US4867987A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical product for the sustained release of ibuprofen
Assignee: Mepha GmbH
•
Filing: 1986-12-19
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Granted: 1989-09-19
•
Expires: 2006-12-19
Abstract
Abstract The product consists of tablets which contain at least 600 mg of ibuprofen and a binder, or a mixture of binders, based on cellulose and cellulose derivatives in the form of microspheres which are coated with an acrylic resin of defined nature and are compressed together with a disintegrant; the tablets are preferably also coated with a lacquer layer. As a consequence of the high content of active compound and its delayed release in the body, the therapeutic treatment with ibuprofen can be reduced to a minimum number of intakes and dose units per day.
Inventors
- 👤 Pyare L. Seth
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 22:26
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K31/00; A61K31/185; A61K31/19; A61K9/20; A61K9/2072; A61K9/2077; A61K9/2081; A61P; A61P25/00; A61P25/04; A61P29/00
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
174 words
A pharmaceutical product for the sustained release of ibuprofen in the body, in the form of tablets which contain the active compound in microspheres, disintegrate fast in an aqueous medium, and have the following composition: (a) ibuprofen in an amount of at least 600 mg and (b) a binder, or a mixture of binders, based on cellulose and cellulose derivatives, all of which are in the form of a homogenous mixture and in the form of microspheres which, in turn, are coated with a layer of (c) an acrylic resin of neutral character and average molecular weight of around 800,000, composed of copolymers of acrylic and methacrylic esters of the partial formula: ##STR2## in which each of R and R' denotes hydrogen or methyl, and each of r" and R'" denotes methyl or ethyl, and the coated microspheres are homogeneously mixed with (d) a disintegrant, or a mixture of disintegrants in an amount which makes up only 10 to 15% of the whole weight, and the resulting homogenous mixture is compressed to form tablets.
Claim 2
Dependent Claim
174 words
A pharmaceutical product for the sustained release of ibuprofen in the body, in the form of tablets which contain the active compound in microspheres, disintegrate fast in an aqueous medium, and have the following composition: (a) ibuprofen in an amount of at least 600 mg and (b) a binder, or a mixture of binders, based on cellulose and cellulose derivatives, all of which are in the form of a homogenous mixture and in the form of microspheres which, in turn, are coated with a layer of (c) an acrylic resin of neutral character and average molecular weight of around 800,000, composed of copolymers of acrylic and methacrylic esters of the partial formula: ##STR2## in which each of R and R' denotes hydrogen or methyl, and each of r" and R'" denotes methyl or ethyl, and the coated microspheres are homogeneously mixed with (d) a disintegrant, or a mixture of disintegrants in an amount which makes up only 10 to 15% of the whole weight, and the resulting homogenous mixture is compressed to form tablets.
Claim 3
Dependent Claim
16 words
The product as claimed in claim 1, wherein the tablets are coated with a lacquer layer.
Claim 4
Dependent Claim
17 words
The product as claimed in claim 1, which contains 600 to 1200 mg of ibuprofen per tablet.
Claim 5
Dependent Claim
18 words
The product as claimed in claim 1, wherein the binder contains microcrystalline cellulose and a water-soluble cellulose derivative.
Claim 6
Dependent Claim
18 words
The product as claimed in claim 1, wherein the acrylic resin is composed of Edragit® E 30 D.
Claim 7
Dependent Claim
25 words
The product as claimed in claim 1, wherein the disintegrant is cellulose, starch, a starch ether, a pectin or a swelling agent of similar action.
Claim 8
Dependent Claim
131 words
A process for the preparation of the pharmaceutical product as claimed in claim 1, which comprises mixing together the ibuprofen and the binder, or the mixture of binders, based on cellulose and cellulose derivatives to give a homogeneous mixture and moistening with water, shaping the mixture into microspheres by extrusion, drying the microspheres, coating with an aqueous dispersion of an acrylic resin of neutral character and average molecular weight of around 800,000, composed of copolymers of acrylic and methacrylic esters of the part-formula: ##STR3## in which each of R and R' denotes hydrogen or methyl, and each of R" and R'" denotes methyl or ethyl, and drying, mixing the coated microspheres with the disintegrant, or the mixture of disintegrants, to give a homogeneous mixture, and compressing the mixture to form tablets.
Claim 9
Dependent Claim
18 words
The process as claimed in claim 7, wherein the resulting tablets are additionally coated with a lacquer layer.
Claim 10
Dependent Claim
21 words
The process as claimed in claim 7, wherein ibuprofen is used in an amount of 600 to 1200 mg per tablet.
Claim 11
Dependent Claim
17 words
The process as claimed in claim 7, wherein Eudragit® E 30 D is used as acrylic resin.
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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) | 1992-09-18 | 1993-03-20 | 1993-09-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-09-18 | 1997-03-20 | 1997-09-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-09-18 | 2001-03-20 | 2001-09-19 | $7700.00 | Window Closed / Lapsed |