TLC-DAR FOR THE ANALYSIS OF BIOLOGICAL SAMPLES - A NEWLY DEVELOPED RAPID TOOL FOR STUDYING DRUG-METABOLISM

This report, illustrated with practical examples, summarizes the advan tages and disadvantages of combined thin-layer chromatography-digital autoradiography (TLC-DAR) and other techniques (hereafter denoted 'non -TLC-DAR techniques') used for plate evaluation in planar chromatograp hy. It is demonstrated that this newly developed method can be widely used for the analysis of a variety of biological samples and, because information is obtained quickly at low cost, it is an excellent tool i n metabolism research. DAR is a convenient and extremely rapid means o f locating and quantifying radioactive metabolites on the TLC plate af ter separation and/or purification. TLC-DAR can be successfully used t o monitor intermediates and/or end products in the synthesis of radiol abeled compounds, to determine the radiochemical purity of chemicals, and to investigate the radiochemical stability of compounds in studies of the metabolism of xenobiotics. Using deramciclane (a new anxiolyti c compound) as an example, it has been shown that DAR can be successfu lly used to obtain information rapidly in different phases of the stud y of in-vitro and in-vivo metabolism. This report summarizes the appli cations and limitations of TLC-DAR in drug metabolism research and com pares various techniques used for detection of beta-emitting isotopes.