Quantitation of Drug Metabolites by Radioactivity Detection Including Accelerator Mass Spectrometry (AMS)

摘要: The use of radioactivity is a well-established approach to generate data from wide range drug metabolism and pharmacokinetic (DMPK) activities, including absorption, distribution, metabolism, excretion (ADME) studies, investigations enzymology enzyme kinetics, tissue distribution studies in toxicology species. A variety methodologies available for the detection quantitation radioactive components, comprising off-line online approaches. Off-line techniques involve fractionation samples into either scintillation vials or microtiter plates followed by radiochemical analysis collected fractions. Online approaches employ radioflow cells, which utilize homogeneous detection, involving addition liquid scintillant, heterogeneous where solid scintillants are used. In addition, accelerator mass spectrometry (AMS), detects individual isotope ions, represents an alternative material. choice balance between sensitivity considerations time cost. terms sensitivity, generally offer improvement over techniques, although stop-flow can enhance while AMS provides dramatic further increase sensitivity. However, typically higher throughput than with being extremely slow costly. For these reasons, case-by-case optimal necessary, based on understanding capabilities various necessary address relevant ADME issues. Keywords: radiochemical detection; metabolites; quantitation; accelerator