[Comparative pharmacokinetics and bioavailability of isosorbide dinitrate and its metabolites isosorbide 5- and 2-mononitrate from delayed-release preparations]. 1982

A Geigenberger, and J Degen, and H Maier-Lenz

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.

UI MeSH Term Description Entries
D007548 Isosorbide Dinitrate A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action. Cardonit 40,Dilatrate,Iso-Bid,Isodinit,Isoket,Isoket Retard-120,Isomak R,Isordil,Isotrate,Nitrosorbide,Sorbitrate,Sorbonit,Dinitrate, Isosorbide,Iso Bid,IsoBid,Isoket Retard 120,Isoket Retard120
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D003692 Delayed-Action Preparations Dosage forms of a drug that act over a period of time by controlled-release processes or technology. Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities

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