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Claims for Patent: 5,004,613

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Claims for Patent: 5,004,613

Title: Oral sustained release pharmaceutical formulation and process
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.
Inventor(s): Radebaugh; Galen W. (Chester, NJ), Murtha; John L. (Holland, PA), Glinecke; Robert (Glenside, PA)
Assignee: McNeil-PPC, Inc. (Milltown, NJ)
Application Number:07/392,748
Patent Claims: 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.

2. The process of claim 1 wherein:

in Step B the wicking agent used is microcrystalline cellulose or powdered cellulose; and

in Step F the erosion promoter used is 2-15 parts by weight of either pregelatinized starch or starch NF or rice starch, or is 1-10 parts by weight of sodium starch glycolate or croscarmellose sodium or crospovidone; the lubricant used is magnesium stearate or stearic acid; and the glidant used is colloidal silicon dioxide or fumed silicon dioxide.

3. The process of claim 2 wherein:

in Step A, when any alcohol is used, it is alcohol USP or dehydrated alcohol USP or methyl alcohol USP or isopropyl alcohol USP, and is used in a quantity equal to or less than the water in the alcohol-water mixture.

4. The process of claim 2 wherein:

in Step A water is used; in Step B the wicking agent used is microcrystalline cellulose; in Step F the erosion promoter used is pregelatinized starch; and the lubricant used is magnesium stearate.

5. The process of claim 1 wherein the mixing of the granulating agent and blended powders in Step C is carried out in a high shear granulator.

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.

7. A composition according to claim 6 wherein the wicking agent is microcrystalline cellulose and the erosion promoter is pregelatinized starch.

8. A composition according to claim 6 wherein by parts by weight of the total composition the granulating agent comprises 5-25 parts by weight povidone and the excipients comprise 5-25 parts by weight hydroxyethyl cellulose, 10-70 parts by weight of a wicking agent, 1-15 parts by weight of an erosion promoter, 0-10 parts by glidant.

9. A composition according to claim 6 wherein by parts by weight of the total composition the granulating agent comprises 5-25 parts by weight of povidone and the excipients comprise 5-25 parts by weight of hydroxyethyl cellulose, 10-70 parts by weight of microcrystalline cellulose, 2-15 parts by weight pregelatinized starch 0-10 parts by weight magnesium stearate, and 0-5 parts by weight colloidal silicon dioxide.

10. A composition according to claim 6 wherein the total amount of granulating agent and excipients is greater than about 6 but less than 15 percent of the total weight of said shaped and compressed composition.

11. A composition according to claim 9 wherein the total amount of granulating agent and excipients is greater than about 6 but less than 15 percent of the total weight of said shaped and compressed composition.

12. A composition according to claim 6 wherein the pharmaceutical active is selected from the group consisting of codeine; codeine phosphate; loperamide; aspirin; naproxen; propoxyphene HCl; meperidine HCl; diphenhydramine; pseudoephedrine; and any pharmaceutically acceptable salts thereof.

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:

(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:

(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;

(C) combining and compressing the immediate release layer of Step A with the sustained release layer of Step B into a bi-layered tablet.

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.

15. The therapeutic composition of claim 14 wherein the immediate release layer comprises a medicament which is the same as the medicament in the immediate release layer.

16. The therapeutic composition of claim 14 wherein the amount of granulating agent and excipients is greater than about 6 percent but less than about 15 percent of the total weight of the sustained release layer of said shaped and compressed bi-layer composition.

17. The therapeutic composition of claim 14 wherein the wicking agent is microcrystalline cellulose and the erosion promoter is pregelatinized starch.

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:

19. A product made by the process of claim 1.

20. A product made by the process of claim 14.
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