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Method for preparing a powdered particulate composition

Assignee: Organon NV
•
Filing: 1990-12-27
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Granted: 1993-08-24
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Expires: 2010-12-27
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Abstract

Abstract Disclosed are powdered particulates or granules useful for the preparation of certain psychotropic compounds (e.g. mianserin are mirtazepine). The resulting suspensions and relatively tasteless, do not have a local anaesthetic effect and are easy to suspend. The granules contain the psychotropic compound, a cellulose derivative, polymer, and a filler.

Inventors

  • 👤 Gerrit B. M. Beuving
  • 👤 Henrik de Nijs

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 19:20
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/55; A61K31/435; A61K31/44; A61K31/445; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1635; A61K9/1652; A61P; A61P25/00; A61P25/18

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 181 words
A process of manufacturing a powdered particulate comprising: dissolving (a) 1-5 parts by weight of the free base of a compound of the formula: ##STR2## in which X=carbon or nitrogen, Y=carbon or nitrogen, R 1 and R 2 are each independently selected from H, OH, O-alkyl (1-4 C atoms), alkyl (1-4 C atoms) and a halogen, R 3 =H or alkyl (1-4 C atoms), and the broken line indicates an extra bond that may be present when Y is a carbon atom, (b) 0.3-3 parts by weight of a cellulose derivative that is soluble in water and organic solvents, and (c) 4-20 parts by weight of a water insoluble pharmaceutically acceptable polymer in an organic solvent; and mixing with the solution formed (d) 40-250 parts by weight of a pharmaceutical filler distinct from said cellulose derivative and also distinct from said water insoluble pharmaceutically acceptable polymer and granulating said mixture, wherein the amount of organic solvent used is an amount of solvent effective for dissolving the compound, cellulose derivative and polymer and for granulating the solution formed with the pharmaceutical filler.
Claim 2
Dependent Claim 181 words
A process of manufacturing a powdered particulate comprising: dissolving (a) 1-5 parts by weight of the free base of a compound of the formula: ##STR2## in which X=carbon or nitrogen, Y=carbon or nitrogen, R 1 and R 2 are each independently selected from H, OH, O-alkyl (1-4 C atoms), alkyl (1-4 C atoms) and a halogen, R 3 =H or alkyl (1-4 C atoms), and the broken line indicates an extra bond that may be present when Y is a carbon atom, (b) 0.3-3 parts by weight of a cellulose derivative that is soluble in water and organic solvents, and (c) 4-20 parts by weight of a water insoluble pharmaceutically acceptable polymer in an organic solvent; and mixing with the solution formed (d) 40-250 parts by weight of a pharmaceutical filler distinct from said cellulose derivative and also distinct from said water insoluble pharmaceutically acceptable polymer and granulating said mixture, wherein the amount of organic solvent used is an amount of solvent effective for dissolving the compound, cellulose derivative and polymer and for granulating the solution formed with the pharmaceutical filler.
Claim 3
Dependent Claim 25 words
A process of manufacturing according to claim 1 further comprising screening the granules obtained to select a particle size of between 100 and 300 μm.
Claim 4
Dependent Claim 25 words
A process of manufacturing according to claim 1 further comprising screening the granules obtained to select a particle size of between 50 and 500 μm.
Claim 5
Dependent Claim 24 words
The process of manufacturing according to claim 1, wherein an acrylate polymer insoluble in water is used as the water insoluble pharmaceutically acceptable polymer.
Claim 6
Dependent Claim 14 words
The process of manufacturing according to claim 1, wherein the cellulose derivative is hydroxypropylcellulose.
Claim 7
Dependent Claim 15 words
The process of manufacturing according to claim 1, wherein mannitol is used as the filler.
Claim 8
Dependent Claim 61 words
The process of manufacturing according to claim 1, wherein the resulting powdered particulate comprises: a) 2-3 parts by weight of said free base, b) 8-15 parts by weight of an acrylic resin, comprising copolymers of acrylic and methacrylic acid esters, that is slightly permeable to water, c) 0.8-1.2 parts by weight of hydroxypropylcellulose, and d) 80-150 parts by weight of mannitol.
Claim 9
Dependent Claim 14 words
The process of manufacturing according to claim 1, wherein the free base is mianserin.

References Cited (Backward Citations)

US4128641A Cited
US4284559A Cited
US4447437A Cited
US4623588A Cited
US4870060A Cited
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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) 1996-08-23 1997-02-22 1997-08-24 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2000-08-23 2001-02-22 2001-08-24 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2004-08-23 2005-02-22 2005-08-24 $7700.00 Window Closed / Lapsed

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