Method of making ibuprofen and narcotic analgesic compositions

• US 6,599,531 B2
• Filed: 12/21/2001
• Issued: 07/29/2003
• Est. Priority Date: 06/12/1996
• Status: Expired due to Term

• Current Assignee: Abbvie Deutschland GmbH & Company KG (Abbvie Incorporated)
• Original Assignee: Knoll Pharmaceutical Company (Abbvie Incorporated)
• Inventors: Lai, Jin-Wang, Kushla, Gregory P., Polli, Gerald P.
• Primary Examiner(s): Kishore, Gollamudi S.
• Assistant Examiner(s): Joynes, Robert M.
• Application Number:
  US10/028,939
• Publication Number:
  US 20020127274A1
• Time in Patent Office: 585 Days
• Field of Search: 424/465, 424/464, 424/470, 424/493, 424/494, 424/468, 424/469, 424/489
• US Class Current: 424/465
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

Abstract

Provided herein are compositions and methods of making compositions of ibuprofen in combination with a narcotic analgesic. Specifically provided is a pharmaceutical tablet composition comprising ibuprofen; a narcotic analgesic; colloidal silicon dioxide; a filler selected from the group consisting of microcrystalline cellulose and powdered cellulose; a disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, and sodium starch glycolate; a binder consisting of an akylhydroxy methylcellulose; a starch; and a lubricant. Also provided herein is a method of preparing a pharmaceutical tablet composition comprising: (a) Granulating ibuprofen, a narcotic analgesic, a first glidant, a first disintegrant, a binder, and starch to form granules wherein said granulating step comprises a wet granulation process; (b) blending the granules with extra-granular material comprised of a second glidant, a second disintegrant, a filler and starch to form a blend of granules and extra-granular material; and (c) compressing the blend into a tablet.

Claims

1. A pharmaceutical tablet composition comprising ibuprofen and hydrocodone bitartrate, said tablet having been prepared by a method comprising the steps of:

(a) granulating ibuprofen, hydrocodone bitartrate, colloidal silicon dioxide, a disintegrant, a filler, and starch to form granules, wherein said granulating step comprises a wet granulation process;

(b) blending the granules with extra-granular material comprised of a lubricant and at least one excipient to form a blend of granules and extra granular material wherein the composition is substantially free of lactose and polyvinylpyrrolidone and wherein the blend flows well, has good compression performance, and can be compressed over a wide range of compression forces with no substantial change in the disintegration time of a tablet made from such blend; and

(c) compressing the blend into a tablet, wherein said ibuprofen, said hydrocodone bitartrate and said lubricant are present in said tablet in a single phase.

2. The pharmaceutical tablet composition as recited in claim 1, wherein the ibuprofen is provided in a range of about 25% to about 63%, by total weight of the tablet;

the hydrocodone bitartrate is provided in a range of about 0.6% to about 3.8%, by total weight of the tablet;

the colloidal silicon dioxide is provided in a range of about 0.5% to about 3% by total weight of the tablet;

the filler is selected from the group consisting of microcrystalline cellulose and powdered cellulose and is provided in range of the total weight of the tablet of about 10% to about 42%;

the disintegrant is selected from the group consisting of croscarmellose sodium, crospovidone, and sodium starch glycolate and is provided in a range, of the total weight of the tablet, of about 4% to about 10%;

the starch is provided in a range, of the total weight of the tablet composition, of about 11% to about 20%; and

the lubricant is provided in an amount less than 1% by weight of the total weight of the tablet; and

wherein a binder is provided in a range, of the total weight of the tablet composition, of about 2% to less than 6%, and the binder comprises an alkylhydroxy methylcellulose;

and wherein the granule comprises granulate material comprised of;

1) the ibuprofen,

2) the hydrocodone,

3) about 0.5% to about 2.0%, of the total weight of the tablet composition, of colloidal silicon dioxide,

4) about 9.5% up to about 22%, of the total weight of the tablet composition, of filler,

5) about 4%, of the total weight of the tablet composition, of disintegrant, and

6) about 6% to about 12%, of the total weight of the tablet composition of starch;

wherein the extra granule material comprises the remaining amount of the tablet material;

the composition provided in the substantial absence of lactose and/or polyvinylpyrrolidone and wherein the composition flows well, has good compression performance, and can be compressed over a wide range of compression forces with no substantial change in the disintegration time of the tablet.

3. The pharmaceutical tablet composition as recited in claim 2, wherein the weight of the filler is provided in range, of the total weight of the tablet composition, of about 15% to about 25%.

4. The pharmaceutical tablet composition as recited in claim 2, wherein the weight of the disintegrant is provided in a range of about 6% to about 8%.

5. The pharmaceutical tablet composition as recited in claim 3, wherein the weight of the disintegrant is provided in a range of about 6% to about 8%.

6. The pharmaceutical tablet composition as recited in claim 2, wherein the weight of the colloidal silicon dioxide is in a range of the total weight of the tablet, of about 1.5% to about 2%.

7. The pharmaceutical tablet composition as recited in claim 3, wherein the weight of the colloidal silicon dioxide is in a range, of the total weight of the tablet, of about 1.5% to about 2%.

8. The pharmaceutical tablet composition as recited in claim 4, wherein the weight of the colloidal silicon dioxide is in a range, of the total weight of the tablet, of about 1.5% to about 2%.

9. The pharmaceutical tablet composition as recited in claim 5, wherein the weight of the colloidal silicon dioxide is in a range, of the total weight of the tablet, of about 1.5% to about 2%.

10. The pharmaceutical tablet composition as recited in claim 2, wherein the weight of the binder is in a range, of the total weight of the tablet, of about 3% to about 4%.

11. The pharmaceutical tablet composition as recited in claim 3, wherein the weight of the binder is in a range, of the total weight of the tablet, of about 3% to about 4%.

12. The pharmaceutical tablet composition as recited in claim 4, wherein the weight of the binder is in a range, of the total weight of the tablet, of about 3% to about 4%.

13. The pharmaceutical tablet composition as recited in claim 5, wherein the weight of the binder is in a range, of the total weight of the tablet, of about 3% to about 4%.

14. The pharmaceutical tablet composition as recited in claim 6, wherein the weight of the binder is in a range, of the total weight of the tablet, of about 3% to about 4%.

15. The pharmaceutical tablet composition as recited in claim 7, wherein the weight of the binder is in a range, of the total weight of the tablet, of about 3% to about 4%.

16. The pharmaceutical tablet composition as recited in claim 8, wherein the weight of the binder is in a range, of the total weight of the tablet, of about 3% to about 4%.

17. The pharmaceutical tablet composition as recited in claim 9, wherein the weight of the binder is in a range, of the total weight of the tablet, of about 3% to about 4%.

18. The pharmaceutical tablet composition as recited in claim 2, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

19. The pharmaceutical tablet composition as recited in claim 3, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

20. The pharmaceutical tablet composition as recited in claim 4, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

21. The pharmaceutical tablet composition as recited in claim 5, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

22. The pharmaceutical tablet composition as recited in claim 6, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

23. The pharmaceutical tablet composition as recited in claim 7, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

24. The pharmaceutical tablet composition as recited in claim 8, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

25. The pharmaceutical tablet composition as recited in claim 9, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

26. The pharmaceutical tablet composition as recited in claim 10, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

27. The pharmaceutical tablet composition as recited in claim 11, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

28. The pharmaceutical tablet composition as recited in claim 12, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

29. The pharmaceutical tablet composition as recited in claim 13, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

30. The pharmaceutical tablet composition as recited in claim 14, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

31. The pharmaceutical tablet composition as recited in claim 15, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

32. The pharmaceutical tablet composition as recited in claim 16, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

33. The pharmaceutical tablet composition as claimed in claim 17, wherein the weight of the starch is in a range, of the total weight of the tablet, of about 6% to about 8%.

34. A pharmaceutical tablet composition comprising ibuprofen and hydrocodone bitartrate, said tablet having been prepared by a method comprising the steps of:

(a) granulating ibuprofen, hydrocodone bitartrate, colloidal silicon dioxide, a disintegrant, a filler and starch to form granules, wherein said granulating step comprises a wet granulation process;

(b) blending the granules with extra-granular material to form a blend of granules and extra granular material wherein the composition is substantially free of lactose and polyvinylpyrrolidone and wherein the blend flows well, has good compression performance, and can be compressed over a wide range of compression forces with no substantial change in the disintegration time of a tablet made from such blend; and

(c) compressing the blend into a tablet, wherein said granules and said extragranular material are present in said tablet in a single phase.

35. A pharmaceutical tablet composition comprising ibuprofen and hydrocodone bitartrate, said tablet having been prepared by a method comprising the steps of:

(a) granulating ibuprofen, hydrocodone bitartrate, colloidal silicon dioxide, a disintegrant, a filler and starch to form granules, wherein said granulating step comprises a wet granulation process;

(b) blending the granules with extra-granular material comprised of a lubricant and at least one excipient to form a blend of granules and extra granular material wherein the composition is substantially free of lactose and polyvinylpyrrolidone and wherein the blend flows well and has good compression performance; and

(c) compressing the blend into a tablet, wherein said ibuprofen, said hydrocodone bitartrate and said lubricant are present in said tablet in a single phase.

36. A pharmaceutical tablet composition comprising ibuprofen and hydrocodone bitartrate, said tablet having been prepared by a method comprising the steps of:

(a) granulating by means of a wet granulation process ibuprofen, hydrocodone, a filler and starch to form granules;

(b) blending the granules with extra-granular material to form a blend of granules and extra granular material wherein the composition is substantially free of lactose and polyvinylpyrrolidone and wherein the blend flows well, and has good compression performance; and

(c) compressing the blend into a tablet, wherein said granules and said extragranular material are present in said tablet in a single phase.