US4499066A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pharmaceutical sustained-release compositions
Assignee: Pfizer Italia SRL
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Filing: 1982-07-30
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Granted: 1985-02-12
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Expires: 2002-07-30
Abstract
Abstract New pharmaceutical sustained-release compositions, formulated as tablets, are prepared by mixing the active ingredient with excipient already granulated and coated with polymers and/or copolymers or a polymers- and/or copolymers-mixture substantially insoluble in water. Such pharmaceutical preparations enable one to enhance or to decrease very easily and precisely the sustained-release effect by regulating the granulometry of the excipient, the excipient/active ingredient ratio, the hardness, and the percentage of the polymers and/or copolymers or of the polymers- and/or copolymers-mixture.
Inventors
- 👤 Luigi Moro
- 👤 Grazia Maffione
- 👤 Guido Neri
- 👤 Alessandro Rigamonti
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 09:14
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/2027
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
102 words
A process for preparing a pharmaceutical sustained-release composition formulated as tablets, comprising: coating particles of an excipient selected from the group consisting of starch, lactose, mannitol, saccarose, glucose, and sorbitol with a polymeric material selected from the group consisting of acrylate polymers and methacrylate polymers and copolymers to form coated granules of the excipient, said polymeric material being substantially insoluble or sparingly soluble in aqueous medium; mixing an uncoated active ingredient with the coated granules of the excipient and compressing the mixture to form tablets having a hardness in the range of from at least 5 kg to less than 20 kg.
Claim 2
Dependent Claim
102 words
A process for preparing a pharmaceutical sustained-release composition formulated as tablets, comprising: coating particles of an excipient selected from the group consisting of starch, lactose, mannitol, saccarose, glucose, and sorbitol with a polymeric material selected from the group consisting of acrylate polymers and methacrylate polymers and copolymers to form coated granules of the excipient, said polymeric material being substantially insoluble or sparingly soluble in aqueous medium; mixing an uncoated active ingredient with the coated granules of the excipient and compressing the mixture to form tablets having a hardness in the range of from at least 5 kg to less than 20 kg.
Claim 3
Dependent Claim
109 words
A pharmaceutical sustained-release composition formulated as tablets having a hardness in the range of from about 5 kg to less than 20 kg prepared by the process of claim 1, said composition comprising an uncoated active ingredient admixed with a granulated excipient selected from the group consisting of starch, lactose, mannitol, saccarose, glucose and sorbitol that has been previously coated with 0.5 to 50% by weight based on the weight of the excipient of a polymeric material selected from the group consisting of acrylate polymers and methacrylate polymers and copolymers, the ratio by weight of the excipient to the active ingredient being in the range of 0.5 to 25.
Claim 4
Dependent Claim
22 words
The composition of claim 2, wherein the excipient is coated with 1 to 10% or more by weight of the polymeric material.
Claim 5
Dependent Claim
26 words
The composition of claim 2, wherein the ratio by weight of the coated excipient to the active ingredient is in the range of 1 to 10.
Claim 6
Dependent Claim
22 words
The composition of claim 2, wherein the particle size of the excipient is in the range of 0.150 mm to 0.685 mm.
Claim 7
Dependent Claim
21 words
The composition of claim 5, wherein the particle size of the excipient is in the range of 0.220 to 0.380 mm.
Claim 8
Dependent Claim
58 words
The composition of claim 2, wherein the particle size of the excipient is in the range of 0.220 to 0.380 mm, the excipient is coated with 1 to 10% or more by weight of the polymeric material, and the ratio by weight of the coated excipient to the active ingredient is in the range of 1 to 10.
Claim 9
Dependent Claim
17 words
A pharmaceutical composition as defined in claim 2, characterized in that the polymeric material comprises methylacrylate/methylmethacrylate copolymer.
Claim 10
Dependent Claim
16 words
A process as defined in claim 1, characterized in that the polymeric material comprises methylacrylate/methylmethacrylate copolymer.
Claim 11
Dependent Claim
30 words
A pharmaceutical composition as defined in any one of claims 8 and 2 to 7, characterized in that the tablets do not disintegrate, but nevertheless allow substantially total drug release.
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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) | 1988-02-12 | 1988-08-13 | 1989-02-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-02-12 | 1992-08-13 | 1993-02-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-02-12 | 1996-08-13 | 1997-02-12 | $7700.00 | Window Closed / Lapsed |