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Last Updated: March 28, 2024

Claims for Patent: 6,090,410


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Summary for Patent: 6,090,410
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:09/141,782
Patent Claims: 1. A pharmaceutical composition comprising from about 0.5 to 40% by weight of a bisphosphonic acid or a pharmaceutically acceptable salt thereof and from about 60% to 99.5% by weight of excipients, said excipients comprising a diluent selected from the group consisting of anhydrous lactose and hydrous fast flow lactose, a binder, a disintegrant, and a lubricant.

2. A pharmaceutical composition comprising from about 0.5 to 40% by weight of a nitrogen containing bisphosphonic acid or a pharmaceutically acceptable salt thereof and from about 60% to 99.5% by weight of excipients, said excipients comprising a diluent selected from the group consisting of anhydrous lactose and hydrous fast flow lactose, a binder, a disintegrant, and a lubricant.

3. A pharmaceutical composition according to claim 2 wherein said nitrogen containing bisphosphonic acid or pharmaceutically acceptable salt thereof is N-methyl-4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition according to claim 2 wherein said nitrogen containing bisphosphonic acid or pharmaceutically acceptable salt thereof is 4-(N,N-dimethylamino)-1-hydroxybutylidene-1,1-bisphosphonic acid or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition according to claim 2 wherein said nitrogen containing bisphosphonic acid or pharmaceutically acceptable salt thereof is 3-amino-1-hydroxypropylidene-1,1-bisphosphonic acid or a pharmaceutically acceptable salt thereof.

6. A pharmaceutical composition according to claim 2 wherein said nitrogen containing bisphosphonic acid or pharmaceutically acceptable salt thereof is 3-(N,N-dimethylamino)-1-hydroxypropylidene-1,1-bisphosphonic acid or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition according to claim 2 wherein said nitrogen containing bisphosphonic acid or pharmaceutically acceptable salt thereof is 1-hydroxy-3-(N-methyl-N-pentylamino)propylidene-1,1-bisphosphonic acid or a pharmaceutically acceptable salt thereof.

8. A pharmaceutical composition according to claim 2 wherein said nitrogen containing bisphosphonic acid or pharmaceutically acceptable salt thereof is 1-hydroxy-2-[3-pyridyl]ethylidene-1,1-bisphosphonic acid or a pharmaceutically acceptable salt thereof.

9. A pharmaceutical composition according to claim 2 wherein said nitrogen containing bisphosphonic acid or pharmaceutically acceptable salt thereof is 4-(hydroxymethylene-1,1-bisphosphonic acid) piperidine or a pharmaceutically acceptable salt thereof.

10. A pharmaceutical composition according to claim 2 wherein said nitrogen containing bisphosphonic acid or pharmaceutically acceptable salt thereof is 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or a pharmaceutically acceptable salt thereof.

11. A pharmaceutical composition according to claim 2 wherein said nitrogen containing bisphosphonic acid or pharmaceutically acceptable salt thereof is 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid monosodium salt trihydrate.

12. 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; 4-(hydroxymethylene-1,1-bisphosphonic acid) piperidine; or a pharmaceutically acceptable salt thereof; and from about 60% to 99.5% by weight of excipients comprising: a diluent selected from the group consisting of anhydrous lactose and hydrous fast flow lactose, a binder, a disintegrant, and a lubricant.

13. A composition according to any of claims 1-12 wherein said diluent is anhydrous lactose.

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