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Claims for Patent: 5,681,590

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Claims for Patent: 5,681,590

Title: Dry mix formulation for bisphosphonic acids
Abstract:Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.
Inventor(s): Bechard; Simon R. (Quebec, CA), Kramer; Kenneth A. (Green Lane, PA), Katdare; Ashok V. (Norristown, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:08/454,100
Patent Claims: 1. A process for the preparation of a tablet containing an active ingredient selected from:

4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid;

N-methyl-4-amino-1-hydroxybutylidene-1,1-bis-phosphonic acid;

4-(N,N-dimethylamino)-1-hydroxybutylidene-1,1-bisphosphonic acid;

3-amino-1-hydroxypropylidene-1,1-bisphosphonic acid;

3-(N,N-dimethylamino)-1-hydroxypropylidene-1,1-bisphosphonic acid;

1-hydroxy-3-(N-methyl-N-pentylamino)propylidene-1,1-bisphosphonic acid;

1-hydroxy-2-[3-pyridyl]ethylidene-1,1-bisphosphonic acid;

4-(hydroxymethylene-1,1-bisphosphonic acid)piperidine;

or a pharmaceutically acceptable salts thereof;

which process comprises:

forming a mixture by mixing the active ingredient with:

a diluent, selected from: anhydrous lactose and hydrous fast

flow lactose,

a dry binder,

a disintegrant,

and optionally one or more additional ingredients selected

from the group consisting of: compression aids, flavors,

flavor enhancers, sweeteners and preservatives;

lubricating the mixture with a lubricant; and

compressing the resultant lubricated mixture into a desired

tablet form.

2. The process of claim 1 wherein the active ingredient is 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid.

3. The process of claim 1 wherein the active ingredient is 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium salt trihydrate.

4. The process of claim 1 wherein the dry binder is microcrystalline cellulose.

5. The process of claim 1 wherein the disintegrant is selected from the group consisting of modified starch, modified cellulose polymer, and croscarmallose sodium, and a combination thereof.

6. The process of claim 1 wherein the disintegrant is croscarmallose sodium.

7. The process of claim 1 wherein the lubricant is magnesium stearate.

8. A solid dosage form containing an active ingredient selected from the group consisting of:

4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid;

N-methyl-4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid;

4-(N,N-dimethylamino)-1-hydroxybutylidene-1,1-bisphosphonic acid;

3-amino-1-hydroxypropylidene-1,1-bisphosphonic acid;

3-(N,N-dimethylamino)-1-hydroxypropylidene-1,1-bisphosphonic acid;

1-hydroxy-3-(N-methyl-N-pentylamino)propylidene-1,1-bisphosphonic acid;

1-hydroxy-2-[3-pyridyl]ethylidene-1,1-bisphosphonic acid; and

4-(hydroxymethylene-1,1-bisphosphonic acid)piperidine;

or a pharmaceutically acceptable salt thereof;

wherein the dosage form is prepared by the process of claim 1.

9. A pharmaceutical composition comprising by weight, about 0.5 to 40% by weight of an active ingredient selected from the group consisting of:

4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid;

N-methyl-4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid;

4-(N,N-dimethylamino)-1-hydroxybutylidene-1,1-bisphosphonic acid;

3-amino-1-hydroxypropylidene-1,1-bisphosphonic acid;

3-(N,N-dimethylamino)-1-hydroxypropylidene-1,1-bis-phosphonic acid;

1-hydroxy-3-(N-methyl-N-pentylamino)propylidene-1,1-bisphosphonic acid;

1-hydroxy-2-[3-pyridyl]ethylidene-1,1-bisphosphonic acid; and

4-(hydroxymethylene-1,1-bisphosphonic acid)piperidine;

or a pharmaceutically acceptable salt thereof;

and from about 60 to 99.5% by weight of excipients consisting essentially of: hydrous fast flow lactose; microcrystalline cellulose; croscarmallose sodium; and magnesium stearate.

10. A pharmaceutical composition comprising by weight, about 0.5 to 40% by weight of an active ingredient selected from the group consisting of:

4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid;

N-methyl-4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid;

4-(N,N-dimethylamino)-1-hydroxybutylidene-1,1-bisphosphonic acid;

3-amino-1-hydroxypropylidene-1,1-bisphosphonic acid;

3-(N,N-dimethylamino)-1-hydroxypropylidene-1,1-bisphosphonic acid;

1-hydroxy-3-(N-methyl-N-pentylamino)propylidene-1,1-bisphosphonic acid;

1-hydroxy-2-[3-pyridyl]ethylidene-1,1-bisphosphonic acid; and

4-(hydroxymethylene-1,1-bisphosphonic acid)piperidine;

or a pharmaceutically acceptable salt thereof;

about 10 to 80% by weight of hydrous fast flow lactose;

about 5 to 50% by weight of microcrystalline cellulose;

about 0.5 to 10% by weight of croscarmallose sodium; and

about 0.1 to 5% by weight of magnesium stearate.

11. The pharmaceutical composition of claim 10 comprising about 0.5 to 25% by weight of the active ingredient, about 30% to 70% by weight of hydrous fast flow lactose; about 30 to 50% by weight of microcrystalline cellulose; about 0.5 to 5% by weight of croscarmallose sodium; and about 0.1 to 2% by weight of magnesium stearate.

12. The pharmaceutical composition of claim 10 wherein the active ingredient is 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid.

13. The pharmaceutical composition of claim 10 wherein the active ingredient is 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium salt trihydrate.

14. A tablet prepared from the pharmaceutical composition of claim 13.

15. A tablet prepared from the pharmaceutical composition of claim 10.

16. A process for the preparation of a table containing as active ingredient a basic nitrogen containing bisphosphonate: which process comprises:

forming a mixture by mixing the active ingredient with:

a diluent, selected from: anhydrous lactose or hydrous fast flow lactose,

a dry binder,

a disintegrant,

and optionally one or more additional ingredients selected

from the group consisting of: compression aids, flavors,

flavor enhancers, sweeteners and preservatives;

lubricating the mixture with a lubricant; and

compressing the resultant lubricated mixture into a desired tablet form.

17. A solid dosage form containing as active ingredient a basic nitrogen containing bisphosphonate wherein the dosage form is prepared by the process of claim 1.
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