Stable suspension formulations of bioerodible polymer matrix microparticles incorporating drug loaded ion exchange resin particles
First Claim
1. A sustained release pharmaceutical compound delivery composition having improved delivery characteristics and enhance long-term storage stability, said composition comprising:
- a non-ionic liquid suspension of microparticulates, said microparticulates formed of an erodible bioadhesive polymeric matrix of poly and polyvinylpyrrolidone wherein the ratio of poly (methylvinylether/maleic anhydride) to polyvinylpyrrolidone ranges from approximately 1;
1 to 4;
1 by weight, incorporating at least one ion exchange resin particle sized from approximately 1 μ
m to 100 μ
m, said ion exchange resin particle having approximately 2 to 50 wt % of a pharmaceutical compound releasably bound thereto.
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Abstract
Sustained release pharmaceutical compound delivery compositions and methods for their production are disclosed wherein ion exchange resin particles are loaded with releasably bound pharmaceutical compounds prior to incorporation in an erodible polymeric matrix to form microparticulates. The microparticulates are suspended in a fluid medium where the encapsulating polymeric matrix shields the drug loaded ion exchange resin from solvent interaction. Administration to a target tissue site initiations erosion of the polymer matrix and release of the loaded pharmaceutical compound.
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Citations
24 Claims
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1. A sustained release pharmaceutical compound delivery composition having improved delivery characteristics and enhance long-term storage stability, said composition comprising:
a non-ionic liquid suspension of microparticulates, said microparticulates formed of an erodible bioadhesive polymeric matrix of poly and polyvinylpyrrolidone wherein the ratio of poly (methylvinylether/maleic anhydride) to polyvinylpyrrolidone ranges from approximately 1;
1 to 4;
1 by weight, incorporating at least one ion exchange resin particle sized from approximately 1 μ
m to 100 μ
m, said ion exchange resin particle having approximately 2 to 50 wt % of a pharmaceutical compound releasably bound thereto.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
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11. A sustained release aqueous pharmaceutical compound delivery composition having improved delivery characteristics and enhanced long term storage ability, said composition comprising:
a nonionic aqueous suspension of microparticulates, said aqueous suspension having a pH value of less than about 5, and said microparticulates formed of a bioerodible, bioadhesive polymeric matrix of poly(methylvinylether/maleic anhydride) and polyvinylpyrrolidone wherein the ratio of poly (methylvinylether/maleic anhydride) to polyvinylpyrrolidone ranges from approximately 1;
1 to 4;
1 by weight, incorporating at least one ion exchange resin particle sized from approximately 1 μ
m to 100 μ
m, said ion exchange resin particle having from 2 to 50 wt % of a pharmaceutical compound releasably bound thereto.- View Dependent Claims (12, 13, 14, 15, 16, 17, 18, 19)
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20. A process for forming a sustained release pharmaceutical compound delivery composition having improved delivery characteristics and enhanced long term storage stability, said process comprising the steps of:
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reversibly loading at least one ion exchange resin particles sized form approximately 1 μ
m to 100 μ
m with from approximately 2 to 50 wt % of at least one pharmaceutical compound;incorporating said loaded ion exchange resin particle into an erodible polymeric matrix formed of poly(methylvinylether/maleic anhydride) and polyvinylpyrrolidone wherein the ratio of poly(methylvinylether/maleic anhydride) to polyvinylpyrrolidone ranges from approximately 1;
1 to 4;
1 by weight; andsuspending said erodible polymeric matrix incorporating said loaded ion exchange resin particle in a nonionic aqueous solution having a pH value of less than about 5. - View Dependent Claims (21, 22, 23, 24)
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Specification