US5490990A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Production of solid pharmaceutical depot forms
Assignee: BASF SE
•
Filing: 1993-06-21
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Granted: 1996-02-13
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Expires: 2013-06-21
Abstract
Abstract A process for the production of solid pharmaceutical depot forms by application of a reconstituted aqueous dispersion of a pharmaceutically acceptable binder to a core which contains active substance or by wet granulation of the pharmaceutical active substance with such a binder dispersion or by direct tableting of an active substance with the redispersible binder powder, wherein the binder has been obtained by emulsion polymerization and subsequent spray drying of the resulting aqueous dispersion with a water-soluble pharmaceutically acceptable spraying aid with a glass transition temperature of at least 60° C. and with or without a pharmaceutically acceptable antiblocking agent.
Inventors
- 👤 Sven Grabowski
- 👤 Astrid Kah-Helbig
- 👤 Axel Sanner
- 👤 Kurt Wendel
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 20:08
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/205; A61K9/2059; A61K9/2027; A61K9/2009; A61K9/2054
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
181 words
A process for the production of solid pharmaceutical depot forms by application of an aqueous dispersion, reconstituted by the addition of water to a pharmaceutically acceptable binder, to a core which contains active substance, wherein the binder is prepared by emulsion polymerization of an ethylenically unsaturated compound selected from the group consisting of C 1-18 alkyl(meth)acrylates, hydroxyalkyl(meth)acrylates, vinyl esters, vinyl lactams, mono- or dicarboxylic acids, monoesters or monoamides of these acids, N-vinylimidazole, N-vinylimidazoline, N-vinylimidazolidine, N-vinylpyridine, monoalkyl- or dialkylaminoalkyl esters or monoalkyl- or dialkylaminoalkylamides of polymerizable carboxylic acids, acrylamidoalkylsulfonic acids, trimethylammonioethyl methacrylate chloride and methylol(meth)acrylamides, which produces a water insoluble polymer, and subsequent spray drying of the resulting aqueous polymer dispersion with 5-50% by weight of a water-soluble pharmaceutically acceptable spraying aid selected from the group consisting of cellulose derivatives, polyvinylpyrrolidones, copolymers of N-vinylpyrrolidone and vinylacetate, starch derivatives and polyvinylalcohols with a glass transition temperature of at least 60° C. and 0-50% by weight, based on the amount of binder, of a pharmaceutically acceptable antiblocking agent, the solid pharmaceutical depot forms exhibiting undiminished release properties of the active substance of the core.
Claim 2
Dependent Claim
181 words
A process for the production of solid pharmaceutical depot forms by application of an aqueous dispersion, reconstituted by the addition of water to a pharmaceutically acceptable binder, to a core which contains active substance, wherein the binder is prepared by emulsion polymerization of an ethylenically unsaturated compound selected from the group consisting of C 1-18 alkyl(meth)acrylates, hydroxyalkyl(meth)acrylates, vinyl esters, vinyl lactams, mono- or dicarboxylic acids, monoesters or monoamides of these acids, N-vinylimidazole, N-vinylimidazoline, N-vinylimidazolidine, N-vinylpyridine, monoalkyl- or dialkylaminoalkyl esters or monoalkyl- or dialkylaminoalkylamides of polymerizable carboxylic acids, acrylamidoalkylsulfonic acids, trimethylammonioethyl methacrylate chloride and methylol(meth)acrylamides, which produces a water insoluble polymer, and subsequent spray drying of the resulting aqueous polymer dispersion with 5-50% by weight of a water-soluble pharmaceutically acceptable spraying aid selected from the group consisting of cellulose derivatives, polyvinylpyrrolidones, copolymers of N-vinylpyrrolidone and vinylacetate, starch derivatives and polyvinylalcohols with a glass transition temperature of at least 60° C. and 0-50% by weight, based on the amount of binder, of a pharmaceutically acceptable antiblocking agent, the solid pharmaceutical depot forms exhibiting undiminished release properties of the active substance of the core.
Claim 3
Dependent Claim
180 words
A process for the production of solid pharmaceutical depot forms by wet granulation of a pharmaceutically active substance, with a aqueous binder dispersion, which has been reconstituted by the addition of water to a binder, wherein the binder is prepared by emulsion polymerization of an ethylenically unsaturated compound selected from the group consisting of C 1-18 alkyl(meth)acrylates, hydroxyalkyl(meth) acrylates, vinyl esters, vinyl lactams, mono- or dicarboxylic acids, monoesters or monoamides of these acids, N-vinylimidazole, N-vinylimidazoline, N-vinylimidazolidine, N-vinylpyridine, monoalkyl- or dialkylaminoalkyl esters or monoalkyl- or dialkylaminoalkylamides of polymerizable carboxylic acids, acrylamidoalkylsulfonic acids, trimethylammonioethyl methacrylate chloride and methylol(meth)acrylamides, which produces a water insoluble polymer, and subsequent spray drying of the resulting aqueous polymer dispersion with 5-50% by weight of a water-soluble pharmaceutically acceptable spraying aid selected from the group consisting of cellulose derivatives, polyvinylpyrrolidones, copolymers of N-vinylpyrrolidone and vinylacetate, starch derivatives and polyvinylalcohols with a glass transition temperature of at least 60° C. and 0-50% by weight, based on the amount of binder, of a pharmaceutically acceptable antiblocking agent, the solid pharmaceutical depot forms exhibiting undiminished release properties of the active substance.
Claim 4
Dependent Claim
180 words
A process for the production of solid pharmaceutical depot forms by wet granulation of a pharmaceutically active substance, with a aqueous binder dispersion, which has been reconstituted by the addition of water to a binder, wherein the binder is prepared by emulsion polymerization of an ethylenically unsaturated compound selected from the group consisting of C 1-18 alkyl(meth)acrylates, hydroxyalkyl(meth) acrylates, vinyl esters, vinyl lactams, mono- or dicarboxylic acids, monoesters or monoamides of these acids, N-vinylimidazole, N-vinylimidazoline, N-vinylimidazolidine, N-vinylpyridine, monoalkyl- or dialkylaminoalkyl esters or monoalkyl- or dialkylaminoalkylamides of polymerizable carboxylic acids, acrylamidoalkylsulfonic acids, trimethylammonioethyl methacrylate chloride and methylol(meth)acrylamides, which produces a water insoluble polymer, and subsequent spray drying of the resulting aqueous polymer dispersion with 5-50% by weight of a water-soluble pharmaceutically acceptable spraying aid selected from the group consisting of cellulose derivatives, polyvinylpyrrolidones, copolymers of N-vinylpyrrolidone and vinylacetate, starch derivatives and polyvinylalcohols with a glass transition temperature of at least 60° C. and 0-50% by weight, based on the amount of binder, of a pharmaceutically acceptable antiblocking agent, the solid pharmaceutical depot forms exhibiting undiminished release properties of the active substance.
Claim 5
Dependent Claim
175 words
A process for the production of drug tablets by direct tabletting of an active substance and 5-99.9% by weight of a conventional pharmaceutical aid, wherein 5-95% by weight, based on the tablet, of a binder powder is prepared by emulsion polymerization of an ethylenically unsaturated compound selected from the group consisting of C 1-18 alkyl(meth)acrylates, hydroxyalkyl(meth)acrylates, vinyl esters, vinyl lactams, mono- or dicarboxylic acids, monoesters or monoamides of these acids, N-vinylimidazole, N-vinylimidazoline, N-vinylimidazolidine, N-vinylpyridine, monoalkyl- or dialkylaminoalkyl esters or monoalkyl- or dialkylaminoalkylamides of polymerizable carboxylic acids, acrylamidoalkylsulfonic acids, trimethylammonioethyl methacrylate chloride and methylol(meth)acrylamides, which produces a water insoluble polymer, and subsequent spray drying of the resulting aqueous polymer dispersion with 5-50% by weight of a water-soluble pharmaceutically acceptable spraying aid selected from the group consisting of cellulose derivatives, polyvinylpyrrolidones, copolymers of N-vinylpyrrolidone and vinylacetate, starch derivatives and polyvinylalcohols with a glass transition temperature of at least 60° C. and 0-50% by weight, based on the amount of binder, of a pharmaceutically acceptable antiblocking agent, the solid tablets exhibiting undiminished release properties of the active substance.
Claim 6
Dependent Claim
175 words
A process for the production of drug tablets by direct tabletting of an active substance and 5-99.9% by weight of a conventional pharmaceutical aid, wherein 5-95% by weight, based on the tablet, of a binder powder is prepared by emulsion polymerization of an ethylenically unsaturated compound selected from the group consisting of C 1-18 alkyl(meth)acrylates, hydroxyalkyl(meth)acrylates, vinyl esters, vinyl lactams, mono- or dicarboxylic acids, monoesters or monoamides of these acids, N-vinylimidazole, N-vinylimidazoline, N-vinylimidazolidine, N-vinylpyridine, monoalkyl- or dialkylaminoalkyl esters or monoalkyl- or dialkylaminoalkylamides of polymerizable carboxylic acids, acrylamidoalkylsulfonic acids, trimethylammonioethyl methacrylate chloride and methylol(meth)acrylamides, which produces a water insoluble polymer, and subsequent spray drying of the resulting aqueous polymer dispersion with 5-50% by weight of a water-soluble pharmaceutically acceptable spraying aid selected from the group consisting of cellulose derivatives, polyvinylpyrrolidones, copolymers of N-vinylpyrrolidone and vinylacetate, starch derivatives and polyvinylalcohols with a glass transition temperature of at least 60° C. and 0-50% by weight, based on the amount of binder, of a pharmaceutically acceptable antiblocking agent, the solid tablets exhibiting undiminished release properties of the active substance.
Claim 7
Dependent Claim
39 words
The process of claim 1, wherein from 5-50% by weight of antiblocking agent selected from the group consisting of colloidal silicon dioxide, talc, calcium, magnesium or sodium carbonate, tricalcium orthophosphate, magnesium orthophosphate, microcrystalline cellulose and magnesium stearate is present.
Claim 8
Dependent Claim
39 words
The process of claim 2, wherein from 5-50% by weight of antiblocking agent selected from the group consisting of colloidal silicon dioxide, talc, calcium, magnesium or sodium carbonate, tricalcium orthophosphate, magnesium orthophosphate, microcrystalline cellulose and magnesium stearate is present.
Claim 9
Dependent Claim
39 words
The process of claim 3, wherein from 5-50% by weight of antiblocking agent selected from the group consisting of colloidal silicon dioxide, talc, calcium, magnesium or sodium carbonate, tricalcium orthophosphate, magnesium orthophosphate, microcrystalline cellulose and magnesium stearate is present.
Claim 10
Dependent Claim
27 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 1, wherein the emulsion polymer employed as binder is comprised of vinyl acetate.
Claim 11
Dependent Claim
27 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 2, wherein the emulsion polymer employed as binder is comprised of vinyl acetate.
Claim 12
Dependent Claim
27 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 3, wherein the emulsion polymer employed as binder is comprised of vinyl acetate.
Claim 13
Dependent Claim
36 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 1, wherein the emulsion polymer employed as binder is comprised of ethyl acrylate and methyl methacrylate in the ratio 2:1 by weight.
Claim 14
Dependent Claim
36 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 2, wherein the emulsion polymer employed as binder is comprised of ethyl acrylate and methyl methacrylate in the ratio 2:1 by weight.
Claim 15
Dependent Claim
36 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 3, wherein the emulsion polymer employed as binder is comprised of ethyl acrylate and methyl methacrylate in the ratio 2:1 by weight.
Claim 16
Dependent Claim
39 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 1, wherein the spray-dried emulsion polymer employed as binder contains a water-soluble N-vinylpyrrolidone polymer which contains 0-50% by weight of vinyl acetate as copolymerized units.
Claim 17
Dependent Claim
39 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 2, wherein the spray-dried emulsion polymer employed as binder contains a water-soluble N-vinylpyrrolidone polymer which contains 0-50% by weight of vinyl acetate as copolymerized units.
Claim 18
Dependent Claim
39 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 3, wherein the spray-dried emulsion polymer employed as binder contains a water-soluble N-vinylpyrrolidone polymer which contains 0-50% by weight of vinyl acetate as copolymerized units.
Claim 19
Dependent Claim
24 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 1, wherein a water-soluble polysaccharide is employed as spraying aid.
Claim 20
Dependent Claim
24 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 2, wherein a water-soluble polysaccharide is employed as spraying aid.
Claim 21
Dependent Claim
24 words
A process for the production of solid pharmaceutical depot forms as claimed in claim 3, wherein a water-soluble polysaccharide is employed as spraying aid.
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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) | 1999-02-12 | 1999-08-14 | 2000-02-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2003-02-12 | 2003-08-14 | 2004-02-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2007-02-12 | 2007-08-14 | 2008-02-13 | $7700.00 | Window Closed / Lapsed |