Research & Development, GlaxoSmithKline, Stevenage, UK.
Department of Clinical, School of Life & Medical Sciences, Pharmaceutical & Biological Sciences, University of Hertfordshire, Hatfield, UK.
Bioanalysis. 2021 Jul;13(14):1101-1111. doi: 10.4155/bio-2021-0109. Epub 2021 Jul 19.
Determination of plasma protein binding () is considered vital for better understanding of pharmacokinetic and pharmacodynamic activities of drugs due to the role of free concentration in pharmacological response. Solid-phase microextraction (SPME) was investigated for measurement of from biological matrices and compared with a gold standard approach (rapid equilibrium dialysis [RED]). SPME-derived values of correlated well with literature values, and those determined by RED. Respectively, average protein binding across three concentrations by RED and SPME was 33.1 and 31.7% for metoprolol, 89.0 and 86.6% for propranolol and 99.2 and 99.0% for diclofenac. This study generates some evidence for SPME as an alternative platform for the determination of PPB.
测定血浆蛋白结合率()对于更好地理解药物的药代动力学和药效动力学活性至关重要,因为游离浓度在药理反应中起着重要作用。本文研究了固相微萃取(SPME)在测定生物基质中药物的蛋白结合率方面的应用,并将其与金标准方法(快速平衡透析[RED])进行了比较。SPME 法测定的蛋白结合率与文献值和 RED 法测定的值相关性良好。分别采用 RED 和 SPME 法在三个浓度下测定的平均蛋白结合率为:美托洛尔 33.1%和 31.7%,普萘洛尔 89.0%和 86.6%,双氯芬酸 99.2%和 99.0%。本研究为 SPME 作为测定蛋白结合率的替代平台提供了一些证据。