EXTENDED RELEASE FORMULATION CONTAINING A WAX

• US 20090238873A1
• Filed: 03/18/2009
• Published: 09/24/2009
• Est. Priority Date: 03/21/2008
• Status: Abandoned Application

• Current Assignee: Mylan Pharmaceuticals Incorporated (Pfizer Inc.)
• Original Assignee: Mylan Pharmaceuticals Incorporated (Pfizer Inc.)
• Inventors: Addicks, William, Redelman, Glenn A., Wargo, David J., Chattaraj, Sarat C., Bhat, Pavan
• Application Number:
  US12/406,272
• Publication Number:
  US 20090238873A1
• Time in Patent Office: Days
• US Class Current: 424/484
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2068 Compounds of unknown constitution, e.g. material from plants or animals oils, fats, waxes, shellac A61K9/2013
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/04 Antibacterial agents

Abstract

Extended release pharmaceutical formulations are disclosed wherein the formulations contain an extended release portion and an immediate release portion, the extended release portion comprising an active pharmaceutical ingredient and a wax. Methods of making such extended release pharmaceutical formulations are also disclosed.

Claims

1. An extended release pharmaceutical formulation comprising an extended release portion and an immediate release portion, said extended release portion comprising:

(a) an active pharmaceutical ingredient (API), and (b) a wax in an amount of about 2% to about 40% by weight of said extended release portion.

2. The extended release pharmaceutical formulation of claim 1, wherein said amount of wax is about 4% to about 30% by weight of said extended release portion.

3. The extended release pharmaceutical formulation of claim 1, wherein said amount of wax is about 6% to about 23% by weight of said extended release portion.

4. The extended release pharmaceutical formulation of claim 1, wherein said active pharmaceutical ingredient is selected from the group consisting of propranolol, metoprolol, metoprolol tartrate, galantamine, bupropion, diltiazem, oxybutynin, hydrochlorothiazide, metformin, opamine, ciprofloxacin, vancomycin, norvancomycin, daunorubicin, vinca alkaloids, cetrizine, venlafaxine, opioid analgesics, theophylline, verapamil, amlodipine, tramadol, diltiazem, timolol, trospium, pramipexole, and pharmaceutically acceptable salts, hydrates, and solvates thereof.

5. The extended release pharmaceutical formulation of claim 1, wherein an amount of said API in said extended release portion ranges from about 5% to about 75% by weight of said extended release portion.

6. The extended release pharmaceutical formulation of claim 1, wherein an amount of said API in said extended release portion ranges from about 30% to about 70% by weight of said extended release portion.

7. The extended release pharmaceutical formulation of claim 1, wherein an amount of said API in said extended release portion ranges from about 55% to about 60% by weight of said extended release portion.

8. The extended release pharmaceutical formulation of claim 1, wherein said active pharmaceutical ingredient is a mixture of a free base and a salt.

9. The extended release pharmaceutical formulation of claim 8, wherein the ratio of said free base to said salt is about 1:

2 to about 2;

1.

10. The extended release pharmaceutical formulation of claim 8, wherein said API is ciprofloxacin.

11. The extended release pharmaceutical formulation of claim 1, wherein said extended release portion further comprises a matrix-forming component selected from the group consisting of succinic acid, citric acid, malic acid, stearic acid, succinic acid, lactic acid, aspartic acid, glutamic acid, gluconic acid, acetic acid, formic acid, hydrochloric acid, sulphuric acid, phosphoric acid, hydrophilic polymers, polyethylene glycols, pH dependent acrylate polymers or copolymers, and pore forming agents.

12. The extended release pharmaceutical formulation of claim 1, wherein said extended release portion further comprises dibasic calcium phosphate in an amount of about 3% to about 30% by weight of said extended release portion.

13. The extended release pharmaceutical formulation of claim 1, wherein said immediate release portion comprises ciprofloxacin.

14. The extended release pharmaceutical formulation of claim 1, wherein the ratio of said extended release portion to said immediate release portion in said formulation is from about 9:

1 or about 1;

9.

15. An extended release pharmaceutical composition comprising an extended release portion and an immediate release portion, said extended release portion comprising a wax and ciprofloxacin.

16. The extended release pharmaceutical formulation of claim 15, wherein an amount of said wax in said extended release portion ranges from about 2% to about 40% by weight of said extended release portion.

17. The extended release pharmaceutical formulation of claim 16, wherein said amount is from about 4% to about 30% by weight of said composition.

18. The extended release pharmaceutical formulation of claim 17, wherein said amount is from about 6% to about 23% by weight of said composition.

19. The extended release pharmaceutical formulation of claim 15, wherein an amount of said active pharmaceutical ingredient in said extended release portion is from about 55% to about 60% by weight of the extended release portion.

20. The extended release pharmaceutical formulation of claim 15, wherein said immediate release portion comprises an active pharmaceutical ingredient selected from the group consisting of propranolol, metoprolol, metoprolol tartrate, galantamine, bupropion, diltiazem, oxybutynin, hydrochlorothiazide, metformin, opamine, ciprofloxacin, vancomycin, norvancomycin, daunorubicin, vinca alkaloids, cetrizine, venlafaxine, opioid analgesics, theophylline, verapamil, amlodipine, tramadol, diltiazem, timolol, trospium, pramipexole, and pharmaceutically acceptable salts, hydrates, and solvates thereof.

21. An extended release pharmaceutical formulation comprising:

a. an extended release portion comprising an API and carnauba wax; and

b. an immediate release portion comprising an API;

said extended and immediate release portions both comprising the same API.

22. The extended release pharmaceutical formulation of claim 21, wherein said API is ciprofloxacin.

23. The extended release pharmaceutical formulation of claim 21, wherein an amount of said carnauba wax is from about 2% to about 40% by weight of said composition.

24. The extended release pharmaceutical formulation of claim 23, wherein said amount of said carnauba wax is from about 4% to about 30% by weight of said composition.

25. An extended release pharmaceutical formulation comprising:

a. an extended release portion comprising ciprofloxacin in an amount of from about 30% to about 70% by weight of said extended release portion;

a wax in the amount of about 6% to about 23% by weight of the extended release portion; and

stearic acid; and

b. an immediate release portion comprising ciprofloxacin in an amount of from about 5% to about 80% by weight of said immediate release portion.

26. The extended release pharmaceutical formulation of claim 25, wherein said ciprofloxacin in said extended and immediate release portions is a mixture of a ciprofloxacin free base and a ciprofloxacin salt.

27. The extended release pharmaceutical formulation of claim 25, wherein said extended and immediate release portions are comprised of particles, wherein a majority of said particles have a size of at least about 40 mesh.

28. The extended release pharmaceutical formulation of claim 25, wherein about 0% to about 20% of said API is released from said formulation after about 0.25 hours;

wherein about 15% to about 35% of said API is released from said formulation after about 0.5 hours;

wherein about 35% to about 50% of said API is released from said formulation after about 1 hour;

wherein about 50% to about 75% of said API is released from said formulation after about 2 hours;

wherein about 60% to about 85% of said API is released from said formulation after about 6 hours; and

wherein at least about 80% of said API is released from said formulation after about 8 hours.

29. The extended release pharmaceutical formulation of claim 25, wherein said amount of API in said extended release portion is from about 55% to about 65%.