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EP0225615A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Resinate sustained release dextromethorphan composition

Assignee: Novartis AG
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Filing: 1986-12-05
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Granted: —
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Expires: 2006-12-05
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Abstract

Abstract The invention relates to a pharmaceutical preparation for controlled, sustained release of dextromethorphan comprising a polystyrene sulfonate resin which has been cross- linked with about 3% to about 10% divinyl benzene, having an average particle size of at least 40 µm and less than 100 pm onto which dextromethorphan has been loaded in a ratio expressed in weight amounts of dextromethorphan-hydrobromide to resin of about 1:6 to about 1:10 and at least one pharmaceutically acceptable adjuvant.

Inventors

  • 👤 Franz Xaver Dr. Fischer
  • 👤 Satish Chandra Dr. Khanna

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-29 06:37
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/485; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/585

Claims Analysis

Total Claims: 28
Claim 1
Independent Claim 73 words
A pharmaceutical composition suitable for controlled, sustained release of a pharmaceutically acceptable acid addition salt of dextromethorphan and which pharmaceutical composition contains a) a cationic, gel-type, microporous ion-exchange resin consisting of a sulfonated polystyrene-divinylbenzene copolymerisate, b) a pharmaceutically acceptable acid addition salt of dextromethorphan in a weight ratio of 1:5 to 1:10 expressed for the weight ratio of dextromethorphan-hydrobromide and the Na-form of the resin and c) at least one pharmaceutically acceptable adjuvant.
Claim 2
Dependent Claim 73 words
A pharmaceutical composition suitable for controlled, sustained release of a pharmaceutically acceptable acid addition salt of dextromethorphan and which pharmaceutical composition contains a) a cationic, gel-type, microporous ion-exchange resin consisting of a sulfonated polystyrene-divinylbenzene copolymerisate, b) a pharmaceutically acceptable acid addition salt of dextromethorphan in a weight ratio of 1:5 to 1:10 expressed for the weight ratio of dextromethorphan-hydrobromide and the Na-form of the resin and c) at least one pharmaceutically acceptable adjuvant.
Claim 3
Dependent Claim 28 words
A pharmaceutical composition according to claim 1 wherein the resin is crosslinked with about 4-8 % by weight with divinylbenzene based on the weight of the dry resin.
Claim 4
Dependent Claim 26 words
A pharmaceutical composition according to claims 1 or 2 wherein the resin is commercially available and has been approved for pharmaceutical purposes for formulation with medicaments.
Claim 5
Dependent Claim 20 words
A pharmaceutical composition according to claim 3, wherein the resin is commercially available under the trade name Amberlite® IRP 69.
Claim 6
Dependent Claim 25 words
The composition of claim 1 wherein said average particle size of the resin in dry state is between about 40 µm and about 80 um.
Claim 7
Dependent Claim 18 words
The composition of claim 5 wherein said average particle size is about 50 µm to about 70 µm.
Claim 8
Dependent Claim 22 words
The composition of claim 5 or 6 wherein at least 95 % of said resin particles are of said average particle size.
Claim 9
Dependent Claim 20 words
A pharmaceutical composition according to claim 1 wherein the dextromethorphan is present in the form of the hydrobromide addition salt.
Claim 10
Dependent Claim 23 words
A pharmaceutical composition according to claim 1 wherein dextromethorphan-hydrobromide and the Na-form of the resinate are present in a weight ratio of 1:6.
Claim 11
Dependent Claim 20 words
The composition of claim 1 wherein said adjuvants are selected from pharmaceutically acceptable solvents, thickeners, sweeteners, flavorings, colorings, and preservatives.
Claim 12
Dependent Claim 29 words
A process for the preparation of pharmaceutical compositions according to claim 1, characterized in that the components a), b) and c) are admixed and formulated into solutions or tablets.
Claim 13
Dependent Claim 11 words
Pharmaceutical compositions for use as antitussives in the treatment of humans.
Claim 14
Dependent Claim 11 words
Pharmaceutical compositions for use as antitussives in the treatment of humans.
Claim 15
Dependent Claim 39 words
Use of a cationic, microporous, ion-exchange resin consisting of a sulfonated polystyrene-divinylbenzene copolymerisate and a pharmaceutically acceptable acid addition salt of dextromethorphan for the preparation of a pharmaceutical composition suitable as antitussively active agent in the treatment of humans.
Claim 16
Dependent Claim 39 words
Use of a cationic, microporous, ion-exchange resin consisting of a sulfonated polystyrene-divinylbenzene copolymerisate and a pharmaceutically acceptable acid addition salt of dextromethorphan for the preparation of a pharmaceutical composition suitable as antitussively active agent in the treatment of humans.
Claim 17
Dependent Claim 12 words
What is claimed is: (for the designated states Austria, Spain and Greece)
Claim 18
Dependent Claim 97 words
A process for the preparation of a pharmaceutical composition suitable for controlled, sustained release of a pharmaceutically acceptable acid addition salt of dextromethorphan in solution and which pharmaceutical composition contains a) a cationic, gel-type, microporous ion-exchange resin consisting of a sulfonated polystyrene-divinylbenzene copolymerisate, b) a pharmaceutically acceptable acid addition salt of dextromethorphan in a weight ratio of 1:5 to 1:10 expressed for the weight ratio of dextromethorphanhydrobromide and the Na-form of the resin and c) at least one pharmaceutically acceptable adjuvant, characterized in that the components a), b) and c) are admixed and formulated to administration forms.
Claim 19
Dependent Claim 97 words
A process for the preparation of a pharmaceutical composition suitable for controlled, sustained release of a pharmaceutically acceptable acid addition salt of dextromethorphan in solution and which pharmaceutical composition contains a) a cationic, gel-type, microporous ion-exchange resin consisting of a sulfonated polystyrene-divinylbenzene copolymerisate, b) a pharmaceutically acceptable acid addition salt of dextromethorphan in a weight ratio of 1:5 to 1:10 expressed for the weight ratio of dextromethorphanhydrobromide and the Na-form of the resin and c) at least one pharmaceutically acceptable adjuvant, characterized in that the components a), b) and c) are admixed and formulated to administration forms.
Claim 20
Dependent Claim 34 words
A process for the preparation of a pharmaceutical composition according to claim 1 wherein the resin is crosslinked with about 4-8 % by weight with divinylbenzene based on the weight of the dry resin.
Claim 21
Dependent Claim 32 words
A process for the preparation of a pharmaceutical composition according to claims 1 or 2 wherein the resin is commercially available and has been approved for pharmaceutical purposes for formulation with medicaments.
Claim 22
Dependent Claim 27 words
A process for the preparation of a pharmaceutical composition according to claim 3, wherein the resin is commercially available under the trade name Amberlite e IRP 69.
Claim 23
Dependent Claim 32 words
A process for the preparation of a pharmaceutical composition of claim 1 wherein said average particle size of the resin in dry state is between about 40 µm and about 80 pm.
Claim 24
Dependent Claim 25 words
A process for the preparation of a pharmaceutical composition of claim 5 wherein said average particle size is about 50 pm to about 70 pm.
Claim 25
Dependent Claim 29 words
A process for the preparation of a pharmaceutical composition of claim 5 or 6 wherein at least 95 % of said resin particles are of said average particle size.
Claim 26
Dependent Claim 26 words
A process for the preparation of a pharmaceutical composition according to claim 1 wherein the dextromethorphan is present in the form of the hydrobromide addition salt.
Claim 27
Dependent Claim 29 words
A process for the preparation of a pharmaceutical composition according to claim 1 wherein dextromethorphan-hydrobromide and the Na-form of the resinate are present in a weight ratio of 1:6.
Claim 28
Dependent Claim 27 words
A process for the preparation of a pharmaceutical composition of claim 1 wherein said adjuvants are selected from pharmaceutically acceptable solvents, thickeners, sweeteners, flavorings, colorings, and preservatives.

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