DISINTEGRABLE ORAL FILMS

• US 20070202057A1
• Filed: 02/16/2007
• Published: 08/30/2007
• Est. Priority Date: 02/17/2006
• Status: Abandoned Application

• Current Assignee: Novartis Ag
• Original Assignee: Novartis Ag
• Inventors: Meyer, Stephan, Slominski, Greg, Fankhauser, Christopher
• Application Number:
  US11/675,822
• Publication Number:
  US 20070202057A1
• Time in Patent Office: Days
• US Class Current: 424/48
• CPC Class Codes: A61K 31/465 Nicotine; Derivatives thereof
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/7007 Drug-containing films, membranes or sheets A61K9/0041, A61K9/0043, A61K9/006, A61K9/0063 take precedence
• CPC Class Codes: A61P 25/34 Tobacco-abuse

Abstract

A water soluble film that is disintegrable in the oral cavity to deliver an active agent is provided. The disintegrable film includes at least one water soluble polymer and an active agent. Also provided are methods for preparing the disintegrable oral film and for using the disintegrable film to administer an effective dosage of an active agent into the oral cavity for absorption through the oral mucosa. According to certain embodiments, the disintegrable film includes at least one water soluble polymer and a nicotine active.

Claims

1. A disintegrable oral film having high mucoadhesivity to the oral mucosa and slow disintegration rate, comprising:

at least 45 weight percent of at least one water soluble film forming polymer, based on the total weight of the dry film; and

an active agent,

wherein said oral film maintains at least partial integrity and active agent release capability after in vitro exposure to artificial human saliva solution for at least 15 minutes.

2. The disintegrable oral film of claim 1, wherein said disintegrable oral film comprises from about 45 to about 90 weight percent of said at least one water soluble polymer, based on the total weight of the dry film.

3. The disintegrable oral film of claim 1, wherein said disintegrable oral film comprises a mixture of two different water soluble film forming polymers.

4. The disintegrable oral film of claim 3, wherein said disintegrable oral film comprises a mixture of a polyalkylene oxide and a cellulose polymer.

5. The disintegrable oral film of claim 4, wherein said polyalkylene oxide is polyethylene oxide and said cellulose polymer is hydroxypropyl methylcellulose.

6. The disintegrable oral film of claim 5, wherein the ratio of polyethylene oxide to hydroxypropyl methylcellulose in the film is from about 1:

2 to about 1;

5 (wt/wt).

7. The disintegrable oral film of claim 6, wherein said ratio of polyethylene oxide to hydroxypropyl methylcellulose in the film is about 1:

2.

8. The disintegrable oral film of claim 6, wherein said ratio of polyethylene oxide to hydroxypropyl methylcellulose in the film is about 1:

3.

9. The disintegrable oral film of claim 6, wherein said ratio of polyethylene oxide to hydroxypropyl methylcellulose in the film is about 1:

4.

10. The disintegrable oral film of claim 6, wherein said ratio of polyethylene oxide to hydroxypropyl methylcellulose in the film is about 1:

5.

11. The disintegrable oral film of claim 1 which additionally comprises a gum.

12. The disintegrable oral film of claim 2 which comprises hydroxypropyl methylcellulose and xanthan gum.

13. The disintegrable oral film of claim 2 which comprises hydroypropyl methylcellulose and arabic gum.

14. The disintegrable oral film of claim 5, wherein said active agent is a nicotine active.

15. The disintegrable oral film of claim 11, wherein said nicotine active comprises free nicotine base, nicotine derivatives, nicotine complexes, nicotine salts, or mixtures thereof.

16. The disintegrable oral film of claim 12, wherein said nicotine active is nicotine bitartrate.

17. A disintegrable oral film for delivery of nicotine comprising:

a mixture of a polyalkylene oxide and a cellulose polymer, wherein the ratio of said polyalkylene oxide to said cellulose polymer present in said film is about 1;

2 to about 1;

5 (wt/wt); and

a nicotine active.

18. The disintegrable oral film of claim 17, wherein said polyalkylene oxide is polyethylene oxide said cellulose polymer is hydroxypropyl methylcellulose.

19. The disintegrable oral film of claim 18, wherein said ratio of polyethylene oxide to hydroxypropyl methylcellulose in the film is about 1:

2.

20. The disintegrable oral film of claim 18, wherein said ratio of polyethylene oxide to hydroxypropyl methylcellulose in the film is about 1:

3.

21. The disintegrable oral film of claim 18, wherein said ratio of polyethylene oxide to hydroxypropyl methylcellulose in the film is about 1:

4.

22. The disintegrable oral film of claim 18, wherein said ratio of polyethylene oxide to hydroxypropyl methylcellulose in the film is about 1:

5.

23. The disintegrable oral film of claim 17, wherein said nicotine active comprises free nicotine base, nicotine derivatives, nicotine complexes, nicotine salts, or mixtures thereof.

24. The disintegrable oral film of claim 23, wherein said nicotine active is nicotine bitartrate.

25. The disintegrable oral film of claim 17 wherein said film maintains at least partial integrity and active agent release capability after in vitro exposure to artificial human saliva solution for at least 15 minutes.

26. A disintegrable oral film for delivery of nicotine comprising:

a mixture of a polyalkylene oxide and a cellulose polymer, wherein the ratio of said polyalkylene oxide to said cellulose polymer present in said film is about 1;

2 to about 1;

5; and

nicotine bitartrate,

wherein said film maintains at least partial integrity and active agent release capability after in vitro exposure to artificial human saliva solution for at least 15 minutes.

27. A method for preparing a disintegrable oral film comprising:

mixing together at least one water soluble film forming polymer, and an active agent to form a mixture; and

forming a film from the mixture, wherein said film comprises at least 45 weight percent of said water soluble polymer based on the total weight of the dry film.

28. A method for preparing a disintegrable oral film comprising:

mixing together at least one polyalkylene oxide polymer, at least one cellulose polymer, and an active agent to form a mixture, wherein the ratio of said polyalkylene oxide polymer to said cellulose polymer present in said film is about 1;

2 to about 1;

5 (wt/wt); and

forming a film from the mixture.

29. A method of administering an active agent comprising:

providing a disintegrable oral film comprising least 45 weight percent of at least one water soluble film forming polymer, based on the total weight of the dry film, and an active agent; and

introducing said film into the oral cavity.

30. A method of administering an active agent comprising:

providing a disintegrable film comprising a mixture of a polyalkylene oxide and a cellulose polymer, wherein the ratio of said polyalkylene oxide to said cellulose polymer present in said film is about 1;

2 to about 1;

5 (wt/wt) and an active agent; and

introducing said film into the oral cavity.

31. A method of administering an active agent comprising:

providing a disintegrable oral film comprising at least one water soluble film forming polymer, wherein said oral film maintains at least partial integrity and active agent release capability after in vitro exposure to artificial human saliva solution for at least 15 minutes; and

introducing said film into the oral cavity.