药物发现中深部脑刺激（DBS）的应用：小鼠连续微量取样药代动力学研究的开展
Utilization of DBS within drug discovery: development of a serial microsampling pharmacokinetic study in mice.
作者信息
Clark Graeme T, Haynes Julian J, Bayliss Mark A J, Burrows Lisa
机构信息
Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Sandwich Laboratories, Kent, UK.
出版信息
Bioanalysis. 2010 Aug;2(8):1477-88. doi: 10.4155/bio.10.91.
BACKGROUND
Dried blood spots (DBS) are rapidly gaining a foothold in the pharmaceutical industry. However, applications in exploratory drug discovery are limited mainly owing to method development time. The development of a generic DBS assay is presented with its application in serial microsampling from mice.
RESULTS
A generic 'fit-for-purpose' assay was developed on FTA(®) Elute, which allowed 90% of compounds tested to reach sensitivity levels of 1 ng/ml. A ten-time point serial mouse pharmacokinetic study was conducted using 20-µl microsamples and DBS. Application of generic 'fit-for-purpose' approach did not compromise data delivery or quality.
CONCLUSIONS
Serial microsampling and DBS in exploratory mouse pharmacokinetic has been shown to provide superior data quality when compared with traditional plasma-based composite studies.
背景
干血斑（DBS）在制药行业正迅速站稳脚跟。然而，其在探索性药物发现中的应用主要因方法开发时间而受到限制。本文介绍了一种通用的DBS分析方法及其在小鼠连续微量采样中的应用。
结果
在FTA®洗脱纸上开发了一种通用的“适用目的”分析方法，使90%的测试化合物达到1 ng/ml的灵敏度水平。使用20 μl微量样品和DBS进行了一项十点连续小鼠药代动力学研究。通用的“适用目的”方法的应用并未影响数据的提供或质量。
结论
与传统的基于血浆的综合研究相比，探索性小鼠药代动力学中的连续微量采样和DBS已被证明能提供更高的数据质量。
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