Mouthwash and Method of Using Same for the Treatment of Mucositis or Stomatitis

• US 20100190735A1
• Filed: 04/01/2010
• Published: 07/29/2010
• Est. Priority Date: 03/28/2006
• Status: Abandoned Application

• Current Assignee: Myrex Pharmaceuticals, Inc.
• Original Assignee: Myrex Pharmaceuticals, Inc.
• Inventors: BHASIN, Deepak
• Application Number:
  US12/752,721
• Publication Number:
  US 20100190735A1
• Time in Patent Office: Days
• US Class Current: 514/31
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 31/7048 having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin , digitoxin or digoxin
• CPC Class Codes: A61K 8/365 Hydroxycarboxylic acids; Ketocarboxylic acids
• CPC Class Codes: A61K 8/41 Amines
• CPC Class Codes: A61K 8/411 Aromatic amines, i.e. where the amino group is directly linked to the aromatic nucleus
• CPC Class Codes: A61K 8/498 having 6-membered rings or their condensed derivatives, e.g. coumarin
• CPC Class Codes: A61K 8/63 Steroids; Derivatives thereof
• 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 31/04 Antibacterial agents
• CPC Class Codes: A61Q 11/00 Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Abstract

An oral rinse formulation for the treatment or prophylaxis of mucositis or stomatitis comprises one or more of the following components in combination with pharmaceutically acceptable excipients or additives: a) at least one corticosteroid; b) at least one anti-histamine; c) at least one topical anaesthetic; and, d) at least one anti-fungal antibiotic agent. A stable nystatin containing formulation is also provided comprising a buffering agent, a preservative, a chelating agent and an anti-oxidant.

Claims

1. A stable oral rinse formulation comprising the following components in combination with pharmaceutically acceptable excipients or additives:

a) at least one corticosteroid;

b) at least one anti-histamine;

c) at least one topical anaesthetic; and

d) at least one anti-fungal antibiotic agent;

wherein, said formulation exhibits stability for at least 2 months at room temperature.

2. The formulation of claim 1 having the following composition:

0.005 to 0.025 mg/ml dexamethasone;

1 to 2 mg/ml diphenhydramine;

1 to 20 mg/ml lidocaine; and

10,000 to 50,000 iu/ml nystatin.

3. The formulation of claim 2 wherein the additives are chosen from the group consisting of:

polysorbate 80, spearmint oil, sorbitol, xanthan gum, sodium benzoate, purified water, aluminium hydroxide, dextrose, sucralose, flavorings and magnesium hydroxide.

4. The formulation of claim 2 further comprising at least one buffering agent, at least one preservative, at least one chelating agent and at least one anti-oxidant.

5. The formulation of claim 4 wherein the buffering agent is a phosphate buffer, the preservative is methyl paraben or propyl paraben, the chelating agent is EDTA, and the anti-oxidant is citric acid or a salt thereof.

6. Use of the formulation of claim 1 for the treatment of oral lesions.

7. The use of claim 1 for the treatment of mucositis or stomatitis.

8. A stable, anti-fungal oral rinse formulation comprising nystatin and a buffering agent, a preservative, a chelating agent and an anti-oxidant, said formulation exhibiting stability for at least 2 months at room temperature.

9. The formulation of claim 8 wherein the buffering agent is a phosphate buffer.

10. The formulation of claim 8 wherein the preservative is methyl paraben or propyl paraben.

11. The formulation of claim 8 wherein the chelating agent is EDTA.

12. The formulation of claim 8 wherein the anti-oxidant is citric acid or a salt thereof.

13. The formulation of claim 8 wherein the nystatin is present in an amount greater than 10,000 iu/ml.

14. A stable, anti-fungal oral rinse formulation comprising:

an anti-fungal antibiotic agent selected from nystatin and amphotericin B;

a phosphate buffer;

a preservative;

a chelating agent; and

,

an antioxidant;

said formulation exhibiting stability for at least 2 months at room temperature.

15. The formulation of claim 14 wherein the nystatin is present in an amount between 10,000 and 50,000 iu/ml.

16. The formulation of claim 14 wherein the preservative is chosen from methyl paraben, propyl paraben and mixtures thereof.

17. The formulation of claim 14 wherein the chelating agent is ethylenediamine tetraacetic acid (EDTA).

18. The formulation of claim 14 wherein the antioxidant is citric acid or a salt thereof.

19. The formulation of claim 14 further comprising:

at least one corticosteroid;

at least one antihistamine; and

at least one topical anaesthetic.

20. The formulation of claim 19, wherein:

the corticosteroid is dexamethasone at a concentration of between 0.005 to 0.025 mg/ml;

the antihistamine is diphenhydramine, at a concentration of between 1 to 2 mg/ml; and

,

the topical anaesthetic is lidocaine, at a concentration of between 1 to 20 mg/ml.