Patent US4434152A successfully refreshed from Google Patents.
US4434152A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Time-release
Assignee: Chinoin Private Co Ltd
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Filing: 1982-04-26
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Granted: 1984-02-28
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Expires: 2002-04-26
Abstract
Abstract Time-release pharmaceutical compositions, suitable for oral administration, are disclosed, which comprise as active ingredient 50 to 70% by weight of a compound of the formula (I) ##STR1## or the formula (Ia) ##STR2## wherein R is hydrogen or --CH 2 COOH, R 1 is hydrogen or alkyl having 1 to 4 carbon atoms, R 2 is alkyl having 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 5 carbon atoms, carbamoly or ureido, R 3 is hydrogen or methyl, and the dotted line stands for two hydrogens or another bond, or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, and which further include 4 to 8% by weight of a hydrophobic substance with a great specific surface; 7 to 12% by weight of a lipoid; 8 to 12% by weight of a polyoxy compound; 4 to 9% by weight of a binding agent; and 0.5 to 4% by weight of an acid stabilizer.
Inventors
- 👤 Tibor Horvath
- 👤 Agnes Udvardy
- 👤 Agoston David
- 👤 Katalin Marmarosi nee Kellner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 18:22
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K9/00; A61K9/20; A61K9/2004
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
159 words
A tablet or dragee core for a time-release pharmaceutical composition, suitable for oral administration, which comprises as active ingredient 50 to 70% by weight of a compound of the formula (I) ##STR5## or the formula (Ia) ##STR6## wherein R is hydrogen or --CH 2 COOH, R 1 is hydrogen or alkyl having 1 to 4 carbon atoms, R 2 is alkyl having 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 5 carbon atoms, carbamoyl or ureido, R 3 is hydrogen or methyl, and the dotted line stands for two hydrogens or another bond, or a pharmaceutically acceptable acid addit ion or quaternary ammonium salt thereof, and which further comprises by weight 1% colloidal silicic acid, 6.5% hydrophobic colloidal silicic acid, 7 to 12% fatty acid, 8 to 12% microcrystalline cellulose, 4 to 9% polyvinylpyrrolidone-vinyl acetate, and 0.5 to 4% of an acid stabilizer selected from the group consisting of betaine in hydrochloric acid tartaric acid and citric acid.
Claim 2
Dependent Claim
159 words
A tablet or dragee core for a time-release pharmaceutical composition, suitable for oral administration, which comprises as active ingredient 50 to 70% by weight of a compound of the formula (I) ##STR5## or the formula (Ia) ##STR6## wherein R is hydrogen or --CH 2 COOH, R 1 is hydrogen or alkyl having 1 to 4 carbon atoms, R 2 is alkyl having 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 5 carbon atoms, carbamoyl or ureido, R 3 is hydrogen or methyl, and the dotted line stands for two hydrogens or another bond, or a pharmaceutically acceptable acid addit ion or quaternary ammonium salt thereof, and which further comprises by weight 1% colloidal silicic acid, 6.5% hydrophobic colloidal silicic acid, 7 to 12% fatty acid, 8 to 12% microcrystalline cellulose, 4 to 9% polyvinylpyrrolidone-vinyl acetate, and 0.5 to 4% of an acid stabilizer selected from the group consisting of betaine in hydrochloric acid tartaric acid and citric acid.
Claim 3
Dependent Claim
62 words
The table or dragee core defined in claim 1 wherein the fatty acid is stearic acid present in the amount of 10.5%, the microcrystalline cellulose is present in an amount of 10%, the polyvinylpyrrolidone-vinyl acetate is present in an amount of 7% and the acid stabilizer is selected from the group consisting of 0.6% betaine in hydrochloric acid and 3.5% citric acid.
Claim 4
Dependent Claim
37 words
The dragee core defined in claim 1 coated by a shell which comprises 55% by weight talc, 17% by weight polyvinylpyrrolidone-vinyl acetate, 17% by weight cellulose, 9% by weight titanium dioxide, and 2% by weight polyoxyethylene 6000.
Claim 5
Dependent Claim
16 words
The time-release pharmaceutical composition defined in claim 1 further comprising an inert filling agent or diluent.
Claim 6
Dependent Claim
19 words
The time-release pharmaceutical composition defined in claim 1 which comprises 1,6-dimethyl-3-carbethoxy-4-oxo-6,7,8,9-tetrahydro-homopyrimidzaolium metosulfate of the formula (I) as active ingredient.
Claim 7
Dependent Claim
18 words
The time-release pharmaceutical composition defined in claim 1 which comprises 6-methyl-9-carboxymethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2-a)pyrimidine of the formula (I) as active ingredient.
Claim 8
Dependent Claim
19 words
The time-release pharmaceutical composition defined in claim 1 which comprises 2,6-dimethyl-3-ethyl-4-oxo-4H-pyrido(1,2-a)pyrimidine hydrochloride of the formula (I) as active ingredient.
Claim 9
Dependent Claim
19 words
The time-release pharmaceutical composition defined in claim 1 which comprises 2,6-dimethyl-3-ethyl-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine hydrochloride of the formula (Ia) as active ingredient.
Claim 10
Dependent Claim
18 words
The time-release pharmaceutical composition defined in claim 1 which comprises 1,6-dimethyl-3-ureido-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine of the formula (Ia) as active ingredient.
Claim 11
Dependent Claim
20 words
The time-release pharmaceutical composition defined in claim 1 which comprises 1,6-dimethyl-3carbethoxy-4-oxo-6,7,8,9-tetrahydro-homopyrimidazolium-metosulfate of the formula (I) and indomethacin as active ingredients.
Claim 12
Dependent Claim
21 words
The time-release pharmaceutical composition defined in claim 1 which comprises 1,6-dimethyl-3-carbethoxy-4-oxo-6,7,8,9-tetrahydro-homopyrimidazolium-metosulfate of the formula (I) and azidocodeine bitartrate as active ingredients.
Claim 13
Dependent Claim
24 words
The time-release pharmaceutical composition defined in claim 1 in the form of a tablet or dragee, containing up to 2.5% by weight of water.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-02-27 | 1987-08-29 | 1988-02-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-02-27 | 1991-08-29 | 1992-02-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-02-27 | 1995-08-29 | 1996-02-28 | $7700.00 | Window Closed / Lapsed |