Back to results
US 5,399,362 AGranted
Once-a-day metoprolol oral dosage form
AssigneeEdward Mendell Co., Inc.
InventorsAnand Baichwal, Troy W. McCall
Life of this patent
Estimating the term…
Abstract
A sustained release oral solid dosage form of metoprolol pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, a cationic cross-linking agent. The formulation provides release of metoprolol for at least about 24 hours.
Claims20
A tablet for the sustained release of metoprolol or a salt thereof, comprising:
- metoprolol or a pharmaceutically acceptable salt thereof in an amount necessary to render a therapeutic effect in a human patient;
- from about 8% to about 35% heteropolysaccharide gum;
- from about 0.5% to about 20% of a cationic cross-linking agent selected from the group consisting of alkali metal and alkaline earth metal sulfates, chlorides, borates, bromides, citrates, acetates, lactates and mixtures thereof and capable of crosslinking with said heteropolysaccharide gum to increase the gel strength when said formulation is exposed to an environmental fluid;
- an inert pharmaceutical diluent selected from the group consisting of monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof;
- the ratio of metoprolol to said heteropolysaccharide gum being from about 1:1 to about 1:5, said dosage form providing a sustained release of metoprolol for at least about 24 hours when exposed to an environmental fluid.
2 more elements
A method of preparing a 24 hour formulation of metoprolol, comprising:
- preparing a sustained release matrix comprising from about 8 to about 35% of a heteropolysaccharide gum and from about 1 to about 20% of a cationic crosslinking agent selected from the group consisting of alkali metal and alkaline earth metal sulfates, chlorides, borates, bromides, citrates, acetate, lactates and mixtures thereof and capable of crosslinking with said heteropolysaccharide gum agent to increase the gel strength when said gum is exposed to an environmental fluid, and an inert pharmaceutical diluent;
- combining said sustained release matrix with metoprolol or a pharmaceutically acceptable salt to provide a drug:gum ratio from about 1:1 to about 1:5;
- and
- tableting the resultant mixture such that each tablet includes a dose of metoprolol sufficient to provide a therapeutic effect for at least about 24 hours.
1 more element
A method of treating a patient with metoprolol, comprising,
- preparing a sustained release matrix comprising from about 8 to about 35% of a heteropolysaccharide gum and from about 1 to about 20% of a cationic crosslinking agent selected from the group consisting of alkali metal and alkaline earth metal sulfates, chlorides, borates, bromides, citrates, acetates, lactates and mixtures thereof and capable of crosslinking with said heteropolysaccharide gum agent to increase the gel strength when said gum is exposed to an environmental fluid, and an inert pharmaceutical diluent;
- combining said sustained release excipient with metoprolol or a pharmaceutically acceptable salt to provide a drug:gum ratio from about 1:1 to about 1:5;
- and
- tableting the resultant mixture such that each tablet includes a dose of metoprolol sufficient to provide a therapeutic effect for at least about 24 hours, and
- administering said tablets to a patient at an appropriate dosing interval.
2 more elements
Dependencies are inferred from the claim text.