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US4663150A Expired / Lapsed US ⏱️ 0.0 years remaining

Sustained absorption pharmaceutical composition

Assignee: Perrigo Co PLC
•
Filing: 1986-05-21
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Granted: 1987-05-05
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Expires: 2006-05-21
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Abstract

Abstract A sustained absorption theophylline-containing pellet for oral administration comprises 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. 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 E. Panoz
  • 👤 Edward J. Geoghegan

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 12:23
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: 18
Claim 1
Independent Claim 235 words
A sustained absorption active ingredient-containing pellet for oral administration, said pellet comprising a core of about four parts of an active ingredient selected from the group consisting of anhydrous theophylline, aminophylline, dyphylline, theophylline calcium salicylate and theophylline sodium glycinate and about one part of an organic acid selected from the group consisting of citric acid, tartaric acid, succinic acid, malic acid, ascorbic acid and fumaric acid or a mixture thereof embedded in a polymeric material which contains a major proportion of a water-soluble polymer and a membrane of a film-forming polymer or mixture thereof surrounding the core whereby said active ingredient is released at a controlled rate in an aqueous medium and said pellet has 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) from 0 to 15% of said active ingredient is released after two hours of measurement in said assembly; (b) from 15 to 35% of said active ingredient is released after 7 hours of measurement in said assembly; (c) from 45 to 65% of said active ingredient is released after 13 hours of measurement in said assembly; and (d) from 80 to 100% of said active ingredient is released after 24 hours of measurement in said assembly.
Claim 2
Dependent Claim 235 words
A sustained absorption active ingredient-containing pellet for oral administration, said pellet comprising a core of about four parts of an active ingredient selected from the group consisting of anhydrous theophylline, aminophylline, dyphylline, theophylline calcium salicylate and theophylline sodium glycinate and about one part of an organic acid selected from the group consisting of citric acid, tartaric acid, succinic acid, malic acid, ascorbic acid and fumaric acid or a mixture thereof embedded in a polymeric material which contains a major proportion of a water-soluble polymer and a membrane of a film-forming polymer or mixture thereof surrounding the core whereby said active ingredient is released at a controlled rate in an aqueous medium and said pellet has 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) from 0 to 15% of said active ingredient is released after two hours of measurement in said assembly; (b) from 15 to 35% of said active ingredient is released after 7 hours of measurement in said assembly; (c) from 45 to 65% of said active ingredient is released after 13 hours of measurement in said assembly; and (d) from 80 to 100% of said active ingredient is released after 24 hours of measurement in said assembly.
Claim 3
Dependent Claim 25 words
A pellet according to claim 1, wherein theophylline is the active ingredient and said theophylline and organic acid are present in a ratio of 4:1.
Claim 4
Dependent Claim 26 words
A pellet according to claim 1, wherein the polymeric material of the core includes a major proportion of a water-soluble polymer selected from hydroxypropylmethylcellulose and polyvinylpyrrolidone.
Claim 5
Dependent Claim 24 words
A pellet according to claim 1, wherein the polymeric material of the core consists solely of a water-soluble polymer selected from hydroxypropylmethylcellulose and polyvinylpyrrolidone.
Claim 6
Dependent Claim 32 words
A pellet according to claim 3, wherein the polymeric material of the core includes a minor proportion of a water-insoluble polymer selected from the group consisting of methylcellulose, ethylcellulose, propylcellulose and shellac.
Claim 7
Dependent Claim 20 words
A pellet according to claim 5, wherein the water-soluble polymer and water-insoluble polymer are present in a ratio of 9:1.
Claim 8
Dependent Claim 22 words
A pellet according to claim 1, wherein said active ingredient, organic acid and polymeric material is built up on an inert core.
Claim 9
Dependent Claim 24 words
A pellet according to claim 7, wherein the inert core is a non-pareil seed having an average diameter of from 0.3 to 0.7 mm.
Claim 10
Dependent Claim 28 words
A pellet according to claim 1, wherein the membrane includes a major proportion of a water-insoluble polymer selected from the group consisting of methylcellulose, ethylcellulose, propylcellulose and shellac.
Claim 11
Dependent Claim 35 words
A pellet according to claim 9, wherein the membrane includes 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 12
Dependent Claim 19 words
A pellet according to claim 10, wherein the membrane consists of ethylcellulose and hydroxypropylmethylcellulose in a ratio of 9:1.
Claim 13
Dependent Claim 45 words
A pellet according to claim 10, wherein the membrane consists of a copolymer of acrylic and methacrylic acid esters which is slightly permeable to water and a copolymer of acrylic and methacrylic acid esters which is freely permeable to water in a ratio of 8:2.
Claim 14
Dependent Claim 19 words
A pellet according to claim 10, wherein the membrane consists of shellac and polyvinylpyrrolidone in a ratio of 9:1.
Claim 15
Dependent Claim 8 words
A capsule comprising pellets according to claim 1.
Claim 16
Dependent Claim 8 words
A tablet comprising pellets according to claim 1.
Claim 17
Dependent Claim 51 words
A pellet according to claim 1, wherein the polymeric material of the core comprises a major proportion of a copolymer of acrylic and methacrylic acid esters which is freely permeable to water and a minor proportion of a copolymer of acrylic and methacrylic acid esters which is slightly permeable to water.
Claim 18
Dependent Claim 45 words
A pellet according to claim 1, wherein the membrane consists of a copolymer of acrylic and methacrylic acid esters which is slightly permeable to water and a copolymer of acrylic and methacrylic acid esters which is freely permeable to water in a ratio of 8:2.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-05-04 1990-11-03 1991-05-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-05-04 1994-11-03 1995-05-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-05-04 1998-11-03 1999-05-05 $7700.00 Window Closed / Lapsed

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