Patent US2182306A successfully refreshed from Google Patents.
US4199560A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Solid oral pharmaceutical product with increased efficacy and predetermined steady state of solubility
Assignee: Novex Talalmanyfejleszto Es Ertekesito Kulkereskedelmi Rt
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Filing: 1978-10-19
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Granted: 1980-04-22
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Expires: 1998-10-19
Abstract
Abstract The present invention relates to a solid oral pharmaceutical preparation with protracted release of the active ingredient consisting of discrete solid granules containing the active ingredient soluble in the stomach and auxiliary agents and of an equally solid external phase surrounding the said granules, whereby the granules forming the internal phase consist of granules prepared from a powder mixture which contains as active ingredient, or in addition to it a non-toxic metal compound, being capable of binding an acid, and being insoluble or but slightly soluble in neutral aqueous medium--particularly bismuth, aluminium or magnesium compound--and auxiliary materials prepared with an aqueous emulsion containing a hydrophobic component and hydrophylic emulsifiers, and the external phase contains a solid, dry, amphoteric gel forming substance in an amount of 1-50 percent w/w related to the total weight of the preparation in admixture with auxiliary agents. The preparation is produced by the wetting of the powder mixture containing the basic metal compound, auxiliary material and in given case additional active ingredient with the aqueous emulsion of the hydrophobic component prepared by applying the hydrophylic emulsifiers then by granulation and admixing the dried granules with the amphoteric gel forming substance, and pressing it into tablets, or filling into capsules.
Inventors
- 👤 Laszlo Gyarmati
- 👤 Istvan Racz
- 👤 Peter Szentmiklosi
- 👤 Janos Plachy
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 06:53
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1652; A61K9/1617; A61K9/20; A61K9/2072; A61K9/2077; A61K9/48; A61K9/4841
Claims Analysis
Total Claims: 5
Claim 1
Independent Claim
197 words
A solid oral pharmaceutical composition with protracted action in the form of tablets or capsules, having an internal phase consisting of solid granules and a solid external phase surrounding the said granules, wherein the granules are prepared from a powdered mixture of the active ingredients and of auxiliary agents granulated with an aqueous emulsion containing 2 to 10% w/w of stearic or palmitic acid, 0.5 to 5% w/w of sodium carboxymethyl cellulose and 1 to 7% w/w of two different non-toxic emulsifiers imparting a HLB-value of 8 to 12, and the said granules contain 10 to 90% w/w of one or more pharmaceutically active compound including at least 5% w/w of a basic bismuth salt insoluble in water in neutral medium, 5 to 20% w/w of a non-toxic gel-forming organic substance selected from the group consisting of sodium carboxymethyl cellulose, sodium alginate and tragacanth and 5 to 7% of solid residue of the said granulating emulsion, and the said solid external phase contains an amphoteric gel-forming substance selected from the group consisting of tragacanth, pectin and sodium carboxymethyl cellulose, in an amount of 1 to 50% of the total weight of the composition, and usual pharmaceutical excipients.
Claim 2
Dependent Claim
197 words
A solid oral pharmaceutical composition with protracted action in the form of tablets or capsules, having an internal phase consisting of solid granules and a solid external phase surrounding the said granules, wherein the granules are prepared from a powdered mixture of the active ingredients and of auxiliary agents granulated with an aqueous emulsion containing 2 to 10% w/w of stearic or palmitic acid, 0.5 to 5% w/w of sodium carboxymethyl cellulose and 1 to 7% w/w of two different non-toxic emulsifiers imparting a HLB-value of 8 to 12, and the said granules contain 10 to 90% w/w of one or more pharmaceutically active compound including at least 5% w/w of a basic bismuth salt insoluble in water in neutral medium, 5 to 20% w/w of a non-toxic gel-forming organic substance selected from the group consisting of sodium carboxymethyl cellulose, sodium alginate and tragacanth and 5 to 7% of solid residue of the said granulating emulsion, and the said solid external phase contains an amphoteric gel-forming substance selected from the group consisting of tragacanth, pectin and sodium carboxymethyl cellulose, in an amount of 1 to 50% of the total weight of the composition, and usual pharmaceutical excipients.
Claim 3
Dependent Claim
88 words
A pharmaceutical composition as claimed in claim 1, wherein the granules contain 30 to 80% w/w of at least one basic metal compound capable of binding gastric acid selected from the group consisting of magnesium oxide, magnesium trisilicate, aluminum oxide and aluminum hydroxide, including at least 5% of basic bismuth nitrate or carbonate, 5 to 20% w/w of a non-toxic gel-forming organic substance selected from the group consisting of sodium carboxymethyl cellulose, sodium alginate and tragacanth and 5 to 7% of solid residue of the said granulating emulsion.
Claim 4
Dependent Claim
161 words
A process for preparing a solid oral pharmaceutical composition having protracted action, characterized in that a powder mixture containing 30 to 80% w/w of pharmaceutically active ingredients including at least 5% w/w of a basic bismuth salt capable of binding acid and substantially insoluble in water in neutral medium and auxiliary agents including 5 to 20% w/w of a non-toxic organic gel-forming agent is granulated by wetting it with an aqueous emulsion containing 2 to 10% w/w of stearic or palmitic acid, 0.5 to 5% w/w of sodium carboxymethyl cellulose and 1 to 7% w/w of two different non-toxic emulsifiers imparting a HLB-value of 8 to 12, the dried granules are admixed with 1 to 50% by weight, calculated on the total weight of the composition, of a dry powdered amphoteric gel-forming substance selected from the group consisting of tragacanth, pectin and sodium carboxymethyl cellulose and with usual pharmaceutical excipients and the mixture is pressed into tablets or filled into capsules.
Claim 5
Dependent Claim
161 words
A process for preparing a solid oral pharmaceutical composition having protracted action, characterized in that a powder mixture containing 30 to 80% w/w of pharmaceutically active ingredients including at least 5% w/w of a basic bismuth salt capable of binding acid and substantially insoluble in water in neutral medium and auxiliary agents including 5 to 20% w/w of a non-toxic organic gel-forming agent is granulated by wetting it with an aqueous emulsion containing 2 to 10% w/w of stearic or palmitic acid, 0.5 to 5% w/w of sodium carboxymethyl cellulose and 1 to 7% w/w of two different non-toxic emulsifiers imparting a HLB-value of 8 to 12, the dried granules are admixed with 1 to 50% by weight, calculated on the total weight of the composition, of a dry powdered amphoteric gel-forming substance selected from the group consisting of tragacanth, pectin and sodium carboxymethyl cellulose and with usual pharmaceutical excipients and the mixture is pressed into tablets or filled into capsules.
References Cited (Backward Citations)
US2166868A
Cited
US2146867A
Cited
US2836540A
Cited
US2774710A
Cited
US2793979A
Cited
US2854376A
Cited
US2805977A
Cited
US2875130A
Cited
US3079303A
Cited
US3062720A
Cited
US3108046A
Cited
US3175942A
Cited
US3362880A
Cited
US3555151A
Cited
US3579634A
Cited
US3944660A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-04-22 | 1983-10-22 | 1984-04-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-04-22 | 1987-10-22 | 1988-04-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-04-22 | 1991-10-22 | 1992-04-22 | $7700.00 | Window Closed / Lapsed |