US5084278A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Taste-masked pharmaceutical compositions
Assignee: NORTEC DEVELOPMENT ASSOCIATES Inc (NORTEC) A CORP OF NEW JERSEY
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Filing: 1989-06-02
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Granted: 1992-01-28
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Expires: 2009-06-02
Abstract
Abstract In accordance with the present invention, these and other objects are achieved by a pharmaceutical composition comprised of 1) a pharmaceutical core which is further comprised of a pharmaceutically active dose of a compound and, 2) a microencapsulating polymer which coats the pharmaceutical core and is capable of taste-masking the active compound. The polymer coating maintains its integrity, i.e., does not fracture and release active when tabletted and/or chewed, and can provide immediate release of the active compound in the stomach, or alternatively, in certain embodiments, can release the active agent in the upper intestinal tract or in sustained release fashion. Additionally, the polymeric coating compositions or the pharmaceutical core may contain diluents, fillers, bulking agents, and plasticizers. The polymeric coatings may also contain pigments and opacifiers to promote compliance and enhance the storage stability of light sensitive active agents.
Inventors
- 👤 Atul M. Mehta
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 07:06
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2072; A61K9/2077; A61K9/2081; A61K9/0012; A61K9/0053; A61K9/0056; A61K9/48; A61K9/50; A61K9/5005; A61K9/5021; A61K9/5026; A61K9/5036; A61K9/5042; A61K9/5047
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
120 words
A chewable taste-masked pharmaceutical composition having controlled release characteristics, comprising: (a) a microcapsule of about 10 microns to about 1.5 mm in diameter having a core including a pharmaceutically active agent and a polymer mixture coating having sufficient elasticity to withstand chewing; (b) said polymeric mixture comprising (i) about 50% by weight ethyl cellulose that forms a polymeric film at temperatures of at least about 30° C.; and (ii) about 50% by weight of a low temperature film forming copolymer selected from the group consisting of methacrylic acid ester copolymers and styrene acrylate copolymers that form a polymeric film at temperatures less than about 25° C.; and said coating being adapted to release said pharmaceutically active agent in the stomach.
Claim 2
Dependent Claim
120 words
A chewable taste-masked pharmaceutical composition having controlled release characteristics, comprising: (a) a microcapsule of about 10 microns to about 1.5 mm in diameter having a core including a pharmaceutically active agent and a polymer mixture coating having sufficient elasticity to withstand chewing; (b) said polymeric mixture comprising (i) about 50% by weight ethyl cellulose that forms a polymeric film at temperatures of at least about 30° C.; and (ii) about 50% by weight of a low temperature film forming copolymer selected from the group consisting of methacrylic acid ester copolymers and styrene acrylate copolymers that form a polymeric film at temperatures less than about 25° C.; and said coating being adapted to release said pharmaceutically active agent in the stomach.
Claim 3
Dependent Claim
27 words
The composition according to claim 1 wherein the low temperature film forming polymer comprises a polymethacrylic acid ester copolymer having a mean molecular weight of about 800,000.
Claim 4
Dependent Claim
13 words
The composition according to claim 1, wherein said core further comprises a diluent.
Claim 5
Dependent Claim
14 words
The composition according to claim 1, wherein said polymer coating further comprises a plasticizer.
Claim 6
Dependent Claim
27 words
The composition according to claim 3, wherein said plasticizer is selected from the group consisting of polyethylene glycol, triacetin, vinylpyrrolidone, diethyl phthallate, dibutylsebacate, and citric acid esters.
Claim 7
Dependent Claim
33 words
The composition according to claim 1, wherein said pharmaceutically active agent is selected from the group consisting of erythromycin, penicillin, ampicillin, acetaminophen, ibuprofen, dextromethorphan, cimetidine, pseudoephedrine, diphenhydramine, spironolactone, chlorpheniramine, theophylline, phenylbutazone and ranitidine.
Claim 8
Dependent Claim
16 words
The composition according to claim 5 wherein the high temperature film forming copolymer is water soluble.
Claim 9
Dependent Claim
48 words
A chewable taste-masked pharmaceutical composition according to claim 1, wherein the polymeric mixture comprises about 70% by weight ethyl cellulose polymer aqueous dispersion and about 30% by weight of said low temperature film forming polymer, said coating being adapted to release said pharmaceutically active agent in the stomach.
Claim 10
Dependent Claim
106 words
A chewable taste-masked pharmaceutical composition having rapid release characteristics in the upper intestinal tract, comprising: (a) a microcapsule of about 10 microns to about 1.5 mm in diameter having a core including a pharmaceutically active agent and a polymer mixture coating having sufficient elasticity to withstand chewing; (b) said polymeric mixture comprising (i) at least about 50% by weight of a high temperature film forming copolymer comprising an aqueous ethyl cellulose polymer dispersion, that forms a polymeric film at temperatures of at least about 30° C.; and (ii) a low temperature film forming polymer that forms a polymeric film at temperatures less than about 25° C.
Claim 11
Dependent Claim
106 words
A chewable taste-masked pharmaceutical composition having rapid release characteristics in the upper intestinal tract, comprising: (a) a microcapsule of about 10 microns to about 1.5 mm in diameter having a core including a pharmaceutically active agent and a polymer mixture coating having sufficient elasticity to withstand chewing; (b) said polymeric mixture comprising (i) at least about 50% by weight of a high temperature film forming copolymer comprising an aqueous ethyl cellulose polymer dispersion, that forms a polymeric film at temperatures of at least about 30° C.; and (ii) a low temperature film forming polymer that forms a polymeric film at temperatures less than about 25° C.
Claim 12
Dependent Claim
48 words
A chewable taste-masked pharmaceutical composition according to claim 9 wherein the polymeric mixture comprises about 50% by weight ethyl cellulose polymer aqueous dispersion and about 50% by weight of said low temperature film forming polymer, said coating being adapted to release said pharmaceutically active agent in the stomach.
Claim 13
Dependent Claim
27 words
The composition according to claim 9 wherein the low temperature film forming polymer comprises a polymethacrylic acid ester copolymer having a mean molecular weight of about 800,000.
Claim 14
Dependent Claim
13 words
The composition according to claim 9, wherein said core further comprises a diluent.
Claim 15
Dependent Claim
14 words
The composition according to claim 9, wherein said polymer coating further comprises a plasticizer.
Claim 16
Dependent Claim
27 words
The composition according to claim 12, wherein said plasticizer is selected from the group consisting of polyethylene glycol, triacetin, vinylpyrrolidone, diethyl phthallate, dibutylsebacate, and citric acid esters.
Claim 17
Dependent Claim
33 words
The composition according to claim 9, wherein said pharmaceutically active agent is selected from the group consisting of erythromycin, penicillin, ampicillin, acetaminophen, ibuprofen, dextromethorphan, cimetidine, pseudoephedrine, diphenhydramine, spironolactone, chlorpheniramine, theophylline, phenylbutazone and ranitidine.
Claim 18
Dependent Claim
22 words
The composition according to claim 9, wherein the coating provides immediate release in the stomach of the active agent in the core.
Claim 19
Dependent Claim
48 words
A chewable taste-masked pharmaceutical composition according to claim 9, wherein the polymeric mixture comprises about 70% by weight ethyl cellulose polymer aqueous dispersion and about 30% by weight of said low temperature film forming polymer, said coating being adapted to release said pharmaceutically active agent in the stomach.
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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) | 1995-01-27 | 1995-07-29 | 1996-01-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-01-27 | 1999-07-29 | 2000-01-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-01-27 | 2003-07-29 | 2004-01-28 | $7700.00 | Window Closed / Lapsed |