Pharmaceutical sustained release matrix and process
First Claim
1. A shaped and compressed sustained release therapeutic composition comprising an effective amount of an analgesic and a granulating agent and excipients combined into a matrix, characterized by a long-lasting slow and relatively regular incremental release of the analgesic upon administration, wherein the granulating agent and excipients includes a combination of two polymers, ethylcellulose and povidone, wherein the total amount of granulating agent and excipients is an amount effective to form a solid matrix of active and binder materials and is less than 20 percent of the weight of said shaped and compressed composition wherein the total amount of granulating agent, and granulating agent and excipients is in the range of 5 to less than 20 percent of the weight of pair shaped and compressed composition.
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Accused Products
Abstract
A pharmaceutical sustained release homogeneous tablet or homogeneous tablet layer is formed by making a wet granulation using povidone (PVP) in alcohol as the granulating fluid which is mixed with a pharmaceutical active, ethylcellulose, a wicking agent, e.g. microcrystalline cellulose, an erosion promoter, e.g. pregelatinized starch, then drying and milling the granulation and blending with a dry powdered erosion promotor, wicking agent, lubricant, e.g. magnesium stearate and glidant, e.g. silicon dioxide, and compressing the resultant granulation, which upon administration results in a long-lasting slow and relatively regular incremental release of the pharmaceutical active, and multi-layered pharmaceutical active tablets comprising immediate release and/or sustained release layers.
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Citations
17 Claims
- 1. A shaped and compressed sustained release therapeutic composition comprising an effective amount of an analgesic and a granulating agent and excipients combined into a matrix, characterized by a long-lasting slow and relatively regular incremental release of the analgesic upon administration, wherein the granulating agent and excipients includes a combination of two polymers, ethylcellulose and povidone, wherein the total amount of granulating agent and excipients is an amount effective to form a solid matrix of active and binder materials and is less than 20 percent of the weight of said shaped and compressed composition wherein the total amount of granulating agent, and granulating agent and excipients is in the range of 5 to less than 20 percent of the weight of pair shaped and compressed composition.
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3. A shaped and compressed pharmaceutical active sustained release tablet made by wet granulating an analgesic and the Excipients of Part I with the Granulating Agent of Part II to form a granulation, drying and milling the granulation to form a resultant granulation, and then blending with the Excipients of Part III and compressing into a tablet, wherein the analgesic is added in Part I and comprises at least 66% of the total weight of the tablet and the ingredients of parts I, II and II consists essentially of the following:
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space="preserve" listing-type="tabular">______________________________________ Parts by Weight Range Total Ingredient Inactive Ingredients ______________________________________ Part I Excipients Ethyl Cellulose 3-12 Microcrystalline Cellulose 10-35 Pregelatinized Starch 5-25 Part II Granulating Agent Povidone 5-10 Alcohol or Alcohol-Water Part III Excipients Pregelatinized Starch 3-20 Microcrystalline Cellulose 2-10 Magnesium Stearate 2-10 Colloidal Silicon Dioxide 2-10 ______________________________________wherein Alcohol is selected from the group consisting of alcohol USP, dehydrated alcohol USP, methyl alcohol USP and isopropyl alcohol USP.
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- 4. A shaped and compressed bi-layer immediate release and sustained release therapeutic composition comprising a pharmaceutical active in both layers wherein the immediate release layer comprises a pharmaceutical active and pharmaceutically acceptable excipients and the sustained release layer comprises a granulating agent and excipients combined into a matrix, characterized by a long-lasting slow and relatively regular incremental release of the pharmaceutical active upon administration and at least one pharmaceutical active in the sustained release layer is an analgesic wherein the granulating agent and excipients includes a combination of two polymers, ethylcellulose and povidone, and wherein the total amount of granulating agent and excipients is less than 20 percent of the weight of the sustained release layer of said shaped and compressed bi-layer composition.
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9. A shaped and compressed bi-layered immediate release and sustained release pharmaceutical active tablet made by combining an immediate release layer comprising a pharmaceutical active and pharmaceutically acceptable excipients with a sustained release layer made by wet granulating an analgesic and Excipients ingradients of Part II, to form a granulation drying and milling the granulation to form a resultant granulation then blending the resultant granulation with the Excipients of Part III and compressing the two layers into a tablet, wherein the ingredients of Parts I, II and III consist essentially of the following:
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space="preserve" listing-type="tabular">______________________________________ Range of Ingredient Parts by Weight ______________________________________ Part I Pharmaceutical Active 170-2000 Ethyl Cellulose 3-12 Microcrystalline Cellulose 10-35 Pregelatinized Starch 5-25 Part II Granulating Agent Povidone 5-30 Alcohol or Alcohol-Water q.t. Part III Excipients Pregelatinized Starch 3-20 Microcrystalline Cellulose 2-10 Magnesium Stearate 2-10 Colloidal Silicon Dioxide 2-10 ______________________________________wherein Alcohol is selected from the group consisting of alcohol USP, dehydrated alcohol USP, methyl alcohol USP, and isopropyl alcohol USP. - View Dependent Claims (11)
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Specification