US5350584A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Spheronization process using charged resins
Assignee: Merck and Co Inc
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Filing: 1992-06-26
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Granted: 1994-09-27
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Expires: 2012-06-26
Abstract
Abstract The invention comprises a novel process for the spheronization of charged resins. Spherical multiparticlates are produced which range in size from 0.3 mm to 3 mm in diameter. The spherical particle product is microcrystalline-free. The process consists of the steps of mixing followed by wet granulation, spheronization and drying.
Inventors
- 👤 Gregory A. McClelland
- 👤 Gaylen M. Zentner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 20:49
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1682; A61K9/1694; A61K9/1605; A61K9/1629; A61K9/1635
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
102 words
A process for the production of microcrystalline cellulose free multiparticulate comprise a medicament and a charged resin, comprising the steps of: (a) adding a charged resin and an excipient to a mixing vessel; (b) mixing the charged resin and excipient of (a) to obtain a uniform formulation; (c) adding a granulating solution to wet the dry mixture of (b); (d) granulating the mixture until a uniform, wet granulation results; (e) extruding the wet granulation of (d) through a screen to produce strands; (f) spheronizing the strands of (e) to produce microcrystalline cellulose free spherical multiparticulates; (g) collecting and drying the spherical multiparticulates.
Claim 2
Dependent Claim
102 words
A process for the production of microcrystalline cellulose free multiparticulate comprise a medicament and a charged resin, comprising the steps of: (a) adding a charged resin and an excipient to a mixing vessel; (b) mixing the charged resin and excipient of (a) to obtain a uniform formulation; (c) adding a granulating solution to wet the dry mixture of (b); (d) granulating the mixture until a uniform, wet granulation results; (e) extruding the wet granulation of (d) through a screen to produce strands; (f) spheronizing the strands of (e) to produce microcrystalline cellulose free spherical multiparticulates; (g) collecting and drying the spherical multiparticulates.
Claim 3
Dependent Claim
14 words
The process of claim 1 wherein a medicament is added to the dry ingredients.
Claim 4
Dependent Claim
55 words
The process for the production of spherical multiparticulates of claim 1 wherein the charged resin is chosen from the group consisting of sodium polystyrene sulfonate, the chloride salt of cholestyramine resin USP, the acid form of methacrylic acid-divinyl benzene, carboxypolymethylenes prepared from acrylic acid cross-linked with allyl ethers of sucrose or pentaerythritol, and sodium polyacrylate.
Claim 5
Dependent Claim
36 words
The process for the production of spherical multiparticulates of claim 1 wherein the medicament is selected from the group consisting of simvastatin, lovastatin, pravastatin, diltiazem, and the pharmaceutically active salts and crystal forms of these compounds.
Claim 6
Dependent Claim
18 words
The process for the production of spherical multiparticulates of claim 1 wherein the excipients are osmotically active agents.
Claim 7
Dependent Claim
42 words
The process for the production of spherical multiparticulates of claim 5 wherein the osmotically active agents are selected from the group consisting of sodium chloride, sodium dodecyl sulfate, disodium phosphate, monosodium phosphate, citric acid, trisodium citrate, adipic acid, mannitol, sucrose, and lactose.
Claim 8
Dependent Claim
24 words
The process for the production of spherical multiparticulates of claim 1 wherein the dry material is mixed from about 1 to about 60 minutes.
Claim 9
Dependent Claim
20 words
The process for the production of spherical multiparticulates of claim 1 wherein the mixing is accomplished using a planetary mixer.
Claim 10
Dependent Claim
17 words
The process for the production of spherical multiparticulates of claim 1 wherein the granulating solvent is water.
Claim 11
Dependent Claim
22 words
The process for the production of spherical multiparticulates of claim 1 wherein the granulating solvent is a mixture of water and ethanol.
Claim 12
Dependent Claim
29 words
The process for the production of spherical multiparticulates of claim 1 wherein a component of the formulation is dissolved in the granulating solvent prior to the wet granulation step.
Claim 13
Dependent Claim
29 words
The process for the production of spherical multiparticulates of claim 1 wherein the extrusion occurs through a screen having openings of from about 0.5 mm to about 3 mm.
Claim 14
Dependent Claim
31 words
The process for the production of spherical multiparticulates of claim 1 wherein the spheronizer comprises a friction plate which rotates at speeds of from about 500 rpm to about 2000 rpm.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1997-09-26 | 1998-03-28 | 1998-09-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-09-26 | 2002-03-28 | 2002-09-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-09-26 | 2006-03-28 | 2006-09-27 | $7700.00 | Window Closed / Lapsed |