Patent US4994276A successfully refreshed from Google Patents.
US4994276A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Directly compressible sustained release excipient
Assignee: Penwest Pharmaceuticals Co
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Filing: 1988-09-19
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Granted: 1991-02-19
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Expires: 2008-09-19
Abstract
Abstract A free-flowing directly compressible granulation useful as a slow release pharmaceutical excipient is disclosed. The excipient includes a hydrodrophilic matrix which includes a heteropolysaccharide and a polysaccharide material capable of cross-linking the heteropolysaccharide, and an inert diluent.
Inventors
- 👤 Anand R. Baichwal
- 👤 John N. Staniforth
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 22:23
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/205; A61K9/2013; A61K9/2018
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
94 words
A free-flowing, directly compressible slow release granulation for use as a pharmaceutical excipient, comprising from about 20 to about 60 percent by weight of a hydrophilic material comprising a heteropolysaccharide and a polysaccharide gum capable of cross-linking said heteropolysaccharide in the presence of aqueous solutions, and from about 40 to about 80 percent by weight of an inert pharmaceutical filler selected from the group consisting of a monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert pharmaceutical filler to said hydrophilic material being from about 4:1 to about 0.67:1.
Claim 2
Dependent Claim
94 words
A free-flowing, directly compressible slow release granulation for use as a pharmaceutical excipient, comprising from about 20 to about 60 percent by weight of a hydrophilic material comprising a heteropolysaccharide and a polysaccharide gum capable of cross-linking said heteropolysaccharide in the presence of aqueous solutions, and from about 40 to about 80 percent by weight of an inert pharmaceutical filler selected from the group consisting of a monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert pharmaceutical filler to said hydrophilic material being from about 4:1 to about 0.67:1.
Claim 3
Dependent Claim
12 words
The granulation of claim 1, wherein said polysaccharide gum comprises a galactomannan.
Claim 4
Dependent Claim
36 words
The granulation of claim 1, wherein said heteropolysaccharide comprises from about 10 to about 90 percent by weight and said polysaccharide gum comprises from about 90 to about 10 percent by weight, of said hydrophilic material.
Claim 5
Dependent Claim
18 words
The granulation of claim 3, wherein the ratio of said heteropolysaccharide to said polysaccharide gum is about 1:1.
Claim 6
Dependent Claim
14 words
The granulation of claim 3, wherein said heteropolysaccharide comprises xanthan gum or derivatives thereof.
Claim 7
Dependent Claim
12 words
The granulation of claim 5, wherein said polysaccharide gum comprises a galactomannan.
Claim 8
Dependent Claim
12 words
The granulation of claim 6, wherein said galactomannan comprises locust bean gum.
Claim 9
Dependent Claim
44 words
The granulation according to claim 1 wherein a medicament is added and the resulting mixture provides a zero order controlled release when provided as a solid dosage form, the ratio of said medicament to said hydrophilic material being from about 1:3 to about 1:7.
Claim 10
Dependent Claim
22 words
The granulation of claim 7, wherein said inert pharmaceutical filler comprises lactose, dextrose, sucrose, fructose, microcrystalline cellulose, xylitol, sorbitol or mixtures thereof.
Claim 11
Dependent Claim
27 words
The granulation of claim 9 to which a medicament is added, the ratio of said medicament to said hydrophilic material being from about 1:3 to about 1:7.
Claim 12
Dependent Claim
36 words
The granulation of claim 9, wherein a medicament is added and the resultant mixture is compressed to form solid tablets, the ratio of said medicament to said hydrophilic material being from about 1:3 to about 1:7.
Claim 13
Dependent Claim
19 words
The granulation of claim 11, wherein at least 3.5 hours are required to release 50 percent of said medicament.
Claim 14
Dependent Claim
21 words
The granulation of claim 10, wherein the average particle size of said granules is from about 185 to about 250 microns.
Claim 15
Dependent Claim
16 words
The granulation according to claim 3, wherein said hydrophilic material further comprises a second polysaccharide gum.
Claim 16
Dependent Claim
44 words
The granulation according to claim 14, wherein said second polysaccharide gum is selected from the group consisting of tragacanth, accacia, karaya, alginates, agar, pectin, guar, hydroxypropyl guar, carrageenan, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methylcellulose, carboxymethyl cellulose, polyvinyl pyrollidone, and mixtures of any of the foregoing.
Claim 17
Dependent Claim
15 words
The granulation according to claim 14, wherein said second polysaccharide gum comprises propylene glycol alginate.
Claim 18
Dependent Claim
27 words
The granulation according to claim 14, wherein said second polysaccharide gum comprises a hydrocolloid, said hydrocolloid comprising up to about 50% by weight of said hydrophilic material.
Claim 19
Dependent Claim
33 words
The granulation according to claim 1, wherein a medicament is added and the resulting mixture is encapsulated, the ration of said medicament to said hydrophilic material being from about 1:3 to about 1:7.
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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) | 1994-02-18 | 1994-08-20 | 1995-02-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-02-18 | 1998-08-20 | 1999-02-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-02-18 | 2002-08-20 | 2003-02-19 | $7700.00 | Window Closed / Lapsed |