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US4665081A
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Solid nifedipine preparations and a process for preparing same
Assignee: Takada Seiyaku KK
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Filing: 1984-05-25
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Granted: 1987-05-12
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Expires: 2004-05-25
Abstract
Abstract A new solid nifedipine preparation which comprises (a) a particulate dry composition having been obtained by subjecting nifedipine in mixture with casein and one or more inorganic excipients to co-pulverization or (b) a particulate dry composition having been obtained by adding an enteric high molecular substance and a plasticizer optionally with a higher fatty acid ester to the co-pulverized mixture obtained above, subjecting the mixture to co-pulverization and then dry-processing the co-pulverized product to a pharmaceutically acceptable solid form, as well as a process for preparing the solid nifedipine preparation comprising a particulate dry composition (a) or (b) by the specific co-pulverization and a dry compounding method. The solid nifedipine preparation is excellent in dissolution of nifedipine or possesses a controlled dissolution rate of nifedipine. This preparation is useful as a vasodilating medicament for the dual purposes of rapid and gradual release of nifedipine from the preparation for the remedy of angina pectoris or hypertension.
Inventors
- 👤 Kengo Doi
- 👤 Shinichi Nitta
- 👤 Masaki Kusakari
- 👤 Nobuhiko Takahashi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 03:01
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/141; A61K9/143; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K9/146; A61K9/16; A61K9/1605; A61K9/1611; A61K9/1629; A61K9/1658; A61P; A61P9/00; A61P9/08; A61P9/10
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
76 words
A solid nifedipine preparation which comprises a particulate dry composition containing an effective vasodilating or hypotensive amount of nifedipine obtained by the process comprising subjecting nifedipine in mixture with casein and one or more inorganic excipients to co-pulverization in the absence of any liquid vehicle, said inorganic excipient being a member selected from the group consisting of magnesium silicate, magnesium carbonate, dried aluminum hydroxide gel, magnesium oxide, magnesium aluminate metasilicate, synthetic hydrotalcite and magnesium aluminum hydroxide.
Claim 2
Dependent Claim
76 words
A solid nifedipine preparation which comprises a particulate dry composition containing an effective vasodilating or hypotensive amount of nifedipine obtained by the process comprising subjecting nifedipine in mixture with casein and one or more inorganic excipients to co-pulverization in the absence of any liquid vehicle, said inorganic excipient being a member selected from the group consisting of magnesium silicate, magnesium carbonate, dried aluminum hydroxide gel, magnesium oxide, magnesium aluminate metasilicate, synthetic hydrotalcite and magnesium aluminum hydroxide.
Claim 3
Dependent Claim
34 words
A solid nifedipine preparation according to claim 1, wherein at least 0.5 parts by weight of casein and 0.2-9 parts by weight of said inorganic excipient are used per part by weight of nifedipine.
Claim 4
Dependent Claim
32 words
A solid nifedipine preparation according to claim 1, wherein 1.5-20 parts by weight of casein and 0.3-5 parts by weight of the inorganic excipients are used per part by weight of nifedipine.
Claim 5
Dependent Claim
31 words
A solid nifedipine preparation according to claim 1, wherein one or more water-soluble saccharides are added in an amount up to 6 parts by weight per part by weight of nifedipine.
Claim 6
Dependent Claim
29 words
A solid nifedipine preparation according to claim 4, wherein said saccharide is a member selected from the group consisting of glucose, fructose, mannitol, sorbitol, xylitol, maltose, lactose and sucrose.
Claim 7
Dependent Claim
28 words
A solid nifedipine preparation according to claim 5, wherein the pharmaceutically acceptable solid form is a member selected from the group consisting of granules, tablets, dragees and capsules.
Claim 8
Dependent Claim
114 words
A solid nifedipine preparation which comprises a particulate dry composition obtained by the process comprising subjecting nifedipine in mixture with casein and one or more inorganic excipients to co-pulverization in the absence of any liquid vehicle, said inorganic excipient being a member selected from the group consisting of magnesium silicate, magnesium carbonate, dried aluminum hydroxide gel, magnesium oxide, magnesium aluminate metasilicate, synthetic hydrotalcite and magnesium aluminum hydroxide, adding an enteric high molecular substance and a plasticizer optionally with a higher fatty acid ester to the resultant co-pulverized mixture, subjecting the mixture to co-pulverization and then dry-processing the co-pulverized product to a pharmaceutically acceptable solid form containing an effective vasodilating or hypotensive amount of nifedipine.
Claim 9
Dependent Claim
114 words
A solid nifedipine preparation which comprises a particulate dry composition obtained by the process comprising subjecting nifedipine in mixture with casein and one or more inorganic excipients to co-pulverization in the absence of any liquid vehicle, said inorganic excipient being a member selected from the group consisting of magnesium silicate, magnesium carbonate, dried aluminum hydroxide gel, magnesium oxide, magnesium aluminate metasilicate, synthetic hydrotalcite and magnesium aluminum hydroxide, adding an enteric high molecular substance and a plasticizer optionally with a higher fatty acid ester to the resultant co-pulverized mixture, subjecting the mixture to co-pulverization and then dry-processing the co-pulverized product to a pharmaceutically acceptable solid form containing an effective vasodilating or hypotensive amount of nifedipine.
Claim 10
Dependent Claim
41 words
A solid nifedipine preparation according to claim 7, wherein the enteric high molecular substance is a member selected from the group consisting of cellulose acetate phthalate, hydroxypropylmethylcellulose phthalate, methyl methacrylate copolymer, polyvinyl acetate phthalate, cellulose acetate succinate and styrene-maleric acid copolymer.
Claim 11
Dependent Claim
36 words
A solid nifedipine preparation according to claim 7, wherein the plasticizer is a member selected from the group consisting of polyethylene glycol normally solid at room temperature, triacetin, polyoxyethylene sorbitan monooleate and propylene glycol acetylated monoglyceride.
Claim 12
Dependent Claim
62 words
A solid nifedipine preparation according to claim 7, wherein the higher fatty acid ester is a member selected from the group consisting of sucrose fatty acid ester, sorbitan fatty acid ester and glycerin fatty acid ester, in which the fatty acid moiety is derived from long chain fatty acids with 6-18 carbon atoms and the ester has an HLB value of 1-8.
Claim 13
Dependent Claim
68 words
A solid nifedipine preparation according to claim 7, wherein at least 0.5 part by weight of casein and 0.2-9 parts by weight of the inorganic excipients are used per part by weight of nifedipine and wherein at least 1 part by weight of the enteric high molecular substance and at lease 0.1 part by weight of the plasticizer are used per part by weight of the co-pulverized mixture.
Claim 14
Dependent Claim
25 words
A solid nifedipine preparation according to claim 7, wherein the higher fatty acid ester is present in an mount of 2% based on the mixture.
Claim 15
Dependent Claim
28 words
A solid nifedipine preparation according to claim 7, wherein the pharmaceutically acceptable solid form is a member selected from the group consisting of granules, tablets, dragees and capsules.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-05-11 | 1990-11-10 | 1991-05-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-05-11 | 1994-11-10 | 1995-05-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-05-11 | 1998-11-10 | 1999-05-12 | $7700.00 | Window Closed / Lapsed |