Oral sustained release pharmaceutical formulation and process
First Claim
1. A process of preparing a pharmaceutical-sustained release shaped and compressed tablet characterized by a slow release of pharmaceutical active upon administration comprising the following steps:
- (A) forming a granulating agent by dissolving 5-25 parts by weight of the total composition of povidone in water or in an alcohol-water mixture;
(B) blending together, in parts by weight of the total composition, the following ingredients, with sufficient pharmaceutical active to comprise about 68 to 94 percent by weight of the total composition, in dry powder form, 5-25 parts by weight hydroxyethyl cellulose and 5-25 parts by weight of a wicking agent;
(C) adding and mixing the granulating agent from Step A to the blended powders from Step B, to form a wet granulation;
(D) drying the wet granulation of Step C;
(E) milling the dried granulation from Step D;
(F) thoroughly blending the milled dried granulation from Step E with the following parts by weight of the total composition of ingredients in dry powder form;
1-15 parts by weight erosion promoter, 5-45 parts by weight wicking agent, 0-10 parts by weight lubricant and 0-5 parts by weight glidant; and
(G) compressing the final granulation from Step F into a tablet or tablet layer.
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Accused Products
Abstract
A pharmaceutical sustained release tablet or tablet layer is formed by making a wet granulation, using povidone (PVP) in water or alcohol-water as the granulating fluid which is mixed with a pharmaceutical active, hydroxyethyl cellulose, a wicking agent e.g. microcrystalline cellulose, then drying and milling the granulation and blending with dry powdered erosion promotor, e.g. pregelantinized starch, additional wicking agent, lubricant e.g. magnesium stearate and glidant e.g. silicon dioxide, and compressing the resultant granulation, which upon administration results in a slow release of the pharmaceutical active.
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Citations
20 Claims
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1. A process of preparing a pharmaceutical-sustained release shaped and compressed tablet characterized by a slow release of pharmaceutical active upon administration comprising the following steps:
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(A) forming a granulating agent by dissolving 5-25 parts by weight of the total composition of povidone in water or in an alcohol-water mixture; (B) blending together, in parts by weight of the total composition, the following ingredients, with sufficient pharmaceutical active to comprise about 68 to 94 percent by weight of the total composition, in dry powder form, 5-25 parts by weight hydroxyethyl cellulose and 5-25 parts by weight of a wicking agent; (C) adding and mixing the granulating agent from Step A to the blended powders from Step B, to form a wet granulation; (D) drying the wet granulation of Step C; (E) milling the dried granulation from Step D; (F) thoroughly blending the milled dried granulation from Step E with the following parts by weight of the total composition of ingredients in dry powder form;
1-15 parts by weight erosion promoter, 5-45 parts by weight wicking agent, 0-10 parts by weight lubricant and 0-5 parts by weight glidant; and(G) compressing the final granulation from Step F into a tablet or tablet layer. - View Dependent Claims (2, 3, 4, 5, 19)
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- 6. A shaped and compressed sustained release therapeutic composition comprising a pharmaceutical active, a granulating agent and excipients combined into a matrix, characterized by a slow release of the pharmaceutical active upon administration, wherein the granulating agent and excipients comprise hydroxyethyl cellulose, povidone, a wicking agent and an erosion promoter and wherein the total amount of granulating agent and excipients is effective to bind the active in a sustained release solid matrix but is less than about 32 percent and more than about 6 percent of the weight of said shaped and compressed composition.
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13. A process of preparing sustained release bi-layer medicament tablet comprising a first layer of immediate release and a second layer of sustained slow release of medicament according to the steps of:
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(A) preparing an immediate release layer comprising a medicament and pharmaceutically acceptable excipients; and (B) preparing a sustained release layer comprising a medicament as the active ingredient according to the steps of; (1) forming a granulating agent by dissolving about 5-25 parts by weight of the total sustained release layer of povidone in alcohol or an alcohol-water mixture; (2) blending together a sufficient amount of medicament to comprise 68 to 94 percent of the total weight of the sustained release layer with the following ingredients in dry powder form in parts by weight of the total sustained release layer as indicated;
space="preserve" listing-type="tabular">______________________________________ Ingredient Parts by Weight ______________________________________ hydroxyethyl cellulose 5-25 wicking agent 5-25;
______________________________________(3) adding the granulating agent from Step 1 to the blended powders from Step 2, and forming a wet granulation; (4) drying the wet granulation of Step 3; (5) milling the dried granulation Step 4; (6) thoroughly blending the milled dried granulation from Step 5 with the following ingredients in dry powder form;
space="preserve" listing-type="tabular">______________________________________ Ingredient Parts by Weight ______________________________________ erosion promoter 1-15 wicking agent 5-45 lubricant 0-10 glidant 0-5;
and ______________________________________(C) combining and compressing the immediate release layer of Step A with the sustained release layer of Step B into a bi-layered tablet.
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- 14. A shaped and compressed bi-layer therapeutic composition comprising a medicament in a first immediate release layer and a medicament in a second sustained release layer wherein the immediate release layer comprises a medicament and pharmaceutically acceptable excipients and the sustained release layer comprises a medicament, a granulating agent and excipients combined into a matrix, wherein the granulating agent and excipients of the sustained release layer include hydroxyethyl cellulose, povidone, a wicking agent and erosion promoter and wherein the total amount of said granulating agent and excipients is effective to bind the acetaminophen in a sustained release solid matrix but is less than about 32 percent of the weight of the sustained release layer of said shaped and compressed bi-layer composition.
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18. A shaped and compressed bi-layered immediate release layer and sustained release layer medicament tablet made by combining an immediate release layer comprising one or medicaments and pharmaceutically acceptable excipients with a sustained release layer made by wet granulating a sufficient amount of one or more medicaments to comprise 68 to 94 percent of the total weight of the sustained release layer with the Excipients of Part I and the Granulating Agent of Part II, drying and milling the resultant granulations, and then blending with the Excipients of Part III and compressing the two layers into a tablet, wherein the ingredients of Parts I, II and III comprise the following:
space="preserve" listing-type="tabular">______________________________________ Range of Parts by Weight of the Total Ingredient Sustained Release Layer ______________________________________ Part I Excipients Hydroxyethyl Cellulose 5-25 Microcrystalline Cellulose 5-25 Part II Granulating Aqent Povidone 5-25 Alcohol or Alcohol-Water q.s. Part III Excipients Pregelatinized Starch 2-15 Microcrystalline Cellulose 5-45 Magnesium Stearate 0-10 Colloidal Silicon Dioxide 0-5 ______________________________________
Specification