Studies on Drug Metabolism by Use of Isotopes. XIV. Mass Spectrometric Quantification of Urinary Metabolites of Deuterated l-Ephedrine in Rabbits
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As part of problems on the applicability of a drug labeled with deuterium to metabolic studies in man, an analytical method for urinary metabolites by deuterium-tracer technique was investigated and its reliability was compared with that of ^<14>C-tracer technique. l-Ephedrine [arom.-^2H_5] or l-ephedrine [α-^<14>C] was subcutaneously injected to rabbits and the main urinary metabolites (1-phenyl-1,2-propanediol and hippuric acid) excreted for 24 hr after dosing were analyzed. A deuterated metabolite such as the diol absent in normal urine was submitted to the inverse isotope dilution analysis using the unlabeled compound both as an internal standard and as a carrier. The molar ratio of the unlabeled to the deuterated compound was determined by mass spectrometry. The amount of deuterated hippuric acid diluted with the endogenous material present in urine was determined by using both the direct isotope dilution analysis and the inverse isotope dilution analysis. It was found that reliability of the deuterium-tracer technique was comparable with that of the ^<14>C-tracer technique on the basis of data obtained from both techniques.
- 公益社団法人日本薬学会の論文
- 1975-02-25
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