Granule formation

• US 20080131516A1
• Filed: 02/07/2008
• Published: 06/05/2008
• Est. Priority Date: 10/26/2001
• Status: Active Grant

• Current Assignee: Merck Canada Incorporated (Merck & Co., Inc.)
• Original Assignee: Merck Canada Incorporated (Merck & Co., Inc.)
• Inventors: Down, Brian
• Granted Patent: US 8,007,830 B2
• Time in Patent Office: Days
• US Class Current: 424/490
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/1676 having a drug-free core with discrete complete coating layer containing drug adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/04 Antipruritics
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/16 Otologicals
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present invention relates to oral granules of montelukast sodium.

Claims

1. Oral granules of montelukast sodium.

2. Oral granules of montelukast sodium comprising a pharmaceutically acceptable substrate coated with montelukast sodium.

4. Oral granules of claim 2 wherein said substrate is spray-dried mannitol.

5. Oral granules of claim 2 wherein said substrate is Pearlitol SD 200.

6. Oral granules of claim 4 wherein said substrate is spray-dried mannitol further agglomerated with a pharmaceutically acceptable binder.

7. Oral granules of claim 6 wherein said binder is selected from hydroxypropyl cellulose, hydroxypropyl methylcellulose, methylcellulose, ethylcellulose, polyvinylpyrrolidone.

8. Oral granules of claim 7 wherein said binder is hydroxypropyl cellulose.

3. Oral granules of montelukast sodium comprising a free-flowing pharmaceutically acceptable substrate coated with montelukast sodium.

9. A flowable and dispersible pharmaceutical composition which comprises granules comprising a pharmaceutically acceptable substrate coated with montelukast sodium, and a pharmaceutically acceptable lubricant.

10. A composition of claim 9 wherein said granules comprise a free-flowing pharmaceutically acceptable substrate coated with montelukast sodium.

11. A composition of claim 9 wherein said granules comprise spray-dried mannitol coated with montelukast sodium.

12. A composition of claim 9 wherein said granules comprise Pearlitol SD 200 coated with montelukast sodium.

13. A composition of claim 9 wherein said granules comprise spray-dried mannitol further agglomerated with a pharmaceutically acceptable binder, and coated with montelukast sodium.

14. A composition of claim 9 wherein said binder is selected from hydroxypropyl cellulose, hydroxypropyl methylcellulose, methylcellulose, ethylcellulose, polyvinylpyrrolidone.

15. A composition of claim 14 wherein said binder is hydroxypropyl cellulose.

16. A composition of claim 9 wherein said lubricant is magnesium stearate or talc.

17. A composition of claim 9 wherein said lubricant is magnesium stearate.

18. A composition of claim 11 wherein said lubricant is magnesium stearate.

19. A composition of claim 12 wherein said lubricant is magnesium stearate.

20. A composition of claim 13 wherein said lubricant is magnesium stearate.