Patent EA-000223-B1 (EA)
Title: Direct compressed solid pharmaceutical dosage form and method thereof
Inventor: HUNTER EDWARD A
IPC: A61K47/04
Filed: 1996-11-12
Abstract: 1. A direct compressed solid pharmaceutical dosage form, comprising: a) from about 40 to about 95% by weight acetaminophen; b) from about 1 to about 60% by weight of a direct compression vehicle comprising microcrystalline cellulose; and coprocessed with from about 0.I to about 20% by weight silicon dioxide. c) from about 0.01 to about 4.0% by weight of a pharmaceutically-acceptable lubricant; 2. The solid pharmaceutical dosage form of Claim 1, wherein comprises from about 60% to about 85% by weight of acetaminophen. 3. The solid dosage form of Claim 1, wherein said silicon dioxide has an average primary particle size of from 1 nm to about 100 μm. 4. The solid dosage form of Claim 3, wherein said silicon dioxide is present in an amount of from about 0.5 to about 10% by weight, based on the weight of said microcrystalline cellulose. 5. The solid dosage form of Claim 5, wherein said silicon dioxide is present in an amount of from about 1.25 to about 5% by weight, based on the weight of said microcrystalline cellulose. 6. The solid dosage form of Claim 1, wherein said lubricant is sodium stearyl fumarate and said lubricant is present in an amount of from about 0.1 to about 1.0% by weight. 7. The solid dosage form of Claim 1, further comprising a disintegrant. 8. The solid dosage form of Claim 7, wherein said direct compression vehicle is present in an amount of from about 2 to about 25% by weight of said solid dosage form. 9. The solid dosage form of Claim 1, wherein said acetaminophen comprises at least about 75% by weight of said solid dosage form and said solid dosage form has an average tablet hardness of about 6.5 kP. 10. The solid dosage form of Claim 9, wherein said pharmaceutical dosage form comprises from about 10 to about 1000 milligrams of acetaminophen. 11. A method of preparing a direct compressed solid pharmaceutical dosage form comprising: a) combining from about 40 to about 95% by weight acetaminophen and from about 1 to about 60% by weight of a direct compression vehicle comprising microcrystalline cellose coprocessed with from about 0.I to about 20% by weight silicon dioxide under shear conditions to obtain a first homogenous granulate; b) combining said first homogenous granulate with from about 0.01 to about 4.0% of a pharmaceutically-acceptable lubricant; and c) compressing said homogenous granulate into a solid pharmaceutical dosage form. 12. The method of Claim 11, wherein said pharmaceutical dosage form comprises from about 60% to about 85% by weight acetaminophen. 13. The method of Claim 11, wherein said acetaminophen is in granular form. 14. The method of Claim 11, wherein said silicon dioxide is colloidal silicon dioxide and has an average primary particle size of from 1 nm to about 100 μm and said silicon dioxide is present in an amount of from about 0.5 to about 10% by weight, based on the weight of said microcrystalline cellulose. 15. The method of Claim 12, wherein said lubricant is sodium stearyl fumarate that is present in an amount of from about 0.01 to about 4.0% by weight. 16. The method of Claim 11, wherein said first homogeneous granulate further comprises silicon dioxide in an amount ranging from about 0.1 to about 5% by weight of said dosage form. 17. The method of Claim 11, further comprising combining a disintegrant with said acetaminophen and said direct compression vehicle under said high shear conditions. 18. The method of Claim 11, wherein said direct compression vehicle is present in an amount of from about 2 to about 25% by weight of said solid dosage form. 19. The method of Claim 11, wherein said acetaminophen comprises at least 75% by weight of said solid dosage form and step and (c) comprises the step of compressing said homogenous granulate at a compression force of about 25kN to prepare a tablet average hardness being about 6.5 kP.