在比较内灌注与吸入输送时,暴露和耐受性的差异
Mikael Brülls1, Elin Holmedal2, Ramon Hendrickx3
1Early Product Development and Manufacturing, Pharmaceutical Sciences, BioPharmaceuticals R&D, AstraZeneca, Gothenburg, Sweden.
Journal of aerosol medicine and pulmonary drug delivery
|September 3, 2025
概括
与吸入药物相比,药物通过内灌注进入肺部会导致更高的全身暴露和更低的肺部药物水平. 这种侵入性方法可能会导致药物过早泄露到循环中.
科学领域:
- 药物动力学和药物输送
- 呼吸系统医学
- 生物医学工程
背景情况:
- 药物局部输送到肺部对于治疗呼吸系统疾病至关重要.
- 内灌注和吸入是常见的使用途径.
- 了解暴露差异对于优化治疗结果至关重要.
研究的目的:
- 为了比较肺部和全身药物暴露后的内灌注与吸入输送.
- 评估药物耐受性的使用途径的影响.
- 阐明针对肺部药物的这些输送方法之间的药理学差异.
主要方法:
- 动物通过内灌注和吸入输送获得三种不同药物的等效肺剂量.
- 在药物注射后立即量化了血和肺部药物分量.
- 在两种治疗条件下,对一种化合物的耐受性进行了评估.
主要成果:
- 与吸入输送相比,内灌注导致血初始度显著提高.
- 在灌注后,药物的较低初始分量仍留在肺部.
- 一种药物在吸入后表现出更好的耐受性,而不是在内灌注时.
结论:
- 内灌注的侵入性可能导致药物在施用期间过早泄露到全身循环中.
- 吸入药物似乎为向肺部的药物提供了更有利的药理学特征.
- 药物使用途径显著影响药物暴露和耐受性.
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