US5028433A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Readily absorbable drug formulation of NB-818
Assignee: MSD KK
•
Filing: 1989-11-22
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Granted: 1991-07-02
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Expires: 2009-11-22
Abstract
Abstract A readily absorbable drug formulation obtained by incorporating to a water-soluble or enteric polymer, both a nonionic surfactant and (±)-2-carbamoyloxymethyl-4- (2,3-dichlorophenyl)-6-methyl-1,4-dihydropyrodine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester.
Inventors
- 👤 Sueaki Ishimaru
- 👤 Kiyohisa Ouchi
- 👤 Kimito Takeuchi
- 👤 Masaki Yamada
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 23:36
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/21; A61K31/215; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K9/00; A61K9/14; A61K9/16; A61K9/167; A61K9/1676
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
36 words
An orally administratable drug formulation having effective bioavailability in a pharmacologically effective dosage comprising a water-soluble or enteric polymer, a nonionic surfactant and (±)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester.
Claim 2
Dependent Claim
36 words
An orally administratable drug formulation having effective bioavailability in a pharmacologically effective dosage comprising a water-soluble or enteric polymer, a nonionic surfactant and (±)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester.
Claim 3
Dependent Claim
55 words
The drug formulation according to claim 1, wherein the nonionic surfactant is at least one member of the group consisting of glycerin fatty acid ester, glyceryl monostearate, acetylated glycerin stearate, acetylated glycerin fatty acid ester, sorbitan fatty acid ester, sorbitan monlaurate, sorbitan sesquioleate, sorbitan monooleate, sorbitan trioleate, polyoxyl 40 stearate and sucrose fatty acid ester.
Claim 4
Dependent Claim
38 words
The drug formulation according to claim 1, wherein the water-soluble or enteric polymer is at least one member of the group consisting of hydroxypropylmethylcellulose, methylcellulose, polyvinylpyrrolidone, hydroxypropylmethylcellulose phthalate, a methyl acrylate.metacrylic acid copolymer, carboxymethylethylcellulose and cellulose acetate phthalate.
Claim 5
Dependent Claim
55 words
The drug formulation according to claim 1, which contains from 0.1 to 3.0 parts by weight of the nonionic surfactant and from 0.2 to 4.0 parts by weight of the water-soluble or enteric polymer, relative to 1 part by weight of (+)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester.
Claim 6
Dependent Claim
82 words
A tablet formulation obtained by incorporating from 0.5 to 5.0% by weight, based on the total amount, of at least one member selected from the group consisting of light anhydrous silicic acid, magnesium alumino-methasilicate, magnesium alumino-silicate, aluminum hydroxide, synthetic hydrotalcite, fine titanium oxide and aluminum silicate, as a binder, to solid dispersion granules comprising a pharmacologically effective mixture of (±)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester, a nonionic surfactant and a water-soluble or enteric polymer.
Claim 7
Dependent Claim
82 words
A tablet formulation obtained by incorporating from 0.5 to 5.0% by weight, based on the total amount, of at least one member selected from the group consisting of light anhydrous silicic acid, magnesium alumino-methasilicate, magnesium alumino-silicate, aluminum hydroxide, synthetic hydrotalcite, fine titanium oxide and aluminum silicate, as a binder, to solid dispersion granules comprising a pharmacologically effective mixture of (±)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester, a nonionic surfactant and a water-soluble or enteric polymer.
Claim 8
Dependent Claim
113 words
A tablet formulation obtained by incorporating from 5.0 to 35% by weight, based on the total amount, of at least one member selected from the group consisting of a swellable polymer disintegrant capable of forming stress in a solid formulation, a disintegrant having a nature of a binder and capable of providing a disintegrating effect by the surface tension of water penetrated into a solid formulation through the spaces among particles and a disintegrant having both of the above-mentioned properties, to solid dispersion granules comprising a pharmacologically effective mixture of (±)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester, a nonionic surfactant and a water-soluble or enteric polymer.
Claim 9
Dependent Claim
113 words
A tablet formulation obtained by incorporating from 5.0 to 35% by weight, based on the total amount, of at least one member selected from the group consisting of a swellable polymer disintegrant capable of forming stress in a solid formulation, a disintegrant having a nature of a binder and capable of providing a disintegrating effect by the surface tension of water penetrated into a solid formulation through the spaces among particles and a disintegrant having both of the above-mentioned properties, to solid dispersion granules comprising a pharmacologically effective mixture of (±)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester, a nonionic surfactant and a water-soluble or enteric polymer.
Claim 10
Independent Claim
35 words
A method for preparing solid dispersion granules, which comprise incorporating to a water-soluble or enteric polymer, both a nonionic surfactant and (±)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester.
Claim 11
Independent Claim
35 words
A method for preparing solid dispersion granules, which comprise incorporating to a water-soluble or enteric polymer, both a nonionic surfactant and (±)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester.
Claim 12
Dependent Claim
54 words
A method for preparing a tablet formulation, which comprises incorporating a binder as defined in claim 5 to solid dispersion granules comprising a pharmacologically effective amount of (±)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester, a nonionic surfactant and a water-soluble or enteric polymer, followed by compression molding.
Claim 13
Independent Claim
121 words
A method for preparing a tablet formulation, which comprises incorporating from 5.0 to 35% by weight, based on the total amount, of at least two disintegrants selected from a group consisting of a swellable polymer disintegrant capable of forming stress in a solid formulation, a disintegrant having a nature of a binder and capable of providing a disintegrating effect by the surface tension of water penetrated into a solid formulation through the spaces among particles and a disintegrant having such two types of properties, to solid dispersion granules comprising a pharmacologically effective mixture of (±)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester, a nonionic surfactant and a water-soluble or enteric polymer, followed by compression molding.
Claim 14
Independent Claim
121 words
A method for preparing a tablet formulation, which comprises incorporating from 5.0 to 35% by weight, based on the total amount, of at least two disintegrants selected from a group consisting of a swellable polymer disintegrant capable of forming stress in a solid formulation, a disintegrant having a nature of a binder and capable of providing a disintegrating effect by the surface tension of water penetrated into a solid formulation through the spaces among particles and a disintegrant having such two types of properties, to solid dispersion granules comprising a pharmacologically effective mixture of (±)-2-carboxyoxymethyl-4-(2,3-dichlorophenyl-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester or (-)-2-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-b 6methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-isopropyl ester 5-methyl ester, a nonionic surfactant and a water-soluble or enteric polymer, followed by compression molding.
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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) | 1994-07-01 | 1994-12-31 | 1995-07-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-07-01 | 1998-12-31 | 1999-07-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-07-01 | 2002-12-31 | 2003-07-02 | $7700.00 | Window Closed / Lapsed |