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Details for Patent: 6,858,231

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Details for Patent: 6,858,231

Title: Pharmaceutical excipient having improved compressibility
Abstract:A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.
Inventor(s): Sherwood; Bob E. (Amenia, NY), Staniforth; John H. (Bath, GB), Hunter; Edward A. (Glenham, NY)
Assignee: J. Rettenmaier & Soehne GmbH + Co. KG (Rosenberg, DE)
Filing Date:Jan 08, 2003
Application Number:10/338,361
Claims:1. A method for preparing a pharmaceutical excipient comprising: forming an aqueous shiny of microcrystalline cellulose in the form of a wet cake; forming an aqueous slurry of silicon dioxide having a particle size of from about 1 in to about 100 .mu.m; separately introducing said microcrystalline shiny and said silicon dioxide slurry into a drying apparatus for combination therein, to obtain an excipient comprising a plurality of agglomerated particles of microcrystalline cellulose in intimate association with said silicon dioxide, the amount of silicon dioxide being from about 0.5% to about 20% relative to the amount of microcrystalline cellulose, by weight.

2. The method of claim 1, wherein said silicon dioxide of said aqueous slurry of silicon dioxide has an average primary particle size from about 5 mu to about 40 .mu.m.

3. The method of claim 1, wherein said agglomerated particles have a bulk density from about 0.35 g/ml to about 0.55 g/ml.

4. The method of claim 1, wherein said agglomerated particles have a bulk density from about 0.2 g/ml to about 0.6 g/ml.

5. The method of claim 1, wherein said agglomerated particles further comprise a member of the group consisting of non-silicon metal oxides, starches, starch derivatives, surfactants, polyalkylene oxides, celluloses, cellulose ethers, cellulose esters and mixtures thereof.

6. The method of claim 1, wherein said aqueous slurry of microcrystalline cellulose slurry contains from about 0.5% to about 25% microcrystalline cellulose by weight in the form of a wet cake.

7. The method of claim 1, wherein said aqueous slurry of microcrystalline cellulose contains from about 15% to about 20% microcrystalline cellulose in the form of a wet cake.

8. The method of claim 1, wherein said aqueous slurry of microcrystalline cellulose contains from about 17% to about 19% microcrystalline cellulose in the form of a wet cake.

9. The method of claim 1, wherein said silicon dioxide is colloidal silicon dioxide.

10. The method of claim 1, wherein said silicon dioxide has a surface area from about 10 m.sup.2 /g to about 500 m.sup.2 /g.

11. The method of claim 1, wherein said silicon dioxide has a surface area from about 50 m.sup.2 /g to about 500 m.sup.2 /g.

12. The method of claim 1, wherein said silicon dioxide has a surface area from about 175 m.sup.2 /g to about 350 m.sup.2 /g.

13. The method of claim 1, wherein said silicon dioxide is present in an amount from about 0.5% to about 10% by weight, based on the weight of said microcrystalline cellulose.

14. The method of claim 1, wherein said silicon dioxide is present in an amount from about 1.25% to about 5% by weight, based on the weight of said microcrystalline cellulose.

15. The method of claim 1, wherein said agglomerated particles have an average particle size from about 10 .mu.m to about 1,000 .mu.m.

16. The method of claim 1, wherein said agglomerated particles have an average particle size from about 10 .mu.m to about 500 .mu.m.

17. The method of claim 1, wherein said agglomerated particles have an avenge particle size from about 30 .mu.m to about 250 .mu.m.

18. The method of claim 1, wherein said agglomerated particles have a moisture content of from about 0.5 to about 15%.

19. The method of claim 1, wherein said agglomerated particles have a moisture content of from about 2.5 to about 6%.

20. The method of claim 1, wherein said agglomerated particles have a moisture content of from about 3.0 to about 5%.

21. The method of claim 1, wherein said drying of said aqueous slurry of microcrystalline cellulose and said aqueous slurry of silicon dioxide is accomplished by a method selected from the group consisting of spray drying, flash drying, ring drying, micron drying, tray drying, vacuum drying, radio-frequency drying and microwave drying.

22. The method of claim 1, wherein said drying of said aqueous slurry of microcrystalline cellulose and said aqueous slurry of silicon dioxide is accomplished by spray drying.

23. A method for preparing a solid dosage form, comprising: (a) forming an aqueous slurry of microcrystalline cellulose in the form of a wet cake; (b) forming an aqueous slurry of silicon dioxide having a particle size of from about 1 nm to about 100 .mu.m; (c) separately introducing said microcrystalline slurry and said silicon dioxide slurry separately into a drying apparatus for combination therein, to obtain an excipient comprising a plurality of agglomerated particles of microcrystalline cellulose in intimate association with said silicon dioxide, the amount of silicon dioxide being from about 0.5% to about 20% relative to the amount of microcrystalline cellulose, by weight. (d) mixing an active ingredient with said agglomerated particles; (e) incorporating said mixture obtained in step (d) into a plurality of solid unit doses.

24. The method of claim 23, wherein said silicon dioxide of said aqueous slurry of silicon dioxide has an average primary particle size from about 5 mu to about 40 .mu.m.

25. The method of claim 23, wherein said agglomerated particles have a bulk density from about 0.35 g/ml to about 0.55 g/ml.

26. The method of claim 23, wherein said agglomerated particles have a density from about 0.2 g/ml to about 06 g/ml.

27. The method of claim 23, wherein said agglomerated particles further comprise a member of the group consisting of non-silicon metal oxides, starches, starch derivatives, surfactants, polyalkylene oxides, celluloses, cellulose ethers, cellulose esters and mixtures thereof.

28. The method of claim 23, further comprising wet granulating said mixture obtained in step (c) prior to incorporating said mixture into said solid unit doses.

29. The method of claim 23, wherein said aqueous slurry of microcrystalline cellulose slurry contains from about 0.5% to about 25% microcrystalline cellulose by weight in the form of a wet cake.

30. The method of claim 23, wherein said aqueous slurry of microcrystalline cellulose contains from about 15% to about 20% microcrystalline cellulose in the form of a wet cake.

31. The method of claim 23, wherein said aqueous slurry of microcrystalline cellulose contains from about 17% to about 19% microcrystalline cellulose in the form of a wet cake.

32. The method of claim 23, wherein said silicon dioxide is colloidal silicon dioxide.

33. The method of claim 23, wherein said silicon dioxide has a surface area from about 10 m.sup.2 /g to about 500 m.sup.2 /g.

34. The method of claim 23, wherein said silicon dioxide has a surface area from about 50 m.sup.2 /g to about 500 m.sup.2 /g.

35. The method of claim 23, wherein said silicon dioxide has a surface area from about 175 m.sup.2 /g to about 350 m.sup.2 /g.

36. The method of claim 23, wherein said silicon dioxide is present in an amount from about 0.5% to about 10% by weight, based on the weight of said microcrystalline cellulose.

37. The method of claim 23, wherein said silicon dioxide is present in an amount from about 1.25% to about 5% by weight, based on the weight of said microcrystalline cellulose.

38. The method of claim 23, wherein said agglomerated particles have an average particle size from about 10 .mu.m to about 1,000 .mu.m.

39. The method of claim 23, wherein said agglomerated particles have an average particle size from about 10 .mu.m to about 500 .mu.m.

40. The method of claim 23, wherein said agglomerated particles have an average particle size from about 30 .mu.m to about 250 .mu.m.

41. The method of claim 23, wherein said agglomerated particles have a moisture content of from about 0.5 to about 15%.

42. The method of claim 23, wherein said agglomerated particles have a moisture content of from about 2.5 to about 6%.

43. The method of claim 23, wherein said agglomerated particles have a moisture content of from about 3.0 to about 5%.

44. The method of claim 23, wherein said drying of said aqueous slurry of microcrystalline cellulose and said aqueous slurry of silicon dioxide is accomplished by a method selected from the group consisting of spray drying, flash drying, ring drying, micron drying, tray drying, vacuum drying, radio-frequency drying and microwave drying.

45. The method of claim 23, wherein said drying of said aqueous slurry of microcrystalline cellulose and said aqueous slurry of silicon dioxide is accomplished by spray drying.
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