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EP0294103A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

A sustained-release preparation and production thereof

Assignee: Takeda Pharmaceutical Co Ltd
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Filing: 1988-05-26
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Granted: —
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Expires: 2008-05-26
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Abstract

Abstract The present invention concerns a sustained-release microcapsule preparation comprising an ion exchange resin with 6 to 16% crosslinking, containing a drug adsorbed to not less than 80% of its theoretical ion adsorption amount and coated with a water-permeable polymer. The sustained-release preparation of this invention contains a high concentration of an absorbed drug: it shows neither cracking nor breaking in its coat and exhibits good sustained-release properties which enhance its dosage form design and makes it easy to take.

Inventors

  • 👤 Muneo Nonomura
  • 👤 Yasuyuki Suzuki
  • 👤 Masayuki Yamada

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-02 14:10
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5036; A61K9/5042; A61K9/5047; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/585; A61K9/5026

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 35 words
A sustained-release microcapsule preparation comprising an ion exchange resin of 6 to 16% crosslinking, containing a drug adsorbed to not less than 80% of its theoretical ion adsorption amount, and coated with a water-­permeable polymer.
Claim 2
Dependent Claim 35 words
A sustained-release microcapsule preparation comprising an ion exchange resin of 6 to 16% crosslinking, containing a drug adsorbed to not less than 80% of its theoretical ion adsorption amount, and coated with a water-­permeable polymer.
Claim 3
Dependent Claim 17 words
The preparation according to claim 1, wherein the ion exchange resin is a synthetic insoluble porous polymer.
Claim 4
Dependent Claim 16 words
The preparation according to claim 2, wherein the polymer is a copolymer of styrene and divinylbenzene.
Claim 5
Dependent Claim 17 words
The preparation according to claim 1, wherein the ion exchange resin is an acidic ion exchange resin.
Claim 6
Dependent Claim 25 words
The preparation according to claim 1, wherein the drug has a pKa from 6 to 10 or from 2 to 5 with a stericallybulky structure.
Claim 7
Dependent Claim 13 words
The preparation according to claim 1, wherein the drug is for respiratory tract.
Claim 8
Dependent Claim 19 words
The preparation according to claim 1, wherein the drug is a free form derived from the corresponding salt form.
Claim 9
Dependent Claim 14 words
The preparation according to claim 6, wherein the drug is dihydrocodein, phenylpropanolamine or dl-methylephedrin.
Claim 10
Dependent Claim 17 words
The preparation according to claim 1, wherein the ion exchange resin complex is coated with non-natural polymer.
Claim 11
Dependent Claim 20 words
The preparation according to claim 1, wherein the mean particle size of the microcapsule is from 5 to 1,000 µm.
Claim 12
Dependent Claim 18 words
A suspension for oral administration containing the preparation according to claim 1 in suspension in a purified water.
Claim 13
Dependent Claim 42 words
A method of producing the preparation according to claim 1, which comprises coating an ion exchange resin of 6 to 16% crosslinking and containing a drug adsorbed to not less than 80% of its theoretical ion adsorption amount with a water-permeable polymer.
Claim 14
Dependent Claim 66 words
The method according to claim 12, wherein the drug-ion exchange resin complex is produced by adding an ion exchange resin of 6 to 16% crosslinking to an aqueous solution of a drug in a free form prepared by reacting a salt of the drug with an ion exchange resin in an aqueous solvent capable of dissolving both the salt and the free form of the drug.

References Cited (Backward Citations)

US3313686A Cited
DE1908946A1 Cited
DE2246037A1 Cited
US4221778A Cited
EP0154009A1 Cited

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