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|Title:||Oral sustained release acetaminophen formulation and process|
|Abstract:||An acetaminophen-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 acetaminophen, hydroxyethyl cellulose, a wicking agent e.g. microcrystalline cellulose, then drying and milling the granulation and blending with dry powdered erosion promoter, e.g. pregelatinized starch, 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 acetaminophen.|
|Inventor(s):||Radebaugh; Galen W. (Maple Glen, PA), Murtha; John L. (Holland, PA), Glinecke; Robert (Glenside, PA)|
|Assignee:||McNeilab, Inc. (Spring House, PA)|
1. A process of preparing an acetaminophen-sustained release shaped and compressed tablet characterized by a slow release of the acetaminophen upon administration comprising
the following steps:
(A) forming a povidone granulating agent comprising the step of 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, from about 68 to 94 percent acetaminophen 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 povidone 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 in pregelatinized starch; and the lubricant used is magnesium stearate.
5. The process of claim 11 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 acetaminophen, a granulating agent and excipients combined into a matrix, characterized by a slow release of the acetaminophen upon administration, wherein the granulating agent and excipients comprise hydroxyethyl cellulose and povidone, and wherein the total amount of granulating agent and excipients is effective to bind the acetaminophen 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 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 weight of a lubricant, and 0-5 parts by weight of a glidant.
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 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.
9. The composition of claim 8 wherein the parts by weight refer to milligrams per tablet, and wherein the ingredients are present either in the weights indicated or in such weights multiplied by an appropriate fraction.
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 8 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. The tablet of claim 7 wherein the specific ingredients and amounts used are:
13. The tablet of claim 12 wherein the parts by weight shown refer to milligrams per tablet.
14. A shaped and compressed acetaminophen sustained release tablet made by wet granulating a sufficient amount of acetaminophen to comprise from about 68 to 94 percent of the total composition 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 into a tablet, wherein the ingredients of Parts I, II and III comprise the following:
15. A product made by the process of claim 1.
16. A product made by the process of claim 2.
17. A product made by the process of claim 4.
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