[Comparative pharmacokinetics and bioavailability of isosorbide dinitrate and its metabolites isosorbide 5- and 2-mononitrate from delayed-release preparations].
The present comparative pharmacokinetic study performed to establish the relative bioavailability for an isosorbide dinitrate (ISDN) retard preparation (Sorbidilat-retard) included 6 healthy, male and female volunteers. In a randomised cross-over scheme the volunteers received a capsule Sorbidilat retard forte and a tablet of a standard preparation which contained as well 40 mg isosorbide dinitrate as retard formulation. Blood samples were taken over a period of 24 h and isosorbide dinitrate, 5-isosorbide mononitrate and 2-isosorbide mononitrate measured in the serum by means of gas chromatography with electron-capture detection. The resorption rate for all three substances revealed only minor differences between Sorbidilat and the standard preparation. However, the slightly retarded absorption for the compound from Sorbidilat with a longer period of invasion led to a higher maximal concentration and to higher serum levels of ISDN and the mononitrates over the whole period of observation. The relative bioavailability for all three substances ISDN, 5-isosorbide mononitrate and 2-isosorbide mononitrate, was estimated from the areas under the plasma concentration-time curves and was 2 to 2.5 fold higher for the Sorbidilat preparation than for the standard preparation.
D000328:Adult; D001682:Biological Availability; D003692:Delayed-Action Preparations; D005260:Female; D006801:Humans; D007548:Isosorbide Dinitrate / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism*; D007700:Kinetics; D008297:Male
D003692:Delayed-Action Preparations; C030398:isosorbide-2-mononitrate; D007548:Isosorbide Dinitrate; C030397:isosorbide-5-mononitrate
Vergleichende Pharmakokinetik und Bioverfügbarkeit von Isosorbiddinitrat und seiner Metaboliten 5- und 2-Isosorbidmononitrat aus zwei Retardpräparaten.