Modified release formulations containing drug-ion exchange resin complexes
First Claim
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1. An orally ingestible aqueous pharmaceutical suspension composition comprising:
- (A) barrier coated particulates which provide about a twelve hour release profile which comprise(i) a particulate matrix comprising a particulate hydrocodone-cation exchange resin complex and a water insoluble polymer or copolymer or a hydrophilic polymer, said particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or hydrophilic polymer) matrix capable of passing through a number 40 mesh screen,said particulate hydrocodone-cation exchange resin complex comprising hydrocodone bound to a pharmaceutically acceptable water insoluble cation exchange resin, wherein said water insoluble polymer or copolymer, or hydrophilic polymer, is present in said particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or hydrophilic polymer) matrix in an amount of about 3% to about 30% by weight, based on the weight of said particulate hydrocodone-cation exchange resin complex, and(ii) a cured high tensile strength, water permeable, water insoluble, non ionic polymeric diffusion barrier coating over said particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or said hydrophilic polymer) matrix defined in (i), said cured barrier coating applied as an aqueous dispersion, said cured barrier coating comprising;
(a) about 70% w/w to about 90% w/w polyvinylacetate polymer,(b) a stabilizer, and(c) about 2.5 to about 20% w/w of plasticizer effective to enhance the tensile strength of said cured barrier coating, whereby said cured coating provides about a twelve hour release profile to the hydrocodone in said particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or hydrophilic polymer) matrix), wherein the weight percentage is based on the weight of the cured barrier coating layer;
(B) an uncoated particulate drug-cation exchange resin complex of a size capable of passing through a number 40 mesh screen, wherein said uncoated drug-cation exchange resin complex is a dl-chlorpheniramine bound to a pharmaceutically acceptable water insoluble cation exchange resin complex or a dexchlorpheniramine bound to a pharmaceutically acceptable water insoluble cation exchange resin; and
(C) a pharmaceutically acceptable aqueous suspension base, wherein said coated particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or or hydrophilic polymer) matrix defined in (ii) and said uncoated particulate drug-ion exchange resin complex defined in (B) are suspended in said base.
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Abstract
A coated drug-ion exchange resin complex comprising a core composed of a drug complexed with a pharmaceutically acceptable ion-exchange resin is provided. The drug-ion exchange resin complex is in admixture with a release retardant. The coating is a polyvinyl acetate polymer and a plasticizer. Methods of making and products containing this coated complex are described.
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Citations
24 Claims
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1. An orally ingestible aqueous pharmaceutical suspension composition comprising:
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(A) barrier coated particulates which provide about a twelve hour release profile which comprise (i) a particulate matrix comprising a particulate hydrocodone-cation exchange resin complex and a water insoluble polymer or copolymer or a hydrophilic polymer, said particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or hydrophilic polymer) matrix capable of passing through a number 40 mesh screen,said particulate hydrocodone-cation exchange resin complex comprising hydrocodone bound to a pharmaceutically acceptable water insoluble cation exchange resin, wherein said water insoluble polymer or copolymer, or hydrophilic polymer, is present in said particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or hydrophilic polymer) matrix in an amount of about 3% to about 30% by weight, based on the weight of said particulate hydrocodone-cation exchange resin complex, and(ii) a cured high tensile strength, water permeable, water insoluble, non ionic polymeric diffusion barrier coating over said particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or said hydrophilic polymer) matrix defined in (i), said cured barrier coating applied as an aqueous dispersion, said cured barrier coating comprising;(a) about 70% w/w to about 90% w/w polyvinylacetate polymer, (b) a stabilizer, and (c) about 2.5 to about 20% w/w of plasticizer effective to enhance the tensile strength of said cured barrier coating, whereby said cured coating provides about a twelve hour release profile to the hydrocodone in said particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or hydrophilic polymer) matrix), wherein the weight percentage is based on the weight of the cured barrier coating layer;(B) an uncoated particulate drug-cation exchange resin complex of a size capable of passing through a number 40 mesh screen, wherein said uncoated drug-cation exchange resin complex is a dl-chlorpheniramine bound to a pharmaceutically acceptable water insoluble cation exchange resin complex or a dexchlorpheniramine bound to a pharmaceutically acceptable water insoluble cation exchange resin; and (C) a pharmaceutically acceptable aqueous suspension base, wherein said coated particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer or copolymer or or hydrophilic polymer) matrix defined in (ii) and said uncoated particulate drug-ion exchange resin complex defined in (B) are suspended in said base. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19)
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20. An orally ingestible aqueous pharmaceutical suspension composition, comprising (A) barrier coated particulates which provides about a twelve hour release profile:
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(i) a particulate matrix comprising a particulate hydrocodone-cation exchange resin complex and a water insoluble polymer, said particulate hydrocodone-cation exchange resin complex—
(water insoluble polymer) matrix capable passing through a number 40 mesh screen,said particulate hydrocodone-cation exchange resin complex comprising hydrocodone bound to a pharmaceutically acceptable water insoluble cation exchange resin, wherein said water insoluble polymer is present in an amount of about 3% to about 30% by weight, based on the weight of said particulate hydrocodone-cation exchange resin complex—
(water-insoluble polymer) matrix defined in (i), and wherein said water insoluble cation exchange resin is a copolymer comprising styrene and a divinylbenzene;(ii) a cured high tensile strength, water permeable, water insoluble, non ionic polymeric diffusion barrier coating over said hydrocodone-cation exchange resin complex—
(water insoluble polymer) matrix defined in (i), said cured barrier coating applied as an aqueous dispersion, said cured barrier coating comprising(a) about 75% w/w to about 90% w/w polyvinylacetate polymer, (b) a stabilizer, and (c) about 2.5 to about 20% w/w of plasticizer effective to enhance the tensile strength of said cured barrier coating, whereby said cured coating provides a modified release profile to the drug in said drug- ion exchange resin complex in said matrix; and (B) an uncoated particulate dl-chlorpheniramine-cation exchange resin complex of a size capable of passing through a number 40 mesh screen, said complex comprising dl-chlorpheniramine bound to a pharmaceutically acceptable water insoluble cation exchange resin which comprises a copolymer of styrene and a divinylbenzene; and (C) a pharmaceutically acceptable aqueous suspension base, wherein said coated particulate hydrocodone-cation exchange resin complex (water-insoluble polymer) matrix defined in (ii) and said uncoated particulate dl-chlorpheniramine-cation exchange resin complex defined in (B) are suspended in said base. - View Dependent Claims (21, 22, 23, 24)
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Specification