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Details for Patent: 6,395,303

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Details for Patent: 6,395,303

Title: Process for preparing a directly compressible solid dosage form containing microcrystalline cellulose
Abstract:The present invention provides an improved process for the preparation of a agglomerated solid dosage form, comprising preparing an aqueous slurry of microcrystalline cellulose and a microcrystalline cellulose compressibility augmenting agent and an active agent. The augmenting agent is capable of physically restricting the proximity of the interface between adjacent cellulose surfaces and/or inhibiting interactions between adjacent cellulose surfaces, for example, via the creation of a hydrophobic boundary at cellulose surfaces. The resulting aqueous slurry is dried in a manner which inhibits quasi-hornification, thereby obtaining an agglomerated material which is directly compressible into a solid dosage form.
Inventor(s): Staniforth; John N. (Bath, GB), Sherwood; Bob E. (Amenia, NY), Hunter; Edward A. (Glenham, NY), Davidson; Clifford M. (Morganville, NJ)
Assignee: Edward Mendell Co., Inc. (Patterson, NY)
Filing Date:Jun 04, 1997
Application Number:08/868,745
Claims:1. A process for the preparation of an agglomerated material solid dosage form, comprising preparing an aqueous slurry comprising:

(a) microcrystalline cellulose;

(b) a microcrystalline cellulose compressibility augmenting agent comprising a highly polar dye selected from the group consisting of 3,3'-[[1,1'Biphenyl]- 4,4'-diylbis-(azo)]bis[4-amino-1-naphthalenesulfonic acid] disodium salt; disodium salt of 6-hydroxy-5[(2-4-sulfophenyl) azo]-2-naphthalenesulfonic acid); 5-oxo-1-(p- sulfophenyl)-4-[(p-sulfophenyl)azo]-2-pyrazoline-3-carboxylic acid, trisodium salt); disodium salt of 1-p-sulphophenylazo-2-naphthol-6-sulfonic acid); trisodium-2-hydroxy- 1-(4-sulfonato-1-naphthylazo) naphthalene-6, 8-disulfonate); disodium 4,4'-(2,4- dihydroxy-5-hydroxymethyl-3, 3-phenylene bisazo)di(napthalene-1-sulfonate)); tetrasodium 4-acetamido-5-hyroxy-6-[7-sulfonato-4-(4-sulfonatophenylazo)-1- naphthylazo]naphthalene-1,7-disulfonate); disodium 4-hydroxy-3-(4-sulfanato-1- naphythylazo) Naphthalene-1-sulfonate); trisodium 2-hydroxy-1-(4-sulfonato-1- naphthylazo) naphthalene-3, 6-disulfonate) and mixtures thereof which inhibits interactions between cellulose surfaces via the creation of a hydrophobic boundary at cellulose surfaces; and

(c) an active agent; and thereafter drying the resultant aqueous slurry utilizing a spray drying technique to obtain an agglomerated material which is then directly compressed into a tablet.

2. The process of claim 1, wherein said compressibility augmenting agent further comprises a surfactant having an HLB of at least about 10.

3. The process of claim 1, wherein said compressibility augmenting agent further comprises a surfactant having an HLB of at least about 15.

4. The process of claim 1, wherein said compressibility augmenting agent further comprises a surfactant having an HLB of at least about 15 to about 40.

5. The process of claim 4, wherein said surfactant is sodium lauryl sulfate.

6. The process of claim 4, wherein said surfactant is polysorbate.

7. The process of claim 1, wherein said compressibility augmenting agent further comprises a silicon dioxide having an average primary particle size from about 1 nm to about 100 .mu.m.

8. The process of claim 7, wherein said silicon dioxide is included in an amount from about 0.1% to about 20% by weight, based on the weight of microcrystalline cellulose.

9. The process of claim 2, wherein said surfactant is included in an amount from about 0.1% to about 20% by weight, based on the weight of microcrystalline cellulose.

10. The process of claim 8, wherein said silicon dioxide is colloidal silicon dioxide.

11. The process of claim 1, further comprising adding a sustained release carrier into the aqueous slurry, and drying the aqueous slurry in such a manner as to obtain agglomerated sustained release particles.

12. The process of claim 11, wherein said sustained release carrier is selected from the group consisting of an alkyl cellulose, an acrylic polymer or copolymer, a cellulose ether, a cellulose ester, and mixtures thereof.

13. The process of claim 11, wherein said sustained release carrier is selected from natural or synthetic gums.

14. The process of claim 1, further comprising adding a film forming agent into the aqueous slurry, and drying the aqueous slurry in such a manner as to obtain agglomerated particles having a film coating.

15. The process of claim 1, further comprising compressing the resultant granulate into tablets.

16. The process of claim 11, further comprising compressing the resultant granulate into tablets.

17. The process of claim 14, further comprising compressing the resultant granulate into tablets.

18. The process according to claim 1, wherein the solids content of the aqueous slurry is from about 0.5 to about 25%, by weight.

19. The process according to claim 1, wherein the solids content of the aqueous slurry is from about 15 to about 20%, by weight.

20. The process according to claim 11, wherein the solids content of the aqueous slurry is from about 0.5 to about 25%, by weight.

21. The process according to claim 11, wherein the solids content of the aqueous slurry is from about 15 to about 20%, by weight.

22. The process according to claim 14, wherein the solids content of the aqueous slurry is from about 0.5 to about 25%, by weight.

23. The process according to claim 14, wherein the solids content of the aqueous slurry is from about 15 to about 20%, by weight.

24. A product according to claim 1.

25. A product according to claim 11.

26. A product according to claim 14.

27. The process according to claim 11, wherein a further amount of sustained release carrier is admixed with said agglomerated sustained release particles and the resulting mixture is compressed into tablets.

28. The process of claim 27, wherein said mixture is prepared via wet granulation.

29. The process of claim 27, wherein a further amount of active ingredient is also added.

30. The process of claim 11, further comprising compressing said agglomerated sustained release particles into a tablet, and further applying an additional portion of said sustained release carrier as a coating onto said tablet.

31. The process of claim 1, wherein the resultant aqueous slurry is dried in a manner which inhibits quasi-hornification.

32. The process of claim 1, wherein said composition comprises from about 0.1 to about 20% of said highly polar dye based on the weight of microcrystalline cellulose.

33. The process of claim 1, comprising utilizing a spary drying technique to dry the aqueous slurry.

34. The process of claim 1, wherein said highly polar dye has an HLB of at least about 10.

35. The process of claim 1, wherein said highly polar dye has an HLB of at least about 15.

36. The process of claim 1, wherein said highly polar dye has an HLB of at least about 15 to about 40.
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