EP0391518A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Sustained-release pharmaceutical preparation
Assignee: Kinaform Technology Inc
•
Filing: 1990-02-01
•
Granted: —
•
Expires: 2010-02-01
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 polymethacrylic 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
EP
Data Source
google_patents
Last Synchronized
2026-10-24 22:04
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5073; A61K9/5078; A61K9/5084
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
86 words
A sustained-release pharmaceutical preparation comprising an admixture of: a) a uncoated or single walled coated drug, and; b) multi-units of microparticles of multi-walled coated medicament comprising a core of said drug coated with an inner wall microencapsular enteric coating which will not dissolve or disperse readily in the stomach, but which dissolves or disperses in the intestines and an outer wall 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
86 words
A sustained-release pharmaceutical preparation comprising an admixture of: a) a uncoated or single walled coated drug, and; b) multi-units of microparticles of multi-walled coated medicament comprising a core of said drug coated with an inner wall microencapsular enteric coating which will not dissolve or disperse readily in the stomach, but which dissolves or disperses in the intestines and an outer wall 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 and furosemide.
Claim 6
Dependent Claim
23 words
The sustained-release pharmaceutical preparation of claim 4 further including a solid acid incorporated in or layered onto said inner wall microencapsular enteric coating.
Claim 7
Dependent Claim
38 words
The sustained-release pharmaceutical preparation of claim 5 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 8
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 9
Dependent Claim
50 words
The sustained-release pharmaceutical preparation of claim 7 further including a solid acid layer 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 incorporated in or layered onto said inner wall enteric coating.
Claim 10
Dependent Claim
21 words
The sustained-release pharmaceutical preparation of claim 8 wherein said admixture consists of about 15% uncoated drug, and 85% multi-walled coated medicament.
Claim 11
Dependent Claim
110 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 phthalate, hydroxypropyl methyl cellulose phthalate, hydroxethyl ethyl cellulose phthalate, cellulose acetate tetrahydroxphthalate acrylic resin, and cellulose acetate trimellitate. c) an acid 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 incorporated in or layered onto said inner wall microencapsular enteric coating. d) an outer wall microencapsular control coating selected from the group consisting of methacrylic acid ester copolymer and ethyl cellulose.
Claim 12
Dependent Claim
110 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 phthalate, hydroxypropyl methyl cellulose phthalate, hydroxethyl ethyl cellulose phthalate, cellulose acetate tetrahydroxphthalate acrylic resin, and cellulose acetate trimellitate. c) an acid 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 incorporated in or layered onto said inner wall microencapsular enteric coating. d) an outer wall microencapsular control coating selected from the group consisting of methacrylic acid ester copolymer and ethyl cellulose.
Claim 13
Dependent Claim
29 words
The multi-walled coated medicament of claim 10 wherein said core drug is selected from the group consisting of aspirin, acetaminophen, indomethacin, propranolol hydrochloride, dextromethorphan hydrobromide, disopyramide phosphate and furosemide.
Claim 14
Dependent Claim
19 words
The multi-walled coated medicament of claim 11 wherein said inner wall enteric coating is a polymethacrylic acid/acrylic acid copolymer.
Claim 15
Dependent Claim
15 words
The multi-walled coated medicament of claim 12 wherein said acid layer coating is citric acid.
Claim 16
Dependent Claim
20 words
The multi-walled coated medicament of claim 13 wherein said outer wall microencapsular control coating is a methacrylic acid ester copolymer.
Claim 17
Dependent Claim
13 words
The multi-walled coated medicament of claim 14 wherein said core drug is indomethacin.
Claim 18
Dependent Claim
44 words
The multi-walled coated medicament of claim 15 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 19
Dependent Claim
22 words
The multi-walled coated medicament of claim 10 wherein a second said water-soluble drug layer is outside said outer wall microencapsular control coating.
Claim 20
Dependent Claim
23 words
The multi-walled coated medicament of claim 17 wherein a second said outer wall microencapsulated control coating is outside said second water-soluble drug layer.
Claim 21
Dependent Claim
26 words
The multi-walled coated medicament of claim 10 wherein a second said water-soluble drug layer is between an acid layer and said outer wall microencapsulated control coating.
Claim 22
Dependent Claim
28 words
The multi-walled coated medicament of claim 10 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)
No citation records indexed.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.