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US4806361A Expired / Lapsed US ⏱️ 0.0 years remaining

Medicaments in sustained release unit dose form

Assignee: STWB Inc
•
Filing: 1985-05-24
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Granted: 1989-02-21
•
Expires: 2005-05-24
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Abstract

Abstract Sustained-release compositions for oral administration comprising medicament-coated nonpareils surrounded by a sustaining coating of at least three admixed polymers afford exceptionally good plasma levels of the medicament.

Inventors

  • 👤 Paul J. Harrison
  • 👤 John R. Langridge
  • 👤 Christopher J. Potter

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 11:37
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K9/50; A61K9/5073; A61K9/5078

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 151 words
A sustained release pharmaceutical composition for oral administration containing, as the active ingredient, a medicament of the formula: ##STR2## where R is lower-alkyl having from 1 to 4 carbon atoms which comprises a plurality of beads each composed of an inert particulate core having adhered thereto a coating comprising particles of said medicament and further coated with a sustaining coating comprising three admixed polymers, the first said polymer being soluble at all pH values of 1.5 and above, the second said polymer being insoluble in gastric juices at pH values below about 5 but soluble therein at pH values of about 5 and above and the third said polymer being insoluble in the contents of the gastrointestinal tract at all pH values normally encountered therein, and wherein the ratio of the weight of the third polymer to the combined weight of the other two polymers is about 1.5:1 to about 2:1.
Claim 2
Dependent Claim 151 words
A sustained release pharmaceutical composition for oral administration containing, as the active ingredient, a medicament of the formula: ##STR2## where R is lower-alkyl having from 1 to 4 carbon atoms which comprises a plurality of beads each composed of an inert particulate core having adhered thereto a coating comprising particles of said medicament and further coated with a sustaining coating comprising three admixed polymers, the first said polymer being soluble at all pH values of 1.5 and above, the second said polymer being insoluble in gastric juices at pH values below about 5 but soluble therein at pH values of about 5 and above and the third said polymer being insoluble in the contents of the gastrointestinal tract at all pH values normally encountered therein, and wherein the ratio of the weight of the third polymer to the combined weight of the other two polymers is about 1.5:1 to about 2:1.
Claim 3
Dependent Claim 24 words
A pharmaceutical composition according to claim 1 wherein said first polymer constitutes about 15-20 wt. % of the polymer mixture forming the sustaining coating.
Claim 4
Dependent Claim 20 words
A pharmaceutical composition according to claim 2 wherein the inert cores of the beads are in the form of nonpareils.
Claim 5
Dependent Claim 20 words
A pharmaceutical composition according to claim 3 wherein said first polymer is selected from hydroxypropylmethylcellulose, sodium carboxymethyl cellulose and polyvinylpyrrolidone.
Claim 6
Dependent Claim 14 words
A pharmaceutical composition according to claim 4 wherein said second polymer is hydroxypropylmethylcellulose phthalate.
Claim 7
Dependent Claim 14 words
A pharmaceutical composition according to claim 5 wherein said third polymer is ethyl cellulose.
Claim 8
Dependent Claim 37 words
A pharmaceutical composition according to claim 6 wherein said first polymer is hydroxypropylmethylcellulose and wherein the ratio of the weight of the ethylcellulose to the combined weight of the hydroxypropylmethylcellulose and the hydroxypropylmethylcellulose phthalate is about 1.5:1.
Claim 9
Dependent Claim 12 words
A pharmaceutical composition according to claim 6 wherein said medicament is 1,2-dihydro-3-cyano-6-methyl-5-(4-pyridinyl)-2(1H)-pyridinone.
Claim 10
Dependent Claim 16 words
A pharmaceutical composition according to claim 8 in unit dosage form contained within a gelatine capsule.
Claim 11
Dependent Claim 138 words
A process for producing a pharmaceutical composition according to claim 1 which comprises: (1) coating inert core particles with particles of said medicament and a binder for adhering said medicament particles to said core particles and (2) applying to said coated core particles a sustaining coating solution comprising three admixed polymers, the first said polymer being soluble at all pH values of 1.5 and above, the second said polymer being insoluble in gastric juices at pH values below about 5 but soluble therein at pH values of about 5 and above and the third said polymer being insoluble in the contents of the gastrointestinal tract at all pH values normally encountered therein, and wherein the ratio of the weight of the third polymer to the combined weight of the other two polymers is about 1.5:1 to about 2:1.
Claim 12
Dependent Claim 39 words
A process according to claim 10 wherein said sustaining coating is formed by applying to the medicament-coated core particles a solution of said three polymers in a volatile solvent therefor and evaporating the solvent from the particles thus coated.
Claim 13
Dependent Claim 38 words
A process according to claim 11 wherein said solution is produced by forming a dispersion of the three polymers in a suitable medium, adding a lower boiling solvent to the dispersion and stirring to give a clear solution.
Claim 14
Dependent Claim 19 words
A process according to claim 12 wherein the inert cores of the beads are in the form of nonpareils.
Claim 15
Dependent Claim 11 words
A process according to claim 13 wherein the medicament is 1,2-dihydro-3-cyano-6-methyl-5-(4-pyridinyl)-2(1H)-pyridinone.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-02-21 1992-08-22 1993-02-21 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-02-21 1996-08-22 1997-02-21 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-02-21 2000-08-22 2001-02-21 $7700.00 Window Closed / Lapsed

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