US4844905A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Granule remaining in stomach
Assignee: Eisai Co Ltd
•
Filing: 1987-02-12
•
Granted: 1989-07-04
•
Expires: 2007-02-12
Abstract
Abstract A granule of drug to remain in the stomach comprises a core comprising a pharmaceutically effective ingredient, a foaming layer coated on said core and an expansive film coated on said layer.
Inventors
- 👤 Masaki Ichikawa
- 👤 Sumio Watanabe
- 👤 Yasuo Miyake
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 13:14
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/0012; A61K9/0053; A61K9/0065; A61K9/0002; A61K9/0007; A61K9/14; A61K9/16; A61K9/48; A61K9/50; A61K9/5073; A61K9/5078
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
148 words
A granule of a pharmaceutical composition adapted to remain in the stomach, comprising: a core containing a pharmaceutical effective ingredient; a gas-generating layer coated on said core, said gas-generating layer comprising sodium bicarbonate and an organic acid capable of generating and evolving CO 2 gas when contacted by gastric juice; and an expandible film coated on and enveloping said gas-generating layer, said film being permeable to gastric juice to permit gastric juice to move therethrough into contact with said gas-generating layer and thereby to generate CO 2 gas inside said film, said film being impermeable to CO 2 gas so that said CO 2 gas generated in said gas-generating layer is retained inside said film and said film is expanded like a balloon by said CO 2 gas so that said granule becomes capable of floating on gastric juice and remains buoyant thereon for a period of time.
Claim 2
Dependent Claim
148 words
A granule of a pharmaceutical composition adapted to remain in the stomach, comprising: a core containing a pharmaceutical effective ingredient; a gas-generating layer coated on said core, said gas-generating layer comprising sodium bicarbonate and an organic acid capable of generating and evolving CO 2 gas when contacted by gastric juice; and an expandible film coated on and enveloping said gas-generating layer, said film being permeable to gastric juice to permit gastric juice to move therethrough into contact with said gas-generating layer and thereby to generate CO 2 gas inside said film, said film being impermeable to CO 2 gas so that said CO 2 gas generated in said gas-generating layer is retained inside said film and said film is expanded like a balloon by said CO 2 gas so that said granule becomes capable of floating on gastric juice and remains buoyant thereon for a period of time.
Claim 3
Dependent Claim
43 words
A granule as claimed in claim 1 in which said granule is capable of floating within 15 minutes after being placed on an artificial gastric juice acetate buffer solution having a pH of 4 and remain floating thereon for at least 5 hours.
Claim 4
Dependent Claim
27 words
A granule as claimed in claim 1, in which said gas-generating layer comprises an inner layer containing sodium bicarbonate and an outer layer containing an organic acid.
Claim 5
Dependent Claim
38 words
A granule as claimed in claim 1, in which said expandible film comprises a polymer which allows gastric juice to pass therethrough and expands by gas produced by the action between the gastric juice and the gas-generating layer.
Claim 6
Dependent Claim
40 words
A granule as claimed in claim 1, which comprises said core, 5 to 20 percent by weight, based on said core, of said gas-generating layer and 5 to 20 percent by weight, based on said core, of said expandible film.
Claim 7
Dependent Claim
54 words
A granule as claimed in claim 1 in which said gas-generating layer contains from 10 to 15 wt. % of sodium bicarbonate, based on the weight of said core, and the amount of said expandible film is from 7 to 15 wt. %, based on the weight of said core and said gas-generating layer.
Claim 8
Dependent Claim
14 words
A granule as claimed in claim 1 having a size of about 1 mm.
Claim 9
Dependent Claim
120 words
A capsule comprising a plurality of granules having different residence times in a stomach, said granules comprising a core containing a pharmaceutically effective ingredient; a foamable layer coated on said core in an amount of 5 to 20 percent by weight, based on said core, said foamable layer comprising an inner layer containing a bicarbonate and an outer layer containing an organic acid; and an expansive film coated on said foamable layer, said expansive film comprising a polymer which allows gastric juice to pass therethrough and expands by foam produced by the action between the gastric juice and said foamable layer, said expansive film being present in an amount of 5 to 20 percent by weight based on said core.
Claim 10
Dependent Claim
120 words
A capsule comprising a plurality of granules having different residence times in a stomach, said granules comprising a core containing a pharmaceutically effective ingredient; a foamable layer coated on said core in an amount of 5 to 20 percent by weight, based on said core, said foamable layer comprising an inner layer containing a bicarbonate and an outer layer containing an organic acid; and an expansive film coated on said foamable layer, said expansive film comprising a polymer which allows gastric juice to pass therethrough and expands by foam produced by the action between the gastric juice and said foamable layer, said expansive film being present in an amount of 5 to 20 percent by weight based on said core.
Claim 11
Dependent Claim
35 words
The capsule of claim 8, wherein the inner foamable layer contains sodium bicarbonate and the outer foamable layer contains an organic acid selected from the group consisting of tartaric acid, succinic acid and citric acid.
Claim 12
Dependent Claim
40 words
The capsule of claim 8, wherein the polymer of the expansive film is one or more members selected from the group consisting of polymers of polyvinyl acetate, acrylic resins, shellac, hydroxypropyl methylcellulose phthalate, cellulose acetate phthalate, methylcellulose, ethylcellulose and hydroxypropylmethylcellulose.
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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) | 1992-07-03 | 1993-01-02 | 1993-07-04 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-07-03 | 1997-01-02 | 1997-07-04 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-07-03 | 2001-01-02 | 2001-07-04 | $7700.00 | Window Closed / Lapsed |