Patent EP0122077A2 successfully refreshed from Google Patents.
EP0122077A2
Expired / Lapsed
EP
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Sustained absorption pharmaceutical composition
Assignee: Elan Corp PLC
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Filing: 1984-03-22
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Granted: —
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Expires: 2004-03-22
Abstract
Abstract A sustained absorption theophylline-containing pellet for oral administrattion comprises a core of theophylline or a pharmacological equivalent thereof and an organic acid embedded in a polymeric material in a multilayer arrangement and an outer membrane which permits release of the theophylline at a controlled rate in an aqueous medium. The pellet has a dissolution rate in vitro in an aqueous medium, which when measured in a basket assembly according to U.S. Pharmacopoeia XX at 37°C and 75 r.p.m., is not more than 15% of the total theophylline after 2 hours of measurement in a buffer solution at pH 7.5. Not more than 35% of the total theophylline is released after a total of 7 hours of measurement and not more than 65% of the total theophylline is released after a total of 13 hours.
Inventors
- 👤 Donald Eugene Panoz
- 👤 Edward James Geoghegan
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-31 11:03
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/519; A61K31/52; A61K9/00; A61K9/48; A61K9/50; A61K9/5073; A61K9/5078
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
187 words
l. A sustained absorption theophylline-containing pellet for oral administration, characterised in that the pellet has a core of theophylline or a pharmacological equivalent thereof and an organic acid embedded in a polymeric material in a multi-layer arrangement and an outer membrane which permits release of the theophylline at a controlled rate in an aqueous medium, said pellet having a dissolution rate in an aqueous medium which is substantially independent of pH and which when measured in a basket assembly according to U.S. Pharmacopoeia XX at 37°C and 75 r.p.m., in a buffer solution at pH 7.5 has the following characteristics: a) up to 15% of the total theophylline is released during the first two hours of measurement in said assembly; b) between 15 and 35% of the total theophylline is released after a total of 7 hours of measurement in said assembly; c) between 45 and 65% of the total theophylline is released after a total of 13 hours of measurement in said assembly; and d) between 80 and 100% of the total theophylline is released after a total of 24 hours of measurement in said assembly.
Claim 2
Dependent Claim
24 words
A pellet according to Claim 1, wherein the core contains as active ingredient anhydrous theophylline aminophylline, dyphylline, theophylline calcium salicylate or theophylline sodium glucinate.
Claim 3
Dependent Claim
30 words
A pellet according to Claim 1 or 2, wherein the organic acid is citric acid, tartaric acid, succinic acid, malic acid, ascorbic acid or fumaric acid or a mixture thereof.
Claim 4
Dependent Claim
39 words
A pellet according to any one of Claims 1 - 3, characterised in that the polymeric material of the core includes a major proportion of a polymer which is rapidly soluble in water, especially hydroxypropylmethylcellulose, polyvinylpyrrolidone or EUDRAGIT RL.
Claim 5
Dependent Claim
38 words
A pellet according to any one of Claims 1-4, which includes a minor proportion of a water-insoluble polymer, especially methylcellulose, ethylcellulose, propylcellulose, Shellac or EUDRAGIT RS, the water-soluble and water-insoluble polymers being present in a ratio of 9:1.
Claim 6
Dependent Claim
40 words
A pellet according to any preceding claim, wherein the multi-layer arrangement of theophylline, organic acid and polymeric material is built up on an inert core in a manner known per se, the core preferably having between 20 and 120 layers.
Claim 7
Dependent Claim
45 words
A pellet according to any preceding claim, wherein the outer membrane includes a major proportion of a water-insoluble polymer and a minor proportion of a water-soluble polymer, the ratio of water-insoluble to water-soluble polymer being determined by the inherent solubility characteristics of the polymers selected.
Claim 8
Dependent Claim
42 words
A pellet according to any preceding claim characterised in that the outer membrane consists of: ethylcellulose and hydroxypropylcellulose in a ratio of 9:1; EUDRAGIT RS and EUDRAGIT RL in a ratio of 8:2; or Shellac and polyvinylpyrrolidone in a ratio of 9:1.
Claim 9
Dependent Claim
14 words
A capsule or tablet comprising pellets according to any one of the preceding claims.
Claim 10
Dependent Claim
61 words
A process for the production of a pellet according to any one of claims 1-8 comprising forming a core of theophylline or a pharmacological equivalent thereof and an organic acid embedded in a polymeric material in a multi-layer arrangement and enclosing the core in an outer membrane which permits release of the theophylline in the manner set out in claim 1.
References Cited (Backward Citations)
No citation records indexed.
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