Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Sandwich, Kent CT13 9NJ, UK.
Lab Anim. 2011 Apr;45(2):124-6. doi: 10.1258/la.2010.010155. Epub 2011 Feb 25.
The use of dried blood spots (DBS) in preclinical studies has seen an enormous increase over the past two years. Despite its positive impact on the 3Rs (reduce, replace and refine), its uptake in exploratory drug discovery has been limited due mainly to protracted method development time in bioanalysis but also the need for small volumes (<20 μL) to be sampled manually. Automatic blood sampling technology such as the DiLab(®) AccuSampler(®) is widely used in drug discovery to facilitate exploratory rodent-based pharmacokinetic and pharmacokinetic/pharmacodynamic studies with minimal animal handling. Propranolol was orally administered to a Han-Wistar rat attached to either a standard DiLab(®) AccuSampler(®) or a retrofitted unit designed to directly collect the DBS samples. In all, 50 or 20 μL blood samples were then collected via the standard or retrofitted unit, respectively, at six timepoints over a 7 h period. After drying and storage the DBS samples were analysed for propranolol via liquid chromatography-mass spectrometry. In this report we demonstrate that a standard DiLab(®) AccuSampler(®) can be easily retrofitted to facilitate automatic dried blood spot sampling and that time-concentration data generated from these samples are equivalent to that from manually spotted samples.
在过去的两年中,干血斑(DBS)在临床前研究中的应用有了巨大的增长。尽管它对 3R(减少、替代和优化)有积极的影响,但由于生物分析中方法开发时间延长,以及需要手动采集小体积(<20 μL)的样本,其在探索性药物发现中的应用受到限制。DiLab(®) AccuSampler(®)等自动采血技术在药物发现中被广泛应用,以方便最小动物处理的基于啮齿动物的探索性药代动力学和药代动力学/药效学研究。将普萘洛尔口服给予连接到标准 DiLab(®) AccuSampler(®)或改装单元的 Han-Wistar 大鼠,该改装单元旨在直接采集 DBS 样本。总共在 7 小时的时间内,通过标准或改装单元分别采集了 50 或 20 μL 的血液样本。在干燥和储存 DBS 样本后,通过液质联用技术分析普萘洛尔。在本报告中,我们证明了标准的 DiLab(®) AccuSampler(®)可以很容易地进行改装,以方便自动采集干血斑样本,并且从这些样本中获得的时间浓度数据与手动采集样本的结果相当。