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EP0194838A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Controlled-release pharmaceutical formulation

Assignee: Astellas Pharma Inc
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Filing: 1986-03-10
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Granted: —
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Expires: 2006-03-10
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Abstract

Abstract A pharmaceutical controlled release formulation is disclosed which does not substantially disintegrate but gradually releases a physiologically active substance in the gastrointestinal tract and which comprises a granulation product - (granules) obtained by adding release controlling agent (e.g. an aqueous suspension of a water insoluble macromolecular substance, an aqueous emulsion thereof, a water containing organic-solvent solution thereof, or water) to a mixture of i) physiologically active substance and ii) carrier substance (e.g. crystalline cellulose) in an amount of at least 5 0% by weight based on the weight of the product, and granulating the resultant mixture. The active substance containing granules have a high mechanical strength, disperse widely in the gastrointestinal tract when administered, are water permeable but do not substantially disintegrate in the gastrointestinal tract

Inventors

  • 👤 Muneo Fukui
  • 👤 Kouji Tomuro
  • 👤 Shigeru Masuyama
  • 👤 Atsushi 703-3 Kitamotodanchi Kajiyama
  • 👤 Tamio Hikosaka
  • 👤 Masayoshi Aruga
  • 👤 Yoshiaki Soeishi
  • 👤 Saburo Higuchi

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-05 11:04
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: 7
Claim 1
Independent Claim 71 words
A pharmaceutical controlled-release formulation characterised in that it does not substantially disintegrate but gradually releases a physiologically active substance in the gastrointestinal tract and in that it comprises a granulation product (granules) obtained by adding release controlling agent to a mixture of i) physiologically active substance and ii) carrier substance in an amount of at least 50% by weight based on the weight of the product, and granulating the resultant mixture.
Claim 2
Dependent Claim 71 words
A pharmaceutical controlled-release formulation characterised in that it does not substantially disintegrate but gradually releases a physiologically active substance in the gastrointestinal tract and in that it comprises a granulation product (granules) obtained by adding release controlling agent to a mixture of i) physiologically active substance and ii) carrier substance in an amount of at least 50% by weight based on the weight of the product, and granulating the resultant mixture.
Claim 3
Dependent Claim 15 words
The pharmaceutical formulation as claimed in claim 1, wherein the carrier substance is crystalline cellulose.
Claim 4
Dependent Claim 35 words
The pharmaceutical formulation as claimed in claim 1 or 2 wherein the release controlling agent is an aqueous suspension of a water-insoluble macromolecular substance, an aqueous emulsion thereof, a water-containing organic-solvent solution thereof, or water.
Claim 5
Dependent Claim 22 words
The pharmaceutical formulation as claimed in claim 3, wherein the water-insoluble macromolecular substance is a methyacrylic acid-ethyl acrylate copolymer or ethyl cellulose.
Claim 6
Dependent Claim 18 words
The pharmaceutical formulation as claimed in any preceding claim wherein the physiologically active substance is 5-{2-[2-(o-ethoxyphenoxy)ethyfaminoj-propyt}-2-methoxybenzenesulfonamide hydrochloride (YM-12617).
Claim 7
Dependent Claim 21 words
The pharmaceutical formulation as claimed in any preceding claim wherein the granulation product is granules of diameter 0.1 to 1.5 mm.

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