US4892730A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Processes for preparation of solid, rapidly released medicament preparations containing dihydropyridines
Assignee: Bayer AG
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Filing: 1988-09-20
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Granted: 1990-01-09
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Expires: 2008-09-20
Abstract
Abstract Solid dihydropyridines, e.g. nifedipine and nimodipine preparations having a maximum standard deviation of the active compound content of 3% contain 1 part by weight of nifedipine, 2 to 6 parts by weight of PVP with a mean molecular weight of 15,000 to 50,000, 3.5 to 15 parts by weight of cellulose, 0.25 to 4 parts by weight of starch and 0.5 to 4 parts by weight of cross-linked insoluble PVPP, and, if appropriate, one or more further pharmaceutical auxiliaries and excipients. These preparations show a good release of dihydropyridine with good content uniformity.
Inventors
- 👤 Ahmed Hegasy
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 02:01
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K9/00; A61K9/14; A61K9/141; A61K9/146; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1652; A61K9/20; A61K9/2072; A61K9/2077
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
119 words
A process for the production of a solid medicament preparation, which process comprises dissolving 1 part by weight of dihydropyridine as active compound and 2.0 to 6.0 parts by weight of PVP having a mean molecular weight of 15,000 to 50,000, in 2 to 20 parts by weight of an amount of an organic solvent which is sufficient to dissolve the dihydropyridine and PVP, then granulating this resultant solution with 4 to 23 parts by weight of absorptive excipients comprising a mixture of 3.5 to 15 parts by weight cellulose, 0.25 to 4 parts by weight starch and 0.25 to 4 parts by weight crosslinked insoluble PVPP, then further processing the resulting granules to give the solid medicament preparation.
Claim 2
Dependent Claim
119 words
A process for the production of a solid medicament preparation, which process comprises dissolving 1 part by weight of dihydropyridine as active compound and 2.0 to 6.0 parts by weight of PVP having a mean molecular weight of 15,000 to 50,000, in 2 to 20 parts by weight of an amount of an organic solvent which is sufficient to dissolve the dihydropyridine and PVP, then granulating this resultant solution with 4 to 23 parts by weight of absorptive excipients comprising a mixture of 3.5 to 15 parts by weight cellulose, 0.25 to 4 parts by weight starch and 0.25 to 4 parts by weight crosslinked insoluble PVPP, then further processing the resulting granules to give the solid medicament preparation.
Claim 3
Dependent Claim
21 words
A process according to claim 1, in which 5.25 to 17 parts by weight of the said absorptive excipients are employed.
Claim 4
Dependent Claim
24 words
A process according to claim 1, in which the organic solvent is selected from ethanol, acetone, methylene chloride, chloroform, and mixtures of these solvents.
Claim 5
Dependent Claim
26 words
A process according to claim 1, which further comprises conducting the further processing of the resulting granules in the presence of further formulation auxiliaries and/or excipients.
Claim 6
Dependent Claim
28 words
A process according to claim 4, wherein the further formulation auxiliaries and/or excipients are selected form the group consisting of lactose, powdered sugar, mannitol, glycocoll and calcium carbonate.
Claim 7
Dependent Claim
19 words
A process according to claim 1, wherein the dihydropyridine is selected from the group consisting of nifedipine and nimodipine.
Claim 8
Dependent Claim
17 words
A process according to claim 1, wherein said dihydropyridine has a maximum relative standard deviation of 1.413%.
Claim 9
Dependent Claim
19 words
A process according to claim 1, wherein the active compound has a mean standard deviation of at most 2.5%.
Claim 10
Dependent Claim
17 words
A process according to claim 1, wherein the active compound is released in less than 30 minutes.
Claim 11
Dependent Claim
42 words
A process according to claim 1, wherein the absorptive excipients comprise a powder mixture of 4 to 12 parts by weight of cellulose, 0.25 to 2.0 parts by weight of starch and 1 to 3 parts by weight of crosslinked insoluble PVPP.
Claim 12
Dependent Claim
11 words
A process according to claim 1, wherein said dihydropyridine is nifedipine.
Claim 13
Dependent Claim
11 words
A process according to claim 1, wherein said dihydropyridine is nimodipine.
References Cited (Backward Citations)
US4412986A
Cited
US4216155A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-01-08 | 1993-07-10 | 1994-01-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-01-08 | 1997-07-10 | 1998-01-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-01-08 | 2001-07-10 | 2002-01-09 | $7700.00 | Window Closed / Lapsed |