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Dose-dependent pharmacokinetics of metabolites of dipyrone in saliva

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Summary

Metabolites of dipyrone have been determined in the saliva of 18 volunteers following the oral intake of 0.5 g, 1.0 g, 1.5 g, 2.0 g and 2.5 g dipyrone. High concentrations were measured for N-methyl-aminoantipyrine (MAA), the other analgetic active metabolite, 4-aminoantipyrine was found in minor quantities only. N-formyl-antipyrine was not present in the saliva of some volunteers after low doses but could be determined following the intake of doses from 1.5 g – 2.5 g in saliva of all volunteers. N-acetyl-antipyrine appears late in saliva, acetylation rates varied greatly interindividually. Concentrations of the metabolites in saliva mimic the respective non-protein bound fraction in plasma found by other authors. Send reprint request to: Prof. Dr. P. Rohdewald, Institut für Pharmazeutische Chemie der Westfälischen Wilhelms-Universität Münster, Hittorfstr. 58/62, D-4400 Münster (FRG).

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Neddermann, E., Rohdewald, P. Dose-dependent pharmacokinetics of metabolites of dipyrone in saliva. European Journal of Drug Metabolism and Pharmacokinetics 13, 105–111 (1988). https://doi.org/10.1007/BF03191311

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