US5026559A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Sustained-release pharmaceutical preparation
Assignee: KINAFORM TECHNOLOGY Inc 1101-C LYONS ROAD DAYTON OH 45459 A CORP OF OH
•
Filing: 1989-04-03
•
Granted: 1991-06-25
•
Expires: 2009-04-03
Abstract
Abstract A sustained-release pharmaceutical preparation comprising an admixture of uncoated and/or single walled coated drug, and multi-units of microparticles of a multi-walled coated drug. The microparticle structure preferably has a core drug, an inner wall microencapsular enteric coating, such as a polymethyacrylic acid/acrylic acid copolymer or cellulose acetate phthalate, a solid acid such as citric acid, adipic acid, or an acidic ion exchange resin layered onto or included in the enteric layer, and an outer wall microencapsulated control coating, such as a polymethacrylic acid ester copolymer or ethyl cellulose. The multi-walled coated drug has a delayed, gradual, long-term release which takes place in the intestines while the uncoated and/or single walled coated drug has immediate therapeutic properties upon dissolution in the stomach. The enteric coating and control coating may be applied to core drug granules by a coacervation, spray coating or other process. The acid may be a separate layer applied by a spray coating or other process.
Inventors
- 👤 Herman J. Eichel
- 👤 Brent D. Massmann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 10:54
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5073; A61K9/5078; A61K9/5084
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
140 words
A sustained-release pharmaceutical preparation comprising an admixture of: (a) immediate release drug which will release in the stomach, and; (b) multi-units of microparticles, said microparticles comprising a core, an inner wall, a solid acid layer, and an outer wall, said core being a drug which is the same as said immediate release drug, said inner wall being a microencapsular enteric coating which will not dissolve or disperse readily in the stomach, but which dissolves or disperses in the intestines, said solid acid layer being incorporated in or layered onto said inner wall microencapsular enteric coating in order to preserve the impermeability of the enteric coating and delay drug release, and said outer wall being a microencapsular control coating which will not dissolve or disperse readily in the intestines, but which permits release of said drug through said microencapsular control coating.
Claim 2
Dependent Claim
140 words
A sustained-release pharmaceutical preparation comprising an admixture of: (a) immediate release drug which will release in the stomach, and; (b) multi-units of microparticles, said microparticles comprising a core, an inner wall, a solid acid layer, and an outer wall, said core being a drug which is the same as said immediate release drug, said inner wall being a microencapsular enteric coating which will not dissolve or disperse readily in the stomach, but which dissolves or disperses in the intestines, said solid acid layer being incorporated in or layered onto said inner wall microencapsular enteric coating in order to preserve the impermeability of the enteric coating and delay drug release, and said outer wall being a microencapsular control coating which will not dissolve or disperse readily in the intestines, but which permits release of said drug through said microencapsular control coating.
Claim 3
Dependent Claim
47 words
The sustained-release pharmaceutical preparation of claim 1 wherein said inner wall enteric coating is selected from the group consisting of polymethacrylic acid/acrylic acid copolymer, cellulose acetate phthalate, hydroxypropyl methyl cellulose phthalate, polyvinyl acetate phthalate, hydroxyethyl ethyl cellulose phthalate, cellulose acetate tetrahydrophthalate, acrylic resin, and cellulose acetate trimellitate.
Claim 4
Dependent Claim
28 words
The sustained-release pharmaceutical preparation of claim 2 wherein said outer wall microencapsular control coating is selected from the group consisting of methacrylic acid ester copolymer and ethyl cellulose.
Claim 5
Dependent Claim
28 words
The sustained-release pharmaceutical preparation of claim 3 wherein said drug is selected from the group consisting of aspirin, acetaminophen, indomethacin, propranolol hydrochloride, dextromethorphan hydrobromide, disopyramide phosphate an furosemide.
Claim 6
Dependent Claim
38 words
The sustained-release pharmaceutical preparation of claim 1 wherein said acid is selected from the group consisting of citric acid, ascorbic acid, adipic acid, ethylene diamine tetracetic acid, lactic acid, succinic acid, polymeric acids, and acidic ion exchange resins.
Claim 7
Dependent Claim
37 words
The sustained-release pharmaceutical preparation of claim 1 wherein said drug is indomethacin, said inner wall microencapsular enteric coating is a polymethacrylic acid/acrylic acid copolymer and said outer wall microcapsular control coating is a methacrylic acid ester copolymer.
Claim 8
Dependent Claim
21 words
The sustained-release pharmaceutical preparation of claim 6 wherein said admixture consists of about 15% uncoated drug, and 85% multi-walled coated medicament.
Claim 9
Dependent Claim
129 words
A multi-walled coated medicament comprising: (a) a core containing a water-soluble drug, (b) an inner wall microencapsulated enteric coating selected from the group consisting of polymethacrylic acid/acrylic acid copolymer, cellulose acetate phythalate, hydroxethyl ethyl cellulose phythalate, cellulose acetate tetrahydroxphthalate acrylic resin, and cellulose acetate trimellitate, (c) an acid selected from the group consisting of citric acid, ascorbic acid, acidic acid, ethylene diamine tetracetic acid, lactic acid, succinic acid, polymeric acids and acidic ion exchange resins incorporated in or layered onto said inner wall microencapsular enteric coating in order to preserve the impermeability of the enteric polymer and delay drug release, and (d) an outer wall microencapsular control coating selected from the group consisting of methacrylic acid ester copolymer and ethyl cellulose being over said enteric coating and said acid.
Claim 10
Dependent Claim
129 words
A multi-walled coated medicament comprising: (a) a core containing a water-soluble drug, (b) an inner wall microencapsulated enteric coating selected from the group consisting of polymethacrylic acid/acrylic acid copolymer, cellulose acetate phythalate, hydroxethyl ethyl cellulose phythalate, cellulose acetate tetrahydroxphthalate acrylic resin, and cellulose acetate trimellitate, (c) an acid selected from the group consisting of citric acid, ascorbic acid, acidic acid, ethylene diamine tetracetic acid, lactic acid, succinic acid, polymeric acids and acidic ion exchange resins incorporated in or layered onto said inner wall microencapsular enteric coating in order to preserve the impermeability of the enteric polymer and delay drug release, and (d) an outer wall microencapsular control coating selected from the group consisting of methacrylic acid ester copolymer and ethyl cellulose being over said enteric coating and said acid.
Claim 11
Dependent Claim
29 words
The multi-walled coated medicament of claim 8 wherein said core drug is selected from the group consisting of aspirin, acetaminophen, indomethacin, propranolol hydrochloride, dextromethorphan hydrobromide, disopyramide phosphate and furosemide.
Claim 12
Dependent Claim
19 words
The multi-walled coated medicament of claim 9 wherein said inner wall enteric coating is a polymethacrylic acid/acrylic acid copolymer.
Claim 13
Dependent Claim
15 words
The multi-walled coated medicament of claim 10 wherein said acid layer coating is citric acid.
Claim 14
Dependent Claim
20 words
The multi-walled coated medicament of claim 11 wherein said outer wall microencapsular control coating is a methacrylic acid ester copolymer.
Claim 15
Dependent Claim
13 words
The multi-walled coated medicament of claim 12 wherein said core drug is indomethacin.
Claim 16
Dependent Claim
44 words
The multi-walled coated medicament of claim 13 wherein said water-soluble drug is 28%, said inner wall enteric coating is 27%, said acid is layered onto said inner wall enteric coating and is 35% and said outer wall microencapsular control coating is 6% by weight.
Claim 17
Dependent Claim
22 words
The multi-walled coated medicament of claim 8 wherein a second said water-soluble drug layer is outside said outer wall microencapsular control coating.
Claim 18
Dependent Claim
23 words
The multi-walled coated medicament of claim 15 wherein a second said outer wall microencapsulated control coating is outside said second water-soluble drug layer.
Claim 19
Dependent Claim
26 words
The multi-walled coated medicament of claim 8 wherein a second said water-soluble drug layer is between an acid layer and said outer wall microencapsulated control coating.
Claim 20
Dependent Claim
28 words
The multi-walled coated medicament of claim 8 wherein a second said outer wall microencapsulated control coating is between said water-soluble drug and said inner wall microencapsulated enteric coating.
References Cited (Backward Citations)
US3115441A
Cited
US3155590A
Cited
US3341416A
Cited
US3531418A
Cited
US3488418A
Cited
US3492397A
Cited
US4025613A
Cited
JPS5411687A
Cited
JPS56108269A
Cited
EP0077956A1
Cited
US4572833A
Cited
US4520009A
Cited
US4728512A
Cited
US4752470A
Cited
US4808413A
Cited
US4808413B1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-06-24 | 1994-12-24 | 1995-06-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-06-24 | 1998-12-24 | 1999-06-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-06-24 | 2002-12-24 | 2003-06-25 | $7700.00 | Window Closed / Lapsed |