Compositions and methods useful for treatment of respiratory illness

• US 20070254027A1
• Filed: 04/28/2006
• Published: 11/01/2007
• Est. Priority Date: 04/28/2006
• Status: Abandoned Application

• Current Assignee: The Procter & Gamble Company
• Original Assignee: The Procter & Gamble Company
• Inventors: Gledhill, Douglas, Martin, Kelly, Criss, Susan, Ononye, Aloysius
• Application Number:
  US11/413,766
• Publication Number:
  US 20070254027A1
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/16 Amides, e.g. hydroxamic acids
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 31/616 by carboxylic acids, e.g. acetylsalicylic acid
• CPC Class Codes: A61K 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006
• 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 11/04 for throat disorders
• CPC Class Codes: A61P 11/10 Expectorants
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Disclosed are compositions including phenylephrine, its salts, and mixtures thereof, in combination with acetaminophen; and optionally in combination with additional pharmaceutical actives. The compositions have a pH of about 6.5 to about 7.5 and may be substantially free of aldehydes. The invention also provides a method of stabilizing phenylephrine. Also disclosed are methods of treating respiratory illness through administration of a composition comprising phenylephrine, its salts, and mixtures thereof, in combination with acteaminophen; and optionally in combination with additional pharmaceutical actives, wherein the composition has a pH of from about 6.5 to about 7.5 and may be substantially free of aldehydes.

Claims

1. A liquid composition comprising a pharmaceutical active selected from the group consisting of phenylephrine, its free and addition salt forms, and mixtures thereof;

and acetaminophen, wherein said composition has a pH of from about 6.5 to about 7.5.

2. The composition of claim 1 wherein said composition is substantially free of aldehydes.

3. The composition of claim 1 comprising an additional pharmaceutical active.

4. The composition of claim 3 wherein said additional pharmaceutical active is selected from the group consisting of antitussives, antihistamines, non-sedating antihistamines, decongestants, expectorants, analgesics, antipyretic anti-inflammatory agents, local anesthetics, anti-inflammatory agents, demulcents, and mixtures thereof.

5. The composition of claim 4 wherein said additional pharmaceutical active is selected from the group consisting of pharmaceutically acceptable forms of dextromethorphan, ephedrine, pseudoephedrine, phenylpropanolamine, ibuprofen, aspirin, ketoprofen, guaifenesin, ambroxyl, bromhexine, diphenhydramine, chlorpheniramine, doxylamine, triprolidine, clemastine, pyrilamine, promethazine, cetirizine, loratidine, oxycodone, hydrocodone, naproxen, brompheniramine, carbinoxamine, caffeine, benzonatate, pheniramine, fentanyl, azatedine, desloratadine, carbamazepine, buprenorphine, hydromorphone, indomethacin, oxymorphone, phenol, codeine, mesalamine, dichlophenac, sulindac, beclomethaxone, meloxicam, fenoproten, mometasone, menthol, benzocaine, dipyridamole, methscopolamine, and mixtures thereof.

6. The composition of claim 1 further comprising a chelating agent.

7. The composition of claim 6 wherein said chelating agent is selected from the group consisting of:

ethylene diamine tetraacetic acid (EDTA), disodium and calcium salts of EDTA, tetrasodium EDTA, sodium hexametaphosphate (SHMP), citric acid, phosphoric acid, di(hydroxyethyl)glycine, 8-hydroxyquinoline, salts thereof and mixtures thereof.

8. The composition of claim 6 comprising from about 0.0001% to about 1% of said chelating agent, by weight of said composition.

9. The composition of claim 8 comprising from about 0.01% to about 0.3% of said chelating agent, by weight of said composition.

10. The composition of claim 1 further comprising a solvent wherein at least one solvent is selected from the group consisting of:

water, propylene glycol, ethanol, polyethylene glycol, glycerol, sorbitol, and mixtures thereof.

11. The composition of claim 10 comprising from about 30% to about 90% of total solvents, by weight of said composition.

12. The composition of claim 11 comprising from about 35% to about 80% of total solvents, by weight of said composition.

13. The composition of claim 12 comprising from about 40% to about 70% of total solvents, by weight of said composition.

14. The composition of claim 1 further comprising a reducing agent.

15. The composition of claim 14 wherein said reducing agent is selected from the group consisting of metabisulfite and bisulfite, dithiothritol, thiourea, sodium thiosulphate, thioglycolic acid, tert-butyl hydroquinone, acetyl cysteine, hydroquinone, salts thereof and mixtures thereof.

16. The composition of claim 1 further comprising a non-aldehydic aesthetic agent.

17. The composition of claim 16 comprising from about 0.025% to about 5% of said non-aldehydic aesthetic agent, by weight of said composition.

18. The composition of claim 1 further comprising a sweetener.

19. The composition of claim 18 wherein said sweetener comprises sucrose.

20. The composition of claim 18 wherein said sweetener comprises an artificial sweetener.

21. The composition of claim 20 comprising from about 0.0001% to about 5% of said artificial sweetener, by weight of said composition.

22. The composition of claim 20 wherein said artificial sweetener is selected from the group consisting of:

sodium saccharin, acesulfame potassium, sucralose, aspartame, monoammonium glycyrrhizinate, neohesperidin dihydrochalcone, thaumatin, neotame, cyclamates, and mixtures thereof.

23. The composition of claim 1 further comprising a salt selected from the group consisting of sodium chloride, potassium chloride, ammonium chloride, and mixtures thereof.

24. The composition of claim 23 comprising about 0.0001% to about 2% of said salt, by weight of said composition.

25. The composition of claim 24 comprising about 0.25% to about 1% of said salt, by weight of said composition.

26. The composition of claim 1 comprising from about 0.0001% to about 1% phenylephrine, by weight of the composition.

27. The composition of claim 1 comprising from about 0.01% to about 10% of acetaminophen, by weight of the composition.

28. A method for treating a respiratory illness comprising the step of orally administering to a mammal in need of such treatment a liquid composition comprising a pharmaceutical active selected from the group consisting of phenylephrine, its free and addition salt forms, and mixtures thereof;

and acetaminophen, wherein said composition has a pH of from about 6.5 to about 7.5.

29. The method of claim 28 wherein the composition is substantially free of aldehydes.

30. The method of claim 28 further comprising an additional pharmaceutical active selected from the group consisting of antitussives, antihistamines, non-sedating antihistamines, decongestants, expectorants, analgesics, antipyretic anti-inflammatory agents, local anesthetics, anti-inflammatory agents, demulcents, and mixtures thereof.

31. The method of claim 30 wherein said additional pharmaceutical active is selected from the group consisting of pharmaceutically acceptable forms of dextromethorphan, ephedrine, pseudoephedrine, phenylpropanolamine, ibuprofen, aspirin, ketoprofen, guaifenesin, ambroxyl, bromhexine, diphenhydramine, chlorpheniramine, doxylamine, triprolidine, clemastine, pyrilamine, promethazine, cetirizine, loratidine, oxycodone, hydrocodone, naproxen, brompheniramine, carbinoxamine, caffeine, benzonatate, pheniramine, fentanyl, azatedine, desloratadine, carbamazepine, buprenorphine, hydromorphone, indomethacin, oxymorphone, phenol, codeine, mesalamine, dichlophenac, sulindac, beclomethaxone, meloxicam, fenoproten, mometasone, menthol, benzocaine, dipyridamole, methscopolamine, the free and the addition salt forms thereof, and mixtures thereof.

32. The method of claim 28 further comprising an agent selected from the group consisting of:

reducing agents, chelating agents, and mixtures thereof.

33. The method of claim 32 comprising said reducing agent and said chelating agent.

34. The method of claim 28 comprising administering from about 5 ml to about 50 ml of said composition per dose.

35. The method of claim 29 wherein said composition is administered at least once daily.

36. A method of stabilizing phenylephrine comprising the step of combining phenylephrine with acetaminophen in a composition having a pH of from about 6.5 to about 7.5.