US4524060A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Slow release pharmaceutical composition
Assignee: John Wyeth and Brother Ltd
•
Filing: 1983-10-28
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Granted: 1985-06-18
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Expires: 2003-10-28
Abstract
Abstract The invention provides a sustained release pharmaceutical composition comprising a mixture of micronized indoramin or a pharmaceutically acceptable salt thereof, a water-channelling agent, a wetting agent and a disintegrant, the mixture being in the form of a non-compressed pellet and having an enteric coat or a sustained release coat permeable to gastrointestinal juices. Sustained release capsules are also provided comprising a plurality of the aforementioned pellets.
Inventors
- 👤 Ahmed S. Mughal
- 👤 David S. Holmes
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 01:11
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5073; A61K9/5078; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61P; A61P9/00; A61P9/12
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
161 words
A pharmaceutical composition in capsule form comprising a plurality of sustained release pellets each containing about 50 to 90% by weight of a mixture of micronised indoramin or a pharmaceutically acceptable salt thereof, about 4 to 25% by weight of microcrystalline cellulose as a hydrophilic long chain polymer, about 0.5 to 10% by weight of a wetting agent and about 1 to 10% by weight of a disintegrant other than microcrystalline cellulose, the mixture being in the form of a non-compressed pellet and having an enteric coat or a sustained release coat permeable to gastro-intestinal juices, the indoramin having a particle size where 90% of the particles are less than or equal to 15μ, the ratio of indoramin to hydrophilic long chain polymer being about 30:1 to about 2:1 and the ratio of indoramin to wetting agent being about 300:1 to about 5:1 so as to allow at least about 80% release of indoramin into gastro-intestinal media within about 24 hours.
Claim 2
Dependent Claim
161 words
A pharmaceutical composition in capsule form comprising a plurality of sustained release pellets each containing about 50 to 90% by weight of a mixture of micronised indoramin or a pharmaceutically acceptable salt thereof, about 4 to 25% by weight of microcrystalline cellulose as a hydrophilic long chain polymer, about 0.5 to 10% by weight of a wetting agent and about 1 to 10% by weight of a disintegrant other than microcrystalline cellulose, the mixture being in the form of a non-compressed pellet and having an enteric coat or a sustained release coat permeable to gastro-intestinal juices, the indoramin having a particle size where 90% of the particles are less than or equal to 15μ, the ratio of indoramin to hydrophilic long chain polymer being about 30:1 to about 2:1 and the ratio of indoramin to wetting agent being about 300:1 to about 5:1 so as to allow at least about 80% release of indoramin into gastro-intestinal media within about 24 hours.
Claim 3
Dependent Claim
31 words
A composition as claimed in claim 1 in which the ratio of micronised indoramin or pharmaceutically acceptable salt thereof to hydrophilic long chain polymer is from about 10:1 to about 3:1.
Claim 4
Dependent Claim
28 words
A composition as claimed in claim 1 in which the ratio of micronised indoramin or pharmaceutially acceptable salt thereof to wetting agent is from about 150:1 to 30:1.
Claim 5
Dependent Claim
16 words
A composition as claimed in claim 1 wherein 90% of the particles are 5μ or less.
Claim 6
Dependent Claim
27 words
A composition as claimed in claim 1 in which the indoramin or pharmaceutically acceptable salt thereof comprises about 75 to about 90% by weight of the mixture.
Claim 7
Dependent Claim
23 words
A composition as claimed in claim 1 in which the wetting agent comprises from about 0.5 to 3% by weight of the mixture.
Claim 8
Dependent Claim
22 words
A compound as claimed in claim 1 in which the microcrystalline cellulose comprises about 4 to 20% by weight of the mixture.
Claim 9
Dependent Claim
38 words
A composition as claimed in claim 1 in which the wetting agent is a sodium alkyl sulphate, sodium laurate, dioctyl sodium sulphosuccinate, sodium stearate, potassium stearate, sodium oleate, polyethylene glycol, a polyoxyethylene ester, benzalkonium chloride or bis-2-hydroxyethyl oleylamine.
Claim 10
Dependent Claim
26 words
A composition as claimed in claim 1 in which the pellet is prepared by applying the mixture in layers, bound by adhesive, to an inert core.
Claim 11
Dependent Claim
23 words
A composition as claimed in claim 9 in which the inert core is a non-pareil seed of from about 500 to 840μ diameter.
Claim 12
Dependent Claim
131 words
A sustained release pharmaceutical composition in accordance with claim 1 comprising a capsule containing a plurality of pellets, each pellet formed by applying an intimate mixture comprising aboout 50 to 90% by weight of micronised indoramin hydrochloride in which 90% of the particles have a particle size ≦5μ, about 4 to 25% by weight of microcrystalline cellulose, about 1 to 10% by weight of a disintegrant other than microcrystalline cellulose and about 0.5 to 10% by weight of a wetting agent in layers bound by adhesive to an inert core; said pellet having a sustained release or enteric coat applied as a film, the ratios of indoramin hydrochloride to microcrystalline cellulose and wetting agent being in the range from about 10:1 to about 3:1 and about 150:1 to about 30:1, respectively.
Claim 13
Dependent Claim
21 words
A composition as claimed in claim 1 in which the disintegrant is about 2 to 8% by weight of the mixture.
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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) | 1988-06-17 | 1988-12-17 | 1989-06-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-06-17 | 1992-12-17 | 1993-06-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-06-17 | 1996-12-17 | 1997-06-18 | $7700.00 | Window Closed / Lapsed |