Patent EP0287536A1 successfully refreshed from Google Patents.
EP0287536A1
Expired / Lapsed
EP
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Pharmaceutical quinidine composition
Assignee: Lejus Medical AB
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Filing: 1988-03-10
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Granted: —
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Expires: 2008-03-10
Abstract
Abstract The present invention relates to a pharmaceutical composition in a multiple-unit dosage granular form comprising quinidine salt as a therapeutically active compound, and intended to be administered once per 24 hrs, whereby the composition releases quinidine salt in accordance with US Pharmacopea Standards (USP XXI, apparatus 2, 75 rpm) in an artificial gastric juice having pH 1.2 to an extent of less than 30% after 2 hrs of exposure; and releases according to the same Statndard in a phosphate buffer having pH 6.8 to an extent of more than 25%, but less than 90% after 3 hrs of exposure in said phosphate buffer, pH 6.8, (a total exposure of 5 hrs) and releases more than 60% after 8 hrs of exposure (a total of 10 hrs of exposure); and releases less than 100% after 4 hrs of exposure (a total of 6 hrs of exposure) in said phosphate buffer; and releases quinidine salt to an extent of more than 90% after 12 hrs of exposure (a total of 14 hrs of exposure) in said phosphate buffer.
Inventors
- 👤 Curt Henry Appelgren
- 👤 Eva Christina Eskilsson
- 👤 Sören Ingemar Johansson
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-06 14:52
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/49; A61K9/00; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5026; A61K9/5036; A61K9/5042; A61K9/5047
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
182 words
A pharmaceutical composition in a multiple-unit granular dosage form comprising quinidine salt selected from the group consisting of gluconate, sulphate, and hydrogen sulphate as a therpeutically active component, and intended to be administered once per 24 hrs, characterized in that the composition releases quinidine salt in accordance with US Pharmacopea Standards (USP XXI, apparatus 2, 75 rpm) in an artificial gastric juice having pH 1.2 to an extent of less than 30% after 2 hrs; and releases according to the same Standard in a phosphate buffer having pH 6.8 to an extent of more than 25% but less than 90% after 3 hrs of exposure in said phosphate buffer, pH 6.8, (a total exposure of 5 hrs) and releases more than 60% after 8 hrs of exposure (a total of 10 hrs of exposure); and releases less than 100% after 4 hrs of exposure (a total of 6 hrs of exposure) in said phosphate buffer; and releases quinidine salt to an extent of more than 90% after 12 hrs of exposure (a total of 14 hrs of exposure) in said phosphate buffer.
Claim 2
Dependent Claim
182 words
A pharmaceutical composition in a multiple-unit granular dosage form comprising quinidine salt selected from the group consisting of gluconate, sulphate, and hydrogen sulphate as a therpeutically active component, and intended to be administered once per 24 hrs, characterized in that the composition releases quinidine salt in accordance with US Pharmacopea Standards (USP XXI, apparatus 2, 75 rpm) in an artificial gastric juice having pH 1.2 to an extent of less than 30% after 2 hrs; and releases according to the same Standard in a phosphate buffer having pH 6.8 to an extent of more than 25% but less than 90% after 3 hrs of exposure in said phosphate buffer, pH 6.8, (a total exposure of 5 hrs) and releases more than 60% after 8 hrs of exposure (a total of 10 hrs of exposure); and releases less than 100% after 4 hrs of exposure (a total of 6 hrs of exposure) in said phosphate buffer; and releases quinidine salt to an extent of more than 90% after 12 hrs of exposure (a total of 14 hrs of exposure) in said phosphate buffer.
Claim 3
Dependent Claim
24 words
Composition according to claim 1, characterized in that the release in artificial gastric juice, pH 1.2, is less than 20% after hrs of exposure.
Claim 4
Dependent Claim
24 words
Composition according to claims 1-2, characterized in that the release in artificial gastric juice, pH 1.2, is less than 10% after 2hrs of exposure.
Claim 5
Dependent Claim
42 words
Composition according to claims 1-3, characterized in that it comprises a core having a content of 50-95% by weight of quinidine gluconate coated with 2-20% by weight of hydroxypropyl methyl cellulose phtalate, and ethyl cellulose in a mixture having the relationship 70-35:30-65.
Claim 6
Dependent Claim
12 words
Composition according to claim 4, characterized in that the relationship is 60-40:40-60.
Claim 7
Dependent Claim
26 words
Composition according to claims 4-5, characterized in that the hydroxypropyl methyl cellulose phtalate and ethyl cellulose has been added in an amount of 4-12% by weight.
Claim 8
Dependent Claim
26 words
Composition according to claim 6, characterized in that the mixture has been added in an amount of 7-10% by weight of the weight of the granules.
Claim 9
Dependent Claim
21 words
Composition according to claims 4-7, characterized in that ingoing hydroxypropyl methyl cellulose phtalate has a pk a of 5.0-6.5, preferably 5.5.
Claim 10
Dependent Claim
35 words
Composition according to one or more of the preceeding claims, characterized in that ingoing hydroxypropyl methyl cellulosa phtalate has been exchanged for cellulose acetate phtalate, methylmethacrylate methylester (EUDRAGIT L, and S), and/or polyvinyl acetate phtalate.
Claim 11
Dependent Claim
39 words
Composition according to one or more of the preceeding claims, characterized in that ingoing ethyl cellulose has been exchanged for a copolymer of polyethyl acrylate (63-65%), methyl methacrylate (31.7-32.3%), and trimethylammonium ethyl methacrylate chloride (2.5-5%) (EUDRAGIT RS, and RL).
Claim 12
Dependent Claim
43 words
Composition according to claims 1-3, characterized in that it comprises a core having a content of 50-95% by weight of quinidine sulphate coated with 2-20% by weight of a mixture of methyl methacrylate methylester (5%), hydroxypropyl methyl cellulose phtalate (90%), and cetanol (5%).
Claim 13
Dependent Claim
21 words
Composition according to claim 11, characterized in that ingoing hydroxypropyl methyl cellulose phtalate has a pk a of 5.0-6.5, preferably 5.5.
References Cited (Backward Citations)
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