Radioactivity Detectors for High-Performance Liquid Chromatography in Drug Metabolism Studies

Abstract

Sensitive radioactivity detection following high performance liquid chromatography (HPLC) remains a challenge in drug metabolism studies with radiolabeled compounds. The aim of this review article is to give a general overview of scintillation counting techniques and to summarize recent advances in radioactivity detection for HPLC, with a strong emphasis on the application in drug metabolism studies. State of the art and new developments with homogeneous and heterogeneous on-line radioactivity detectors, stop-flow technology, off-line microplate solid scintillation counters (SSC), and accelerator mass spectrometry (AMS) will be discussed.

Design of A Metabolically Stable Tritium‐Tracer of the PI3Kδ‐Inhibitor CDZ173 (Leniolisib) as a Tool to Study Liver Metabolites

“…In order to cope with the analytical requirements of metabolic profiling from a regulatory perspective, radioanalytical tools are needed, that provide excellent sensitivity. Typically, the limit of detection of a tritium‐labelled analyte it is 0.2 – 0.7 Bq (10 – 40 dpm) . Practically this means, that a tritium‐tracer is able to detect the xenobiotic analyte in a pico‐ to femtomolar range allowing accurate and sensitive determination of metabolism pathways in ADME studies.…”

“…Typically, the limit of detection of a tritium-labelled analyte it is 0.2 -0.7 Bq (10 -40 dpm). [20] Practically this means, that a tritiumtracer is able to detect the xenobiotic analyte in a picoto femtomolar range allowing accurate and sensitive determination of metabolism pathways in ADME studies.…”

Strategies for Drawing Quantitative Conclusions from Nontargeted Liquid Chromatography–High-Resolution Mass Spectrometry Analysis

“…Almost full recovery. 44 Yes High LOD. Expensive radiolabeled standards and scintillation materials required.…”

Detection challenges in quantitative polymer analysis by liquid chromatography

“…Radioactivity detectors detect radioactive compounds selectively, typically by means of a scintillation agent that emits light when exited by radioactive decay [34]. Radio activity detectors offer some attractive features such as a high sensitivity (pg) and good linear dynamic range (10 4 , Table 1).…”

“…Radio activity detectors offer some attractive features such as a high sensitivity (pg) and good linear dynamic range (10 4 , Table 1). The applicability of radioactivity detection to polymer analysis is severely limited since it would require radioactive labeling, limiting it to its current main application area, metabolome studies [34,141].…”