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US4772475A Expired / Lapsed US ⏱️ 0.0 years remaining

Controlled-release multiple units pharmaceutical formulation

Assignee: Astellas Pharma Inc
•
Filing: 1986-02-27
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Granted: 1988-09-20
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Expires: 2006-02-27
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Abstract

Abstract A pharmaceutical controlled-release individual unit or multiple units formulation in which the individual unit comprises a granulation product obtained by adding a release controlling agent to a mixture of a physiologically active substance and units-forming substance(s) and granulating and resultant mixture, said granulation product (granules) being substantially not disintegrated but gradually releasing the physiologically active substance in the gastrointestinal tract.

Inventors

  • 👤 Muneo Fukui
  • 👤 Kouji Tomuro
  • 👤 Shigeru Masuyama
  • 👤 Atsushi Kajiyama
  • 👤 Tamio Hikosaka
  • 👤 Masayoshi Aruga
  • 👤 Saburo Higuchi
  • 👤 Yoshiaki Soeishi

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-28 11:50
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2072; A61K9/2077; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1635; A61K9/1652

Claims Analysis

Total Claims: 6
Claim 1
Independent Claim 100 words
A pharmaceutical controlled-release individual unit or multiple unit formulation in which said individual unit consists essentially a granulation product obtained by adding a release controlling agent selected from the group consisting of acrylic acid polymers, acrylic acid copolymers and mixtures thereof with cellulose derivatives, to a mixture of physiologically active substances and crystalline cellulose, in an amount such that at least 50% by weight based on the weight of the units is said crystalline cellulose and granulating the resultant mixture and wherein said granulation product does not substantially disintegrate but gradually releases the physiologically active substance in the gastrointestinal tract.
Claim 2
Dependent Claim 100 words
A pharmaceutical controlled-release individual unit or multiple unit formulation in which said individual unit consists essentially a granulation product obtained by adding a release controlling agent selected from the group consisting of acrylic acid polymers, acrylic acid copolymers and mixtures thereof with cellulose derivatives, to a mixture of physiologically active substances and crystalline cellulose, in an amount such that at least 50% by weight based on the weight of the units is said crystalline cellulose and granulating the resultant mixture and wherein said granulation product does not substantially disintegrate but gradually releases the physiologically active substance in the gastrointestinal tract.
Claim 3
Dependent Claim 27 words
The pharmaceutical formulation as claimed in claim 1, wherein the release controlling agent is a methacrylic acid-ethyl acrylate copolymer or mixtures of said copolymer and ethyl cellulose.
Claim 4
Dependent Claim 16 words
The pharmaceutical formulation as claimed in claim 1, wherein the release controlling agent further contains water.
Claim 5
Dependent Claim 20 words
The pharmaceutical formulation as claimed in claim 1, 2, or 3, wherein the physiologically active substance is 5-{2-[2-(o-ethoxypheoxy)ethylamino]propyl}-2-methoxybenzenesulfonamide hydrochloride (YM-12617).
Claim 6
Dependent Claim 26 words
The pharmaceutical formulation as claimed in claim 1, 2, 3, or 4, wherein the individual unit is granulation product having diameter of 0.1 to 1.5 mm.

References Cited (Backward Citations)

US4472398A Cited
US4495189A Cited
US4305958A Cited
US4241086A Cited
US4261970A Cited
US4438115A Cited
US4469704A Cited
US4501752A Cited
US4552765A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-09-20 1992-03-21 1992-09-20 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-09-20 1996-03-21 1996-09-20 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-09-20 2000-03-21 2000-09-20 $7700.00 Window Closed / Lapsed

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