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Claims for Patent: 5,358,941

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Claims for Patent: 5,358,941

Title: Dry mix formulation for bisphosphonic acids with lactose
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. (Laval, CA), Kramer; Kenneth A. (Green Lane, PA), Katdare; Ashok V. (Norristown, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:07/984,399
Patent Claims: 1. 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; and from about 60 to 99.5% by weight of excipients consisting essentially of:

anhydrous lactose; microcrystalline cellulose; croscarmallose sodium; and magnesium stearate.

2. 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 anhydrous 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.

3. The pharmaceutical composition of claim 2 comprising about 0.5 to 25% by weight of the active ingredient, about 30 to 70% by weight of anhydrous 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.

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

5. The pharmaceutical composition of claim 2 wherein the active ingredient is 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium salt trihydrate.

6. The pharmaceutical composition of claim 5 comprising about 1 to 25% by weight of the active ingredient, 4-amino-1-hydroxybutylidene-1,1bisphosphonic acid monosodium salt trihydrate, about 40 to 60% by weight of anhydrous lactose; about 35 to 45% by weight of microcrystalline cellulose; about 0.5 to by weight of croscarmallose sodium; and about 0.1 to by weight of magnesium stearate.

7. The pharmaceutical composition of claim 5 in the form of a tablet.

8. The pharmaceutical composition of claim 2 in the form of a tablet.
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