提格环素的吸收通过精选的辅助剂得到改善.
Hubert Ziółkowski1, Kalina Szteyn1, Dawid Jędrzkiewicz2
1Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Warmia and Mazury in Olsztyn, Oczapowskiego 13, 10-718 Olsztyn, Poland.
Pharmaceuticals (Basel, Switzerland)
|August 26, 2023
概括
诸如HP-β-CD,TPGS和SDOCH之类的辅助剂显著提高了tigecycline在中的口服生物可用性. 其他测试的化合物显示了不同程度的改善,表明可能有更好的tigecycline吸收.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物运输 药物运输 药物运输
- 兽医医学 兽医医学 兽医医学
背景情况:
- 蒂格环素是一种四环环素抗生素,口服吸收不良.
- 提高tigecycline的口服生物可用性对于有效的治疗应用至关重要.
- 肉作为胃肠道吸收研究的相关动物模型.
研究的目的:
- 评估各种辅助剂对tigecycline的血度和口服生物可用性的影响.
- 确定可以显著改善肉tigecycline吸收的特定辅助剂.
主要方法:
- 提格环素被静脉和口服给肉,有或没有辅助剂.
- 使用高性能液体染色学与合质谱法测量了tigecycline的血度.
- 对血度-时间数据进行了药理动力学分析 (分区和非分区).
主要成果:
- 惠普-β-CD,TPGS和SDOCH大约增加了tigecycline在曲线下的面积和口服生物利用率的两倍.
- 在DM-β-CD和TMC中,这些药理动力学参数的增加较小,但显著.
- 甲酸盐没有显著影响tigecycline的生物可用性.
结论:
- 惠普-β-CD,TPGS和SDOCH有效地提高了tigecycline的口服生物可用性.
- DM-β-CD和TMC也可能提供显著的生物利用性改善,这需要进一步的研究.
- 这些发现表明了改善兽医中口服tigecycline输送的潜在策略.
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