Biotransformation of Isosorbide Dinitrate in Humans

An oral dose of 14C-isosorbide dinitrate was rapidly absorbed and eliminated by human subjects. Up to 99% was excreted in the urine. The drug was completely biotransformed, nearly 50% to the principal metabolite, an isosorbide conjugate, presumably with glucuronic acid. Up to 13% was excreted as fre...

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Veröffentlicht in:	Journal of pharmaceutical sciences 1974-07, Vol.63 (7), p.1147-1149
Hauptverfasser:	Down, W.H., Chasseaud, L.F., Grundy, R.K.
Format:	Artikel
Sprache:	eng
Schlagworte:	Autoradiography Biotransformation Biotransformation-isosorbide dinitrate Biotransformation—isosorbide dinitrate, excretion after oral administration, humans Carbon Radioisotopes Chromatography, Thin Layer excretion after oral administration Feces - analysis Half-Life Humans Isosorbide dinitrate Isosorbide Dinitrate - metabolism Isosorbide dinitrate, radiolabeled—biotransformation and excretion after oral administration, humans Metabolism-isosorbide dinitrate Metabolism—isosorbide dinitrate, humans radiolabeled-biotransformation and excretion after oral administration Time Factors
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Zusammenfassung:	An oral dose of 14C-isosorbide dinitrate was rapidly absorbed and eliminated by human subjects. Up to 99% was excreted in the urine. The drug was completely biotransformed, nearly 50% to the principal metabolite, an isosorbide conjugate, presumably with glucuronic acid. Up to 13% was excreted as free and conjugated 5-isosorbide mononitrate, and 1% was excreted as the free 2-isosorbide mononitrate only. D-Sorbitol possibly accounted for a further 18% of the radioactivity; an unknown metabolite, less polar than isosorbide, accounted for 6%.
ISSN:	0022-3549 1520-6017
DOI:	10.1002/jps.2600630728