的区域差异影响药物吸收.
- 剂量依赖的吸收会影响药物的疗效和药理动力学.
研究的目的:
- 为了评估amlodipine (AML) 穿过阴,大肠和结肠的透性.
- 评估不同剂量 (5毫克和10毫克) 的阿姆洛迪平对其肠道透性的影响.
主要方法:
- 开发并验证了一种HPLC方法来量化AML,美托普罗罗尔和红色.
- 使用修改后的单通肠 perfusion (SPIP) 模型来测量 AML 透性在不同的老鼠肠道段.
- 测量净水流量 (NWF),以评估每个细分部分的生理反应.
主要成果:
- 净水流 (NWF) 显示出显著的变化,特别是结肠中的高正值.
- 阿姆洛迪平的有效透性 (Peff) 在肠道段和剂量之间有所不同.
- 在阴和阴中,AML Peff随着剂量增加 (5毫克至10毫克) 减少.
- 对AML的结肠透性在测试剂量中保持相对不变.
- 具体的佩夫值在1.80 × 10-4厘米/秒至6.79 × 10-4厘米/秒之间,取决于细分和剂量.
结论:
- 阿姆洛迪平的肠道透性表现出显著的区域和剂量依赖的变化.
- 在老鼠中的SPIP模型有效地证明了这些变化.
- 这些发现突显了考虑肠道区域和剂量对于阿姆洛迪平的药用动力学特征的重要性.
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