The present routine to conduct balance and/or tissue dissection distribution studies has now and then been questioned, because the way they are generally conducted does not produce information in proportion to the spending of animal and personnel resources. Usually only total radioactivity is measured and due considerations are not always taken to the metabolic fate of the label. In this study a different strategy is presented-integrating quantitative whole-body radioluminography and different chromatographic methods on extracts of tissue pieces punched from the whole-body sections. In addition to the saving in cost and time, the proposed integrated whole-body radioluminographic/metabolic profile protocol will provide (i) a detailed picture of the distribution of radioactivity at selected dose levels and time points in male, female, and pregnant animals; (ii) the time course of radioactivity in blood/plasma and tissues selected from the images (approximate half-life and AUC); (iii) accumulated urinary and fecal excretion of radioactivity and an estimate of the proportion of radioactive metabolites; (iv) tissue information about the proportion of parent drug versus metabolites of pieces punched from the whole-body sections; and (v) indications of possible tissue binding.
Copyright 2000 Academic Press.