Patent EP0270305A2 successfully refreshed from Google Patents.
EP0270305A2
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EP
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Spheroids
Assignee: Euro Celtique SA
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Filing: 1987-11-26
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Granted: —
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Expires: 2007-11-26
Abstract
Abstract A controlled release pharmaceutical composition comprising a plurality of film coated spheroids, the film coated spheroids comprising a 3-alkylxanthine, a non-water soluble spheronising agent and between 4% and 9% (by weight) water, wherein the in-vitro dissolution rate of the 3-alkylxanthine from the film coated spheroids, when measured by the USP Paddle Method at 100rpm in 900ml aqueous buffer (pH 6.5 at 37°C) is between 7.5% and 25.0% (by wt) release after 1 hour, between 22.5% and 45.0% (by wt) release after 2 hours, between 40.0% and 60.0% (by wt) release after 3 hours, between 50.0% and 75.0% (by wt) release after 4 hours, between 70.0% and 92.5% (by wt) release after 6 hours, and between 80.0% and 100.0% (by wt) release after 8 hours. Preferably the water content is between 4% and 8%, especially between 4% and 7% (by wt) of the film coated spheroid formulation. The preferred 3-alkylxanthine is theophylline (anhydrous or hydrate), whilst the preferred spheronising agent is microcrystalline cellulose.
Inventors
- 👤 Stewart Thomas Leslie
- 👤 Sandra Therese Antoinette Malkowska
- 👤 Joanne Marchant
- 👤 Philip John Neale
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-04 03:17
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1652; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/519; A61K31/52; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5036; A61K9/5042; A61K9/5047
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
124 words
A controlled release pharmaceutical composition comprising a plurality of film coated spheroids, the film coated spheroids comprising a 3-alkylxanthine, a non-water soluble spheronising agent and between 4% and 9% (by weight) water, wherein the in-vitro dissolution rate of the 3-alkylxanthine from the film coated spheroids, when measured by the USP Paddle Method at 100rpm in 900ml aqueous buffer (pH 6.5) at 37°C is between 7.5% and 25.0% (by wt) release after 1 hour, between 22.5% and 45.0% (by wt) release after 2 hours, between 40.0% and 60.0% (by wt) release after 3 hours, between 50.0% and 75.0% (by wt) release after 4 hours, between 70.0% and 92.5% (by wt) release after 6 hours, and between 80.0% and 100.0% (by wt) release after 8 hours.
Claim 2
Dependent Claim
124 words
A controlled release pharmaceutical composition comprising a plurality of film coated spheroids, the film coated spheroids comprising a 3-alkylxanthine, a non-water soluble spheronising agent and between 4% and 9% (by weight) water, wherein the in-vitro dissolution rate of the 3-alkylxanthine from the film coated spheroids, when measured by the USP Paddle Method at 100rpm in 900ml aqueous buffer (pH 6.5) at 37°C is between 7.5% and 25.0% (by wt) release after 1 hour, between 22.5% and 45.0% (by wt) release after 2 hours, between 40.0% and 60.0% (by wt) release after 3 hours, between 50.0% and 75.0% (by wt) release after 4 hours, between 70.0% and 92.5% (by wt) release after 6 hours, and between 80.0% and 100.0% (by wt) release after 8 hours.
Claim 3
Dependent Claim
92 words
A composition according to claim 1 characterised in that the film coated spheroids contain between 4% and 8% (by weight) water and the in vitro dissolution rate of the 3-alkylxanthine is between 8.0% and 22.5% (by wt) release after 1 hour, between 25% and 42.5% (by wt) release after 2 hours, between 42.5% and 60% (by wt) release after 3 hours, between 52.5% and 72.5% (by wt) release after 4 hours, between 72.5% and 92.5% (by wt) release after 6 hours, and between 82.5% and 100% (by wt) release after 8 hours.
Claim 4
Dependent Claim
92 words
A composition according to claim 2 characterised in that the film coated spheroids contain between 4% and 7% (by weight) water and the in vitro dissolution rate of the 3-alkylxanthine is between 8% and 20% (by wt) release after 1 hour, between 25% and 40% (by wt) release after 2 hours, between 42.5% and 57.5% (by wt) release after 3 hours, between 55% and 70% (by wt) release after 4 hours, between 75% and 90% (by wt) release after 6 hours, and between 82.5% and 100% (by wt) release after 8 hours.
Claim 5
Dependent Claim
37 words
A composition according to any one of claims 1 to 3 characterised in that the 3-alkylxanthine comprises a 1,3-dimethylxanthine, or a salt or derivative of a 1,3-dimethylxanthine, especially acepifylline, bamifylline, bufylline, diprophylline, etamiphylline, etofylline, proxyphylline or theophylline.
Claim 6
Dependent Claim
27 words
A composition according to claim 4 characterised in that the 3-alkylxanthine comprises theophylline, aminophylline, choline theophyllinate, theophylline monoethanolamine, theophylline sodium glycinate or theophylline calcium salicylate, especially theophylline.
Claim 7
Dependent Claim
28 words
A composition according to claim 5 characterised in that the film coated spheroids comprise between 40% and 75% (by weight), preferably between 45% and 70% (by weight), theophylline.
Claim 8
Dependent Claim
20 words
A composition according to any one of claims 1 to 6 characterised in that the spheronising agent comprises microcrystalline cellulose.
Claim 9
Dependent Claim
36 words
A composition according to any one of claims 1 to 7 characterised in that the film coated spheroids comprise between 20% and 50%, (by weight) especially between 25% and 45% (by weight), of the spheronising agent.
Claim 10
Dependent Claim
197 words
A process for the preparation of a controlled release pharmaceutical composition according to claim 1 comprising (a) granulating a mixture comprising a 3-alkylxanthine, a non-water soluble spheronising agent and water, (b) extruding the granulated mixture to give an extrudate, (c) spheronising the extrudate until spheroids are formed, (d) drying the spheroids, and (e) coating the spheroids with a film coat that permits release of the 3-alkylxanthine at a controlled rate in an aqueous medium, to give film coated spheroids, wherein the spheroids are dried in step (d) above to such an extent that the film coated spheroids contain between 4% and 9% (by weight) water and the in-vitro dissolution rate of the 3-alkylxanthine from the film coated spheroids, when measured by the USP Paddle Method at 100rpm on 900ml aqueous buffer (pH 6.5) at 37°C is betweem 7.5% and 25.0% (by wt) release after 1 hour. between 22.5% and 45.0% (by wt) release after 2 hours, between 40.0% and 60.0% (by wt) release after 3 hours, between 50.0% and 75.0% (by wt) release after 4 hours, between 70.0% and 92.5% (by wt) release after 6 hours, and between 80.0% and 100% (by wt) release after 8 hours.
References Cited (Backward Citations)
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