Controlled release simvastatin delivery device
First Claim
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1. A drug delivery device for the controlled in situ production and release of a dispersion containing simvastatin, which is:
- (A) a compressed core prepared from an admixture comprising;
(i) a therapeutically effective amount of simvastatin; and
(ii) a polymer which upon hydration forms gelatinous microscopic particles, wherein the polymer is selected from the group consisting of sodium polyacrylate, carboxypolymethylenes, and the pharmaceutically acceptable salts thereof, and wherein the carboxypolymethylenes are prepared from acrylic acid crosslinked with allylethers of sucrose or pentaerythritol; and
(B) a water insoluble, water impermeable polymeric coating comprising a polymer and a plasticizer, which surrounds and adheres to the core, wherein the polymer is selected from the group consisting of cellulose acetate, cellulose acetate butyrate, ethylcellulose, polyvinylacetate, polyvinyl chloride, polymers of acrylic and methacrylic acid esters, and combinations of these polymers, and the plasticizer is selected from the group consisting of dibutylsebacate, diethylphthalate, triethylcitrate and polyethylene glycol, the coating having a plurality of formed apertures exposing between about 1 and about 75% of the core surface;
and wherein the release rate of the beneficial agent from the device is a function of the number and size of the apertures.
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Abstract
Controlled delivery of a beneficial agent in a dispersion is provided using (i) a compressed core which contains the beneficial agent, a polymer which forms gelatinous microscopic particles upon hydration, and if desired, an agent to modulate the hydration; and (ii) a water insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of the dispersion. The release rate of the beneficial agent is a function of the number and size of the apertures in the coating.
207 Citations
28 Claims
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1. A drug delivery device for the controlled in situ production and release of a dispersion containing simvastatin, which is:
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(A) a compressed core prepared from an admixture comprising; (i) a therapeutically effective amount of simvastatin; and (ii) a polymer which upon hydration forms gelatinous microscopic particles, wherein the polymer is selected from the group consisting of sodium polyacrylate, carboxypolymethylenes, and the pharmaceutically acceptable salts thereof, and wherein the carboxypolymethylenes are prepared from acrylic acid crosslinked with allylethers of sucrose or pentaerythritol; and (B) a water insoluble, water impermeable polymeric coating comprising a polymer and a plasticizer, which surrounds and adheres to the core, wherein the polymer is selected from the group consisting of cellulose acetate, cellulose acetate butyrate, ethylcellulose, polyvinylacetate, polyvinyl chloride, polymers of acrylic and methacrylic acid esters, and combinations of these polymers, and the plasticizer is selected from the group consisting of dibutylsebacate, diethylphthalate, triethylcitrate and polyethylene glycol, the coating having a plurality of formed apertures exposing between about 1 and about 75% of the core surface; and wherein the release rate of the beneficial agent from the device is a function of the number and size of the apertures. - 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. A drug delivery device for the controlled in situ production and release of a dispersion containing simvastatin, which is:
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(A) a compressed core prepared from an admixture comprising; (i) from 0.01% to 75% by weight of the core mixture of a therapeutically effective amount of simvastatin; and (ii) from about 5% to about 75% by weight of the core mixture of a polymer which upon hydration forms gelatinous microscopic particles, wherein the polymer is selected from the group consisting of sodium polyacrylate, carboxypolymethylenes and the pharmaceutically acceptable salts thereof, and wherein the carboxypolymethylenes are prepared from acrylic acid crosslinked with allylethers of sucrose or pentaerythritol; and (B) a water insoluble, water impermeable polymeric coating comprising a polymer and a plasticizer, which surrounds and adheres to the core, wherein the polymer is selected from the group consisting of polyvinyl chloride, cellulose acetate, cellulose acetate butyrate, ethylcellulose and combinations of these polymers, and the plasticizer is selected from the group consisting of diethylphthalate, dibutylsebacate and triethylcitrate, the coating having a plurality of formed apertures exposing between about 1 and about 75% of the core surface; and wherein the release rate of drug from the device is a function of the number and size of the apertures. - View Dependent Claims (21, 22)
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23. A process for the preparation of a drug delivery device for the controlled in situ production and release of a dispersion containing a beneficial agent characterized by having a compressed core surrounded by a water insoluble, water impermeable polymeric coating, comprising the steps of:
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(A) preparing a uniform mixture by either dry mixing or wet granulating a polymer which upon hydration produces gelatinous microscopic particles, the beneficial agent and other excipients used in the preparation of the core, wherein the polymer is selected from the group consisting of sodium polyacrylate, carboxypolymethylenes, and the pharmaceutically acceptable salts thereof, and wherein the carboxypolymethylenes are prepared from acrylic acid crosslinked with allylethers of sucrose or pentaerythritol; (B) compressing the uniform mixture into cores; (C) coating the entire core with the water insoluble, water impermeable polymeric coating comprised of a polymer and a plasticizer, wherein the polymer is selected from the group consisting of cellulose acetate, cellulose acetate butyrate, ethylcellulose, polyvinylacetate, polyvinyl chloride, polymers of acrylic and methacrylic acid esters, and combinations of these polymers, and the plasticizer is selected from the group consisting of dibutylsebacate, diethylphthalate, triethylcitrate and polyethylene glycol; and (D) forming apertures through the coating. - View Dependent Claims (24, 25, 26, 27)
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28. A drug delivery device for the controlled in situ production and release of a dispersion containing simvastatin, which is:
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(A) a compressed core prepared from an admixture comprising; (i) a therapeutically effective amount of simvastatin; and (ii) a polymer which upon hydration forms gelatinous microscopic particles, wherein the polymer is selected from the group consisting of sodium polyacrylate, carboxypolymethylenes, and the pharmaceutically acceptable salts thereof, and wherein the carboxypolymethylenes are prepared from acrylic acid crosslinked with allylethers of sucrose or pentaerythritol; and (B) a water insoluble polymeric coating comprising a polymer and a plasticizer, which surrounds and adheres to the core, wherein the polymer is selected from the group consisting of polyvinyl chloride, cellulose acetate, cellulose acetate butyrate, ethylcellulose and combinations of these polymers, and the plasticizer is selected from the group consisting of diethylphthalate, dibutylsebacate, and triethylcitrate, the coating having a plurality of formed apertures exposing between about 1 and about 75% of the core surface; and
wherein the release rate of the beneficial agent from the device is a function of the number and size of the apertures.
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Specification