Tablets having improved bioadhesion to mucous membranes

• US 4,915,948 A
• Filed: 08/31/1987
• Issued: 04/10/1990
• Est. Priority Date: 08/31/1987
• Status: Expired due to Fees

• Current Assignee: Warner-Lambert Company (Pfizer Inc.)
• Original Assignee: Warner-Lambert Company (Pfizer Inc.)
• Inventors: Gallopo, Andrew R., Dills, Steven S.
• Primary Examiner(s): Page, Thurman K.
• Application Number:
  US07/091,575
• Time in Patent Office: 953 Days
• Field of Search: 424/435, 424/464, 424/499
• US Class Current: 424/435
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin

Abstract

A tablet having improved bioadhesion to mucous membranes is disclosed. The tablet comprises effective amounts of a water-soluble biopolymer selected from the group consisting of a xanthan gum, a pectin and mixtures thereof; and a solid polyol having a solubility at room temperature in water greater than about 20 grams of polyol per 100 g of solution. Preferably the biopolymer is xanthan gum and the polyol is a sugar alcohol selected from the group consisting of sorbitol, xylitol, and mixtures thereof.

Claims

1. A tablet having improved bioadhesion to mucous membranes comprising:

(a) a water-soluble natural biopolymer in an amount of from about 40 to about 80 weight percent of the tablet, selected from the group consisting of a xanthan gum, a pectin and mixtures thereof; and

(b) a solid polyol in an amount of from about 20 to about 60 weight percent of the tablet and having a solubility at room temperature in water greater than about 20 grams of polyol per 100 g of solution.

4. The tablet of claim 1 wherein said biopolymer is present in amounts of about 50 to about 70% by weight of the composition and said polyol is present in amounts of about 30 to about 50% by weight of the composition.

5. The tablet of claim 1 wherein said polyol is a sugar alcohol.

6. The tablet of claim 1 wherein said polyol is a sugar alcohol selected from the group consisting of sorbitol, xylitol, and mixtures thereof.

7. The tablet of claim 6 wherein said sugar alcohol is present in an amount of about 20 to about 60% by weight of the tablet and the biopolymer is present in an amount of about 40 to about 80% by weight of the tablet.

8. The tablet of claim 7 wherein said sugar alcohol is present in an amount of about 30 to about 50% by weight and said biopolymer is present in an amount of about 50 to about 70% by weight.

10. The tablet of claim 7 wherein said biopolymer is a xanthan gum.

11. The tablet of claim 8 wherein said biopolymer is a xanthan gum.

12. The tablet of claim 1 wherein there is additionally included an effective amount of a lubricant.

13. The tablet of claim 12 wherein said lubricant is selected from the group consisting of metallic stearates and mixtures thereof.

14. The tablet of claim 13 wherein said lubricant is calcium stearate.

15. The tablet of claim 1 wherein there is additionally included effective amounts of an active agent selected from the group consisting of:

flavorings, local antiseptics, local anesthetics, anti-cariogenic compounds, anti-inflammatory agents, antifungal agents, antiplaque agents, tooth desensitizers, and mixtures thereof.

16. The tablet of claim 15 wherein said active agent is a liquid and said tablet additionally contains an effective amount of a vehicle.

17. The tablet of claim 16 wherein said vehicle is selected from the group consisting of colloidal silica particles, magnesium aluminum silicate, dextrose, magnesium trisilicate, modified maltodextrin, and mixtures thereof.

18. The tablet of claim 17 wherein the active agent is a flavoring.

19. The tablet of claim 18 wherein said flavoring is selected from the group consisting of spearmint oil, cinnamon oil, oil of wintergreen, peppermint oil, and mixtures thereof.

20. The tablet of claim 17 wherein said vehicle is comprised of colloidal silica particles sintered together in chain-like formations.

21. The tablet of claim 1 wherein there is additionally included an effective amount of a sweetener selected from the group consisting of artificial sweeteners, high intensity sweeteners, and mixtures thereof.

22. The tablet of claim 15 wherein said active agent is an anti-cariogenic material comprising an orally ingestible fluoride containing compound.

23. The tablet of claim 22 wherein said active ingredient is selected from the group consisting of sodium fluoride, sodium monofluorophosphate, stannous fluoride and mixtures thereof.

2. A tablet having improved bioadhesion to mucous membranes comprising

(a) a xanthan gum present in amounts of about 40 to about 80% by weight of the composition;

(b) a sugar alcohol having a solubility at room temperature in water greater than about 20 g per 100 g solution selected from the group consisting of sorbitol, xylitol, and mixtures, said sugar alcohol being present in an amount of about 20 to about 60% by weight of the composition;

wherein there is additionally included an effective amount of a lubricant;

wherein there is additionally included an effective amount of an active ingredient selected from the group consisting of flavorings, local anesthetics, local antiseptics, anti-cariogenic compounds, anti-inflammatory agents, antifungal agents, antiplaque agents, tooth desensitizers and mixtures thereof;

wherein there is optionally included an effective amount of a vehicle; and

wherein there is included an effective amount of sweetener selected from the group consisting of artificial sweeteners, high intensity sweeteners, and mixtures;

such that the total of all components equals 100%.

3. The tablet of claim 2 wherein said active ingredient is a liquid flavoring and said vehicle is present.

9. The tablet of claim 2 wherein said biopolymer is a xanthan gum.

24. The tablet of claim 2 wherein said xanthan gum is present in an amount of about 50 to about 70% by weight of the composition and said sugar alcohol is present in an amount of about 30 to about 50% by weight of the composition.