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Details for Patent: 6,866,867

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Details for Patent: 6,866,867

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: (1) preparing an aqueous slurry of (a) microcrystalline cellulose; (b) a microcrystalline cellulose compressibility augmenting agent which (i) physically restricts the proximity of the interface between adjacent cellulose surfaces; (ii) inhibits interactions between adjacent cellulose surfaces, for example, via the creation of a hydrophobic boundary at cellulose surfaces; or (iii) accomplishes both (i) and (ii) above; and (c) an active agent; (2) thereafter drying the resultant aqueous slurry 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: J. Rettenmaier & Soehne GmbH + Co. KG (Rosenberg, DE)
Filing Date:Dec 13, 2001
Application Number:10/015,538
Claims:1. A process for the preparation of an agglomerated solid dosage form, comprising (1) preparing an aqueous slurry of (a) microcrystalline cellulose; (b) a microcrystalline cellulose compressibility augmenting agent which (I) physically restricts the proximity of the interface between adjacent cellulose surfaces; (ii) inhibits interactions between adjacent cellulose surfaces, via the creation of a hydrophobic boundary at cellulose surfaces; or (iii) accomplishes both (I) and (ii) above; (c) an active agent; and (d) an effective amount of a sustained release carrier; (2) thereafter spray drying the resultant aqueous slurry in a manner which inhibits quasi-hornification, thereby obtaining agglomerated particles which are directly compressible into a solid sustained release matrix which provides release of the active agent over a time period of about 8 to about 24 hours.

2. The process of claim 1, further comprising compressing the agglomerated particles into a tablet.

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

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

5. The process of claim 1, wherein said compressibility augmenting agent is a surfactant having an HLB from about 15 to about 40.

6. The process of claim 5, wherein said compressibility augmenting agent is sodium lauryl sulfate.

7. The process of claim 5, wherein said compressibility augmenting agent is a polysorbate.

8. 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.

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

10. The process of claim 3, wherein said surfactant is included in amount from about 0.1% to about 20% by weight, based on the weight of microcrystalline cellulose.

11. The process of claim 9, wherein said silicon dioxide is colloidal silicon dioxide.

12. The process of claim 1, 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 1, wherein said sustained release carrier is selected from natural or a 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 14, further comprising compressing the agglomerated particles into tablets.

16. The process according to claim 1, wherein the aqueous slurry has a solids content from about 0.5 to about 25%, by weight prior to said spray drying step.

17. The process according to claim 1, wherein the aqueous slurry has a solids content from about 15 to about 20%, by weight prior to said spray drying step.

18. The product according to claim 1.

19. The process of claim 1, further comprising admixing a further amount of sustained release carrier with said agglomerated particles and compressing the resulting mixture into tablets.

20. The process of claim 19, further comprising wet granulating said mixture, and then compressing the resulting mixture into tablets.

21. The process of claim 19, further comprising adding a further amount of active ingredient to the mixture.

22. The process of claim 1, further comprising adding a pharmaceutically acceptable filler to the aqueous slurry.

23. The process of claim 22, wherein the pharmaceutically acceptable filler is selected from the group consisting of a monosaccharide, a dissacharide, a polyhydric alcohol, inorganic phosphates, sulfates, carbonates and mixtures thereof.

24. The process of claim 22, wherein the pharmaceutically acceptable filler is selected from the group consisting of sucrose, dextrose, lactose, xylitol, fructose, sorbitol, calcium phosphate, calcium sulfate, calcium carbonate, "off-shelf" microcrystalline cellulose and mixtures thereof.

25. The process of claim 1, wherein said sustained release carrier includes a release modifying agent that alters the release rate of the active agent from the formulation upon exposure to an aqueous medium.

26. The process of claim 25, wherein said release modifying agent is selected from the group consisting of calcium sulfate, sodium chloride, potassium sulfate, sodium bicarbonate, lithium chloride, tripotassium phosphate, sodium borate, potassium bromide, potassium fluoride, sodium bicarbonate, calcium chloride, magnesium chloride, sodium citrate, sodium acetate, calcium lactate, magnesium sulfate and sodium fluoride.

27. The process of claim 1, wherein the slurry includes a plurality of slurries, each of the plurality of slurries containing one of: a) a microcrystalline cellulose; or ii) a microcrystalline cellulose compressibility augmenting agent.

28. The process of claim 1, wherein said sustained release carrier is selected from the group consisting of a polylactide, a polyglycolide, a poly(lactide-co-glycolide), a polyanhydride, a polyorthoester, polycaprolactones, polyphosphazenes, polysaccharidcs, proteinaceous polymers, soluble derivatives of polysaccharides, soluble derivatives of proteinaceous polymers, polypeptides, polyesters and polyorthoesters.

29. A process for the preparation of a sustained release agglomerated solid dosage form, comprising (1) preparing an aqueous slurry of (a) microcrystalline cellulose; (b) a microcrystalline cellulose compressibility augmenting agent comprising: (i) silicon dioxide; or (ii) a surfactant selected from the group consisting of sodium lauryl sulfate, docusate salts, alkyl carboxylates, acyl lactylates, alkyl ether carboxylates, N-acyl sarcosinates, polyvalent alkyl carbonates, N-acyl glutamates, fatty acids, polypeptide condensates sulfuric acid esters, polyoxyethylene compounds, lecithin, ethoxylated alcohols, ethoxylated esters, ethoxylated amides, polyoxypropylene compounds, propoxylated alcohols, ethoxylated/propoxylated block polymers, propoxylated esters, alkanolamides, amine oxides, fatty acid esters of polyhydric alcohols, ethylene glycol esters, diethylene glycol esters, propylene glycol esters, glycerol esters, polyglycerol fatty acid esters, sorbitan esters, sucrose esters, glucose esters, simethicone, acacia, benzalkonium chloride, cholesterol, emulsifying wax, glycerol monostearate, lanolin alcohols, lecithin, poloxamer, polyoxyethylene and castor oil derivatives; or (iii) 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[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-sulfonatopheylazo)-1-naphthylazo] naphthalene-1,7-disulfonate); disodium 4-hydroxy-3-(4-sulfanato-1-naphythylazo) Naphthalene-1-sulfonate); trisodluin 2-hydroxy-1-(4-sulfonato-1-naphthylazo) naphthalene-3,6-disulfonate) and mixtures thereof; or (iv) a combination of two ro more of (I), (ii) and (iii) above; (c) an active agent; and (d) an effective amount of a sustained release carrier; and (2) thereafter spray drying the resultant aqueous slurry in a manner which inhibits quasi-hornification, thereby obtaining agglomerated particles which are directly compressible into a solid sustained release matrix which provides release of the active agent over a time period of about 8 to about 24 hours.
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