通过微透析法测定肺上皮衬液中药物的药代动力学：大鼠支气管中的氨基糖苷类抗生素

Pharmacokinetic measurement of drugs in lung epithelial lining fluid by microdialysis: aminoglycoside antibiotics in rat bronchi.

作者信息

Eisenberg E J, Conzentino P, Eickhoff W M, Cundy K C

机构信息

Department of Drug Delivery, Sterling Winthrop Pharmaceutical Research Division, Great Valley, PA 19355.

出版信息

J Pharmacol Toxicol Methods. 1993 Apr;29(2):93-8. doi: 10.1016/1056-8719(93)90056-k.

DOI:10.1016/1056-8719(93)90056-k

PMID:8318719

Abstract

A novel technique for in vivo intrabronchial pharmacokinetic measurements using microdialysis is described. The technique was applied to the measurement of tobramycin and gentamicin in the anesthetized rat. The concentration versus time profiles of the drugs in the lung epithelial lining fluid (ELF) following intravenous bolus administration were determined. The mean penetration ratios into the ELF were determined and found to be 0.36 +/- 0.06 (mean +/- SEM, n = 5) for gentamicin and 0.56 +/- 0.09 (mean +/- SEM, n = 5) for tobramycin. The findings suggest that the technique can be used for intrabronchial pharmacokinetic measurement of drugs in the lung, either as an extension of the bronchoalveolar lavage technique or as a practical alternative to it.

摘要

描述了一种使用微透析进行体内支气管内药代动力学测量的新技术。该技术应用于麻醉大鼠中妥布霉素和庆大霉素的测量。测定了静脉推注给药后肺上皮衬液（ELF）中药物的浓度-时间曲线。确定了进入ELF的平均渗透比，发现庆大霉素为0.36±0.06（平均值±标准误，n = 5），妥布霉素为0.56±0.09（平均值±标准误，n = 5）。研究结果表明，该技术可用于肺部药物的支气管内药代动力学测量，既可以作为支气管肺泡灌洗技术的扩展，也可以作为其实际替代方法。