Controlled release and taste masking oral pharmaceutical compositions

• US 10,143,698 B2
• Filed: 07/11/2017
• Issued: 12/04/2018
• Est. Priority Date: 06/14/1999
• Status: Expired due to Fees

• Current Assignee: Cosmo Technologies Limited (Cosmo Pharmaceuticals NV)
• Original Assignee: Cosmo Technologies Limited (Cosmo Pharmaceuticals NV)
• Inventors: Villa, Roberto, Pedrani, Massimo, Ajani, Mauro, Fossati, Lorenzo
• Primary Examiner(s): Tran, Susan T
• Application Number:
  US15/646,330
• Publication Number:
  US 20170304322A1
• Time in Patent Office: 511 Days
• Field of Search: None
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• 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: A61K 9/28 Dragees; Coated pills or tablets , e.g. with film or compression coating A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209
• CPC Class Codes: A61K 9/2806 Coating materials
• CPC Class Codes: A61K 9/2813 Inorganic compounds
• CPC Class Codes: A61K 9/282 Organic compounds, e.g. fats
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 11/08 Bronchodilators
• CPC Class Codes: A61P 11/14 : Antitussive agents
• CPC Class Codes: A61P 25/00 : Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 : Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/16 : Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 : Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/22 : Anxiolytics
• CPC Class Codes: A61P 29/00 : Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/10 : for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/04 : Antibacterial agents
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 : Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/12 : Antihypertensives

Abstract

The invention relates to tablet comprising granules dispersed in at least one hydrophilic compound or matrix. The granules contain an active agent, at least one amphiphilic compound and at least one lipophilic compound. The tablet may include a gastro-resistant film coating.

Claims

1. A controlled release oral pharmaceutical composition consisting essentially of:

(1) a tablet core consisting of a mixture comprising;

a) budesonide in an amount to treat intestinal inflammation;

b) magnesium stearate, stearic acid, or a mixture thereof;

c) lecithin; and

d) hydroxyalkyl cellulose; and

(2) a coating on said tablet core, said coating consisting essentially of a gastro-resistant film.

2. The controlled release oral pharmaceutical composition according to claim 1, wherein said mixture further comprises silicon dioxide.

3. The controlled release oral pharmaceutical composition according to claim 1, wherein said mixture comprises magnesium stearate.

4. The controlled release oral pharmaceutical composition according to claim 1, wherein said mixture comprises stearic acid.

5. The controlled release oral pharmaceutical composition according to claim 3, wherein said mixture further comprises silicon dioxide.

6. The controlled release oral pharmaceutical composition according to claim 4, wherein said mixture further comprises silicon dioxide.

7. The controlled release oral pharmaceutical composition according to claim 1, wherein said mixture further comprises starch or a starch derivative.

8. The controlled release oral pharmaceutical composition according to claim 2, wherein said mixture further comprises starch or a starch derivative.

9. The controlled release oral pharmaceutical composition according to claim 3, wherein said mixture further comprises starch or a starch derivative.

10. The controlled release oral pharmaceutical composition according to claim 4, wherein said mixture further comprises starch or a starch derivative.

11. The controlled release oral pharmaceutical composition according to claim 5, wherein said mixture further comprises starch or a starch derivative.

12. The controlled release oral pharmaceutical composition according to claim 6, wherein said mixture further comprises starch or starch derivative.

13. The controlled release oral pharmaceutical composition according to claim 1, wherein said gastro-resistant film comprises methacrylic acid polymer.

14. The controlled release oral pharmaceutical composition according to claim 3, wherein said mixture further comprises silicon dioxide and starch or a starch derivative, and said gastro-resistant film comprises methacrylic acid polymer.

15. The controlled release oral pharmaceutical composition according to claim 14, wherein said mixture comprises starch.

16. The controlled release oral pharmaceutical composition according to claim 14, wherein said mixture comprises a starch derivative.

17. The controlled release oral pharmaceutical composition according to claim 4, wherein said mixture further comprises silicon dioxide and starch or a starch derivative, and said gastro-resistant film comprises methacrylic acid polymer.

18. The controlled release oral pharmaceutical composition according to claim 17, wherein said mixture comprises starch.

19. The controlled release oral pharmaceutical composition according to claim 17, wherein said mixture comprises a starch derivative.

20. A method for treating intestinal inflammatory disease in a patient, comprising administering to the patient the controlled release oral pharmaceutical composition according to claim 1.

21. A method for treating intestinal inflammatory disease in a patient, comprising administering to the patient the controlled release oral pharmaceutical composition according to claim 14.

22. A method for treating intestinal inflammatory disease in a patient, comprising administering to the patient the controlled release oral pharmaceutical composition according to claim 17.

23. The controlled release oral pharmaceutical composition according to claim 1, wherein:

a) said mixture comprises 9 mg of budesonide;

b) said hydroxyalkyl cellulose is hydroxypropyl cellulose, hydroxypropyl methylcellulose, or a mixture of hydroxypropyl cellulose and hydroxypropyl methylcellulose; and

c) said mixture further comprises lactose, silicon dioxide, and microcrystalline cellulose.

24. The controlled release oral pharmaceutical composition according to claim 23, wherein said hydroxyalkyl cellulose is hydroxypropyl cellulose.

25. The controlled release oral pharmaceutical composition according to claim 23, wherein said hydroxyalkyl cellulose is hydroxypropyl methylcellulose.

26. The controlled release oral pharmaceutical composition according to claim 23, wherein said hydroxyalkyl cellulose is a mixture of hydroxypropyl cellulose and hydroxypropyl methylcellulose.

27. The controlled release oral pharmaceutical composition according to claim 23, wherein said mixture further comprises starch or a starch derivative.

28. The controlled release oral pharmaceutical composition according to claim 27, wherein said mixture comprises a starch derivative.

29. A method for treating intestinal inflammatory disease in a patient, comprising administering to the patient the controlled release oral pharmaceutical composition according to claim 23.