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EP0231826A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Theophylline sustained release tablet

Assignee: Farvalsa AG
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Filing: 1987-01-23
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Granted: —
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Expires: 2007-01-23
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Abstract

Abstract Compressed tablets from which theophylline is released at a steady rate with twelve hour dosing intervals are disclosed. The tablets contain 43 to 50 weight percent theophylline; 10 to 20 weight percent water insoluble poly­mer; 10 to l5 weight percent of a polymer selected from the group consisting of water soluble polymers and hydrophilic gel formers which swell in water; and 5 to l5 weight percent acid insoluble polymer having carboxylic groups. The tablet may additionally contain 5 to 9 weight percent hydrophobic lubricant. A preferred composition contains: 43 to 50 weight percent theophylline; 10 to 20 weight percent polyvi­nyl acetate; 10 to l5 weight percent polyvinylpyrrolidine; 5 to l5 weight percent cellulose acetate phthalate and option­ally contains 5 to 7 weight percent of a lubricant mixture containing stearic acid, magnesium stearate and talc.

Inventors

  • 👤 Aracelis M. Avenida Universitaria Ortega

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-06 15:40
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2072; A61K9/2077; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/519; A61K31/52; A61K9/2004; A61K9/2022; A61K9/2027; A61K9/205; A61K9/2054

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 59 words
A pharmaceutical tablet comprising: a) 43 to 50 weight percent theophylline; b) l0 to 20 weight percent water insoluble poly­mer; c) l0 to l5 weight percent of a polymer selected from the group consisting of water soluble poly­mers and hydrophilic gel formers which swell in water; and d) 5 to l5 weight percent acid insoluble polymer having carboxylic groups.
Claim 2
Dependent Claim 59 words
A pharmaceutical tablet comprising: a) 43 to 50 weight percent theophylline; b) l0 to 20 weight percent water insoluble poly­mer; c) l0 to l5 weight percent of a polymer selected from the group consisting of water soluble poly­mers and hydrophilic gel formers which swell in water; and d) 5 to l5 weight percent acid insoluble polymer having carboxylic groups.
Claim 3
Dependent Claim 38 words
The pharmaceutical tablet of Claim l wherein the water insoluble polymer is selected from the group con­sisting of polyvinyl acetate, polyvinyl alcohol, vinyl chlo­ride/vinyl acetate copolymers, acrylate and methacrylate polymers and copolymers, and ethyl and methyl methacrylate copolymers.
Claim 4
Dependent Claim 12 words
The pharmaceutical tablet of Claim l wherein the polymer is polyvinyl acetate.
Claim 5
Dependent Claim 27 words
The pharmaceutical tablet of Claim l wherein the water soluble polymer or gel former is selected from the group consisting of polyvinylpyrrolidone, hydroxypropylcellulose, methylcellulose and sodium carboxymethylcellulose.
Claim 6
Dependent Claim 13 words
The pharmaceutical tablet of Claim l wherein the hydrophilic gel former is polyvinylpyrrolidone.
Claim 7
Dependent Claim 32 words
The pharmaceutical tablet of Claim l wherein the acid insoluble polymer is selected from the group con­sisting of cellulose acetate phthalate, hydroxypropylmethyl cellulose phthalate and esters of acrylic and methacrylic acid copolymers.
Claim 8
Dependent Claim 15 words
The pharmaceutical tablet of Claim l wherein the acid insoluble polymer is cellulose acetate phthalate.
Claim 9
Dependent Claim 15 words
The pharmaceutical tablet of Claim l further comprising 5 to 9 weight percent hydrophobic lubricant.
Claim 10
Dependent Claim 29 words
The pharmaceutical tablet of Claim 8 wherein the lubricant is selected from the group consisting of talc, fatty acids, salts of fatty acids, mineral oil and hydroge­nated vegetable oils.
Claim 11
Dependent Claim 14 words
l0. The pharmaceutical tablet of Claim 8 wherein the fatty acid is stearic acid.
Claim 12
Dependent Claim 26 words
The pharmaceutical tablet of Claim 9 wherein the lubricant comprises: a) 3 parts stearic acid; b) 0.5 part magnesium stearate; and c) l.0 part talc USP.
Claim 13
Dependent Claim 39 words
The pharmaceutical tablet of Claim l comprising: a) 43 to 50 weight percent theophylline; b) l0 to 20 weight percent polyvinyl acetate; c) l0 to l5 weight percent polyvinylpyrrolidine; and d) 5 to l5 weight percent cellulose acetate phthalate.
Claim 14
Dependent Claim 36 words
The pharmaceutical tablet of Claim l compris­ing: a) 50 weight percent theophylline; b) l5 weight percent polyvinylacetate; c) l5 weight percent polyvinyl pyrrolidone: d) l5 weight percent cellulose acetate phthalate; and e) 5 weight percent lubricant.
Claim 15
Independent Claim 91 words
A method of maintaining relatively uniform blood levels of theophylline in a host comprising a) formulating a theophylline tablet containing (i) 43 to 50 weight percent theophyl­line; (ii) l0 to 20 weight percent water in­soluble polymer; (iii) l0 to l5 weight percent of a poly­mer selected from the group consisting of water soluble polymers and hydro­philic gel formers which swell in water; and (iv) 5 to l5 weight percent acid insol­uble polymer having carboxylic groups. b) orally administering one or more of said tab­lets to a host at twelve hour intervals.
Claim 16
Independent Claim 91 words
A method of maintaining relatively uniform blood levels of theophylline in a host comprising a) formulating a theophylline tablet containing (i) 43 to 50 weight percent theophyl­line; (ii) l0 to 20 weight percent water in­soluble polymer; (iii) l0 to l5 weight percent of a poly­mer selected from the group consisting of water soluble polymers and hydro­philic gel formers which swell in water; and (iv) 5 to l5 weight percent acid insol­uble polymer having carboxylic groups. b) orally administering one or more of said tab­lets to a host at twelve hour intervals.
Claim 17
Independent Claim 74 words
The method of Claim l4 wherein the tablet is formulated by: a) wet granulating a mixture of the theophylline and the acid insoluble polymer with an alcoholic solution containing part of the hydrophilic gel former or water solu­ble polymer; b) mixing the remaining hydrophilic gel former or water soluble polymer with the water insoluble polymer; c) mixing the compositions resulting from (a) and (b); and d) comprising the mixture resulting from (d) into tablets.
Claim 18
Independent Claim 21 words
The method of Claim l5 wherein 5 to 9 weight percent hydrophobic lubricant is added to the mixture prior to compression.

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