Microdialysis for in vivo pharmacokinetic/pharmacodynamic characterization of anti-infective drugs
Microdialysis for in vivo pharmacokinetic/pharmacodynamic characterization of anti-infective drugs
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DOI：
10.1016/j.coph.2005.04.010
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发表时间：
2005-10-01
影响因子：
4
通讯作者：
Müller, M
中科院分区：
文献类型：
--
作者：
Brunner, M;Derendorf, H;Müller, M
抗生素的组织渗透不足可能导致治疗失败和细菌耐药性。因此，抗生素的药代动力学评价应基于组织而不是血清浓度。几年来，通过组织活检等方法获得的组织浓度数据已经对抗生素组织分布的正确解释产生了缺陷。微透析-一种半侵入性的基于导管的采样技术-已被用于抗生素组织药代动力学的体内测量。由于大多数抗感染药物选择性进入靶部位，微透析满足药代动力学分布研究的法规要求，并可能在不久的将来成为组织分布研究的参考技术。此外，微透析可能有助于在药物开发过程中定义有意义的抗生素效率替代标志物。
Inadequate tissue penetration of antibiotics can lead to therapeutic failure and bacterial resistance. Pharmacokinetic evaluation of antibiotics should therefore be based on tissue rather than serum concentrations. Over several years, tissue concentration data obtained by methods such as tissue biopsies have flawed the correct interpretation of antibiotic tissue distribution. Microdialysis - a semi-invasive catheter-based sampling technique - has been employed for the in vivo measurement of antibiotic tissue pharmacokinetics. Owing to selective access to the target site for most anti-infective drugs, microdialysis satisfies regulatory requirements for pharmacokinetic distribution studies and might become a reference technique for tissue distribution studies in the near future. Furthermore, microdialysis might contribute to the definition of meaningful surrogate markers for antibiotic efficiency during drug development.