An amorphous form of montelukast sodium and a montelukast sodium lactose co-precipitate, processes for producing same, pharmaceutical compositions containing same and methods of treatment utilizing same are disclosed.
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What is claimed is: 1. A stable, non-hygroscopic, amorphous, free-flowing powder form of montelukast sodium. 2. The amorphous montelukast sodium of claim 1, wherein upon exposure to an atmosphere of about 30% humidity for a period of about one hour, the weight gain thereof is less than 2 weight p
What is claimed is: 1. A stable, non-hygroscopic, amorphous, free-flowing powder form of montelukast sodium. 2. The amorphous montelukast sodium of claim 1, wherein upon exposure to an atmosphere of about 30% humidity for a period of about one hour, the weight gain thereof is less than 2 weight percent of its total weight. 3. The amorphous montelukast sodium of claim 2, wherein said weight gain is less than 0.5 weight percent of its total weight. 4. The amorphous montelukast sodium of claim 1, which retains an amorphous character subsequent to storage at a temperature of at least 25° C. for a time period of at least 2 months. 5. The amorphous montelukast sodium of claim 4, which retains an amorphous character subsequent to storage at a temperature of about 40° C. for a time period of about 3 months. 6. The amorphous montelukast sodium of claim 1, having a bulk density greater than 0.10 g/cm3. 7. The amorphous montelukast sodium of claim 1, having a bulk density greater than 0.20 g/cm3. 8. The amorphous montelukast sodium of claim 1, having a bulk density that ranges between about 0.10 g/cm3 and about 0.40 g/cm3. 9. The amorphous montelukast sodium of claim 1, which retains an amorphous character subsequent to application of a pressure greater than 5000 Kg/cm3 for a period of about one minute. 10. The amorphous montelukast sodium of claim 9, which retains an amorphous character subsequent to application of pressure of about 10000 Kg/cm3 for a period of about one minute. 11. The amorphous montelukast sodium of claim 1, having a powder X-ray diffraction pattern substantially as depicted in FIG. 2. 12. A process of preparing the amorphous montelukast sodium of claim 1, the process comprising: dissolving montelukast sodium in a solvent, to thereby provide a solution of montelukast sodium in said solvent; and removing said solvent from said solution by spray drying, thereby obtaining the amorphous montelukast sodium. 13. The process of claim 12, wherein said solvent is selected from the group consisting of water, a water miscible organic solvent and a combination thereof. 14. The process of claim 13, wherein said water miscible organic solvent is selected from the group consisting of acetone, a C1-C3 alcohol, and any combination thereof. 15. The process of claim 13, wherein said water-miscible solvent is ethanol. 16. The process of claim 12, wherein said solvent is water. 17. The process of claim 12, wherein said solvent is ethanol. 18. The process of claim 12, wherein said solvent is a mixture of water and ethanol. 19. A pharmaceutical composition comprising the amorphous montelukast sodium of claim 1 and a pharmaceutically acceptable carrier wherein the amorphous character is maintained. 20. The pharmaceutical composition of claim 19, formulation in a solid dosage form. 21. The pharmaceutical composition of claim 20, wherein said solid dosage form is selected from the group consisting of a tablet, a capsule, a peel, a dragee, a powder and granules. 22. The pharmaceutical composition of claim 19, packaged in a packaging material and identified in print, in or on said packaging material, for treating a condition selected from the groups consisting of allergic rhinitis and asthma. 23. A method of treating a medical condition in which administration of montelukast sodium is beneficial selected from the group consisting of allergic rhinitis and asthma, the method comprising administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition of claim 19. 24. The method of claim 23, wherein said administering is effected orally. 25. The method of claim 24, wherein said pharmaceutical composition is formulated in a solid dosage form. 26. An amorphous mixture of montelukast sodium and at least one pharmaceutically acceptable excipient wherein the amorphous character is maintained. 27. The mixture of claim 26, wherein said at least one pharmaceutically acceptable excipient comprises lactose. 28. The mixture of claim 27, wherein the ratio between the amorphous montelukast and lactose ranges between about 1:0.1 and about 1:10. 29. The mixture of claim 28, wherein said ratio ranges between about 1:0.5 and 1:2. 30. The mixture of claim 28, wherein said ratio is about 1:1. 31. The mixture of claim 26, wherein upon exposure to an atmosphere of about 30% humidity for a period of one hour, the weight gain thereof is less than 2 weight percent of its total weight. 32. The mixture of claim 31, wherein said weight gain is less than 0.5 weight percent of its total weight. 33. The mixture of claim 26, which retains an amorphous character subsequent to storage at a temperature of at least 25° C. for a time period of at least 2 months. 34. The mixture of claim 33, which an amorphous character subsequent to storage at a temperature of about 40° C. for a tine period of about 3 months. 35. The mixture of claim 26, having a bulk density greater than 0.10 gram/cm3. 36. The mixture of claim 26, having a bulk density greater than t 0.20 gram/cm3. 37. The mixture of claim 26, having a bulk density that ranges between about 0.10 gram/cm3 and about 0.35 gram/cm3. 38. The mixture of claim 26, which retains an amorphous character subsequent to application of pressure of greater than 5,000 kg/cm3 for a period of about one minute. 39. The mixture of claim 38, which retains an amorphous character subsequent to application of pressure of about 10,000 Kg/cm3 for a period of about one minute. 40. The mixture of claim 26, having a powder X-ray diffraction pattern substantially as depicted in FIG. 3, FIG. 4 or FIG. 5. 41. A process of preparing the mixture of claim 26, the process comprising: dissolving montelukast sodium and at least one pharmaceutically acceptable excipient in a solvent, to thereby provide a solution of montelukast sodium in said solvent; removing said solvent from said solution, thereby obtaining the amorphous mixture of montelukast sodium and said at least one excipient. 42. The process of claim 41, wherein said at least one pharmaceutically acceptable excipient is lactose. 43. The process of claim 42, wherein said at least one pharmaceutically acceptable excipient is lactose monohydrate. 44. The process of claim 42, wherein a weight ratio between the amorphous montelukast and lactose ranges between about 1:0.1 and about 1:10. 45. The process of claim 42, wherein said weight ratio ranges between about 1:0.5 and 1:2. 46. The process of claim 42, wherein said ratio is about 1:1. 47. The process of claim 41, wherein said removing said solvent is effected by freeze drying said solution. 48. The process of claim 41, wherein said removing of said solvent is effected by spray drying said solution. 49. The process claim 41, wherein said solvent is selected from the group consisting of water, a water miscible organic solvent and a combination thereof. 50. The process of claim 49, wherein said water miscible organic solvent is selected from the group consisting of acetone, a C1-C3 alcohol, and any combination thereof. 51. The process of claim 49, wherein said water-miscible solvent is ethanol. 52. The process of claim 41, wherein said solvent is water. 53. The process of claim 41, wherein said solvent is ethanol. 54. The process of claim 41, wherein said solvent is a mixture of water and ethanol. 55. A pharmaceutical composition comprising the mixture of claim 26 and a pharmaceutically acceptable carrier wherein the amorphous character is maintained. 56. The pharmaceutical composition of claim 55, formulated in a solid dosage form. 57. The pharmaceutical composition of claim 56, wherein said solid dosage form is selected from the group consisting of a tablet, a capsule, a peel, a dragee, a powder and granules. 58. The pharmaceutical composition of claim 55, packaged in a packaging material and identified in print, in or on said packaging material, for treating a condition selected from the groups consisting of allergic rhinitis and asthma. 59. A method of treating a medical condition in which administration of montelukast sodium is beneficial selected from the group consisting of allergic rhinitis and asthma, the method comprising administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition of claim 55. 60. The method of claim 59, wherein said administering is effected orally. 61. The method of claim 60, wherein said pharmaceutical composition is formulated in a solid dosage form.
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