COMBINED ADMINISTRATION OF BENZONATATE AND GUAIFENESIN

• US 20080176955A1
• Filed: 01/16/2008
• Published: 07/24/2008
• Est. Priority Date: 01/16/2007
• Status: Abandoned Application

• Current Assignee: Victory Pharma, Inc. (Shionogi & Co., Ltd.)
• Original Assignee: Victory Pharma, Inc. (Shionogi & Co., Ltd.)
• Inventors: Heck, Thomas, Cvijanovich, Michael
• Application Number:
  US12/015,413
• Publication Number:
  US 20080176955A1
• Time in Patent Office: Days
• US Class Current: 514/716
• 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 31/085 having an ether linkage to aromatic ring nuclear carbon
• CPC Class Codes: A61K 31/09 having two or more such linkages
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system

Abstract

Pharmaceutical compositions are provided containing a combination of benzonatate and guaifenesin, or pharmaceutically acceptable salts thereof. Methods of using compositions comprising benzonatate and guaifenesin, or pharmaceutically acceptable salts thereof, provide relief from cough, pulmonary congestion or both. The compositions and methods provide relief to opiate-sensitive individuals, in particular, as well as to infants and other pediatric patients.

Claims

1. A pharmaceutical composition comprising a therapeutically effective combination of benzonatate and guaifenesin, or a pharmaceutically acceptable salt thereof.

2. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is an orally available dosage unit.

3. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is formulated for once-per-day (q.d.) dosing.

4. The pharmaceutical composition of claim 3, wherein the pharmaceutical composition is formulated to deliver about 400 to 800 mg of benzonatate and about 1200 to about 2400 mg of guaifenesin per dose.

5. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is formulated for twice-per-day (b.i.d.) dosing.

6. The pharmaceutical composition of claim 5, wherein the pharmaceutical composition is formulated to deliver about 200 to about 400 mg of benzonatate and about 600 to about 1200 mg of guaifenesin per dose.

7. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is an oral capsule, tablet, caplet or gel cap.

8. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is adapted to provide a dose of about 50 mg to about 400 mg of benzonatate and about 100 mg to about 600 mg of guaifenesin per dosage unit.

9. A method of treating a cough, congestion or both, comprising administering to a patient suffering from a cough a therapeutically effective amount of a composition comprising benzonatate, or a pharmaceutically acceptable salt thereof, and guaifenesin.

10. The method of claim 9, wherein the composition comprising benzonatate, or a pharmaceutically acceptable salt thereof, and guaifenesin is administered in an oral dosage form.

11. The method of claim 10, wherein the oral dosage form is an oral tablet, caplet, capsule or gel cap.

12. The method of claim 9, wherein the therapeutically effective amount of the composition is administered once-per-day.

13. The method of claim 12, wherein the therapeutically effective amount of guaifenesin is about 1200 to about 2400 mg and the therapeutically effective amount of benzonatate is about 400 to about 800 mg.

14. The method of claim 9, wherein the therapeutically effective amount of the composition is administered twice-per-day.

15. The method of claim 14, wherein the therapeutically effective amount of guaifenesin is about 600 to about 1200 mg and the therapeutically effective amount of benzonatate is about 200 to about 400 mg.

16. The method of claim 9, wherein the oral dosage form is adapted to deliver about 50 mg to about 400 mg of benzonatate and about 100 mg to about 600 mg of guaifenesin per dose.

17. The method of claim 9, wherein the oral dosage form is adapted to deliver about 100 mg to about 200 mg of benzonatate and about 200 mg to about 400 mg of guaifenesin per dose.

18. The method of claim 9, wherein the patient is sensitive to opiate-derived antitussives or dextromethorphan.

19. The method of claim 9, wherein the patient is a pediatric patient.

20. The method of claim 19, wherein the composition comprising benzonatate, or a pharmaceutically acceptable salt thereof, and guaifenesin is administered in an oral dosage form.

21. The method of claim 20, wherein the oral dosage form is an oral tablet, caplet, capsule or gel cap.

22. The method of claim 19, wherein the therapeutically effective amount of the composition is administered on a once-per-day basis.

23. The method of claim 22, wherein the therapeutically effective amount of guaifenesin is about 150 to about 1200 mg per dose.

24. The method of claim 22, wherein the therapeutically effective amount of benzonatate is about 50 to about 200 mg per dose.

25. The method of claim 19, wherein the therapeutically effective amount of the composition is administered on a twice-per-day basis.

26. The method of claim 25, wherein the therapeutically effective amount of guaifenesin is about 300 to about 600 mg per dose.

27. The method of claim 25, wherein the therapeutically effective amount of benzonatate is about 50 to about 100 mg per dose.

28. A method of treating congestion of the lung, comprising co-administering to a patient a therapeutically effective amount of benzonatate and guaifenesin, wherein the therapeutically effective amount of benzonatate and guaifenesin comprises a first discrete dosage unit comprising benzonatate or a pharmaceutically acceptable salt thereof and a second discrete dosage unit comprising guaifenesin.

29. The method of claim 28, wherein the first dosage unit does not contain guaifenesin.

30. The method of claim 28, wherein the second dosage unit does not contain benzonatate.

31. The method of claim 28, wherein the first dosage unit, the second dosage unit, or both the first and second dosage units are adapted for oral administration

32. The method of claim 28, wherein the first dosage unit, the second dosage unit, or both the first and second dosage units are in the form of an oral tablet, caplet, capsule or gel cap.

33. The method of claim 28, wherein the first dosage unit and the second dosage unit together are adapted to deliver about 50 mg to about 400 mg of benzonatate or a bioequivalent amount of a pharmaceutically acceptable salt of benzonatate and about 100 mg to about 600 mg of guaifenesin per dose.

34. The method of claim 28, wherein the first dosage unit and the second dosage unit together are adapted to deliver about 200 to about 400 mg of benzonatate or a bioequivalent amount of a pharmaceutically acceptable salt thereof and about 600 to about 1200 mg of guaifenesin per dose.

35. The method of claim 34, wherein the dosage forms are adapted for twice-per-day dosing.

36. The method of claim 28, wherein the first dosage unit and the second dosage unit together are adapted to deliver about 400 to about 800 mg of benzonatate or a bioequivalent amount of a pharmaceutically acceptable salt thereof and about 1200 to about 2400 mg of guaifenesin per dose.

37. The method of claim 36, wherein the dosage forms are adapted for once-per-day dosing.

38. The method of claim 28, wherein the first dosage unit and the second dosage unit together are adapted to deliver about 100 mg to about 200 mg of benzonatate or an equivalent amount of a pharmaceutically acceptable salt of benzonatate and about 200 mg to about 400 mg of guaifenesin per dose.

39. The method of claim 28, wherein the first dosage unit is adapted to resist disintegration in the mouth.

40. The method of claim 39, wherein the first dosage unit is in an immediate release or an extended release form.

41. A kit comprising:

(a) a dosage unit comprising benzonatate;

(b) a dosage unit comprising guaifenesin; and

optionally

(c) instructions for the use of the combination of benzonatate and guaifenesin for the treatment of coughing.

42. The kit of claim 41, wherein the dosage unit comprising benzonatate is discrete from the dosage unit comprising guaifenesin.

43. The kit of claim 41, wherein the dosage unit comprising benzonatate contains about 50 to about 800 mg of benzonatate per dosage unit.

44. The kit of claim 41, wherein the dosage unit comprising guaifenesin contains about 50 to about 2400 mg of guaifenesin per dosage unit.

45. The kit of claim 41, wherein the dosage unit comprising benzonatate is in the form of a tablet, a caplet, a capsule or a gel cap.

46. The kit of claim 45, wherein the dosage unit comprising benzonatate is adapted to resist disintegration in the mouth and to dissolve readily in the stomach or intestines.

47. The kit of claim 41, wherein the dosage units are adapted for once-per-day dosing.

48. The kit of claim 47, wherein the kit is adapted for pediatric dosing.

49. The kit of claim 48, wherein the kit is adapted to deliver about 50 to about 200 mg of benzonatate or a bioequivalent amount of a pharmaceutically acceptable salt thereof and about 600 to about 1200 mg of guaifenesin per dose.

50. The kit of claim 47, wherein the kit is adapted to deliver about 400 to about 800 mg of benzonatate or a bioequivalent amount of a pharmaceutically acceptable salt thereof and about 1200 to about 2400 mg of guaifenesin per dose.

51. The kit of claim 41, wherein the dosage units are adapted for twice-per-day dosing.

52. The kit of claim 51, wherein the kit is adapted for pediatric dosing.

53. The kit of claim 52, wherein the kit is adapted to deliver about 50 to about 200 mg of benzonatate or a bioequivalent amount of a pharmaceutically acceptable salt thereof and about 600 to about 1200 mg of guaifenesin per dose.

54. The kit of claim 51, wherein the kit is adapted to deliver about 200 to about 400 mg of benzonatate or a bioequivalent amount of a pharmaceutically acceptable salt thereof and about 600 to about 1200 mg of guaifenesin per dose.

55. The kit of claim 41, wherein the dosage units are adapted for q.i.d. dosing.

56. The kit of claim 55, wherein the kit is adapted to deliver bout 50 to about 400 mg of benzonatate or a bioequivalent amount of a pharmaceutically acceptable salt thereof and about 100 to about 600 mg of guaifenesin per dose.