Methods and pharmaceutical compositions for treating episodic heartburn

• US 5,229,137 A
• Filed: 05/06/1992
• Issued: 07/20/1993
• Est. Priority Date: 05/06/1992
• Status: Expired due to Term

• Current Assignee: Brigham and Women's Hospital Incorporated
• Original Assignee: Brigham and Women's Hospital Incorporated
• Inventors: Wolfe, M. Michael
• Primary Examiner(s): Waddell, Frederick E.
• Assistant Examiner(s): Henley, III, Raymond J.
• Application Number:
  US07/879,662
• Time in Patent Office: 440 Days
• Field of Search: 424/688, 424/687, 424/682, 424/690, 424/692, 424/717, 514/400, 514/461, 514/820, 514/63, 514/365, 514/370, 514/819
• US Class Current: 424/687
• 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 31/34 having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61K 31/425 Thiazoles
• CPC Class Codes: A61K 33/00 Medicinal preparations containing inorganic active ingredients
• CPC Class Codes: A61K 33/08 Oxides; Hydroxides
• CPC Class Codes: A61K 33/10 Carbonates; Bicarbonates

Abstract

Pharmaceutical medications and methods are disclosed for providing instant and sustained relief from pain or symptoms associated with episodic heartburn in humans. The medications consist essentially of antacids and histamine H₂ -receptor antagonists, and may be administered on an as-needed basis in liquid or solid dosage forms. Typical antacids which may be used in combination with the histamine H₂ -receptor antagonist are conventional antacids which are well known and widely used in the treatment of excess acid related gastrointestinal dysfunctions. Exemplary of typical antacids include, sodium bicarbonate, calcium carbonate, magnesium hydroxide and aluminum hydroxide, as well as commercially available high potency, flavored antacids. Histamine H₂ -receptor antagonists which may be used in combination include those conventionally used in the treatment of peptic ulcers, such as, for example, cimetidine, ranitidine, famotidine and nizatidine. In carrying out the methods, an antacid and histamine H₂ -receptor antagonist may be administered together as a single unitary dose in the form of a liquid or solid, or administered together, but separately as either liquids or solids or a combination thereof. The oral medications when formulated as a single unitary dose may include other additives, such as, for example, antiflatulents, flavorings, sweeteners and the like.

Claims

1. A method of providing immediate and sustained relief from pain, discomfort and/or symptoms associated with episodic heartburn in a human, said method comprising:

orally administering to a human together or substantially together an antacid in an amount effective to substantially neutralize gastric acid and a histamine H₂ -receptor antagonist in an amount effective to substantially inhibit or block gastric acid secretion for providing the human with immediate and sustained relief from pain, discomfort and/or symptoms associated with episodic heartburn, the immediate and sustained relief provided lasting longer in duration than when the human is orally treated with only the antacid and the immediate and sustained relief provided being faster than and lasting at least about as long in duration as when the human is orally treated with only the histamine H₂ -receptor antagonist.

2. A method of claim 1, the histamine H₂ -receptor antagonist being cimetidine.

3. A method of claim 1, the histamine H₂ -receptor antagonist being ranitidine.

4. A method of claim 1, the histamine H₂ -receptor antagonist being selected from a group consisting of famotidine and nizatidine.

5. A method of claim 1, the antacid being selected from a group consisting of aluminum hydroxide, calcium carbonate, magnesium hydroxide, sodium bicarbonate and mixtures thereof.

6. A method of claim 1, the antacid being a high potency antacid.

7. A method of claim 1, the antacid being a flavored antacid.

8. A method of claim 2, the cimetidine being administered in a daily dosage amount of between about 200 mg and about 1200 mg.

9. A method of claim 3, the ranitidine being administered in a daily dosage amount of between about 100 mg and about 450 mg.

10. A method of claim 1, said method including the further step of administering an effective gas inhibiting amount of an antiflatulent.

11. A method of claim 10, the antiflatulent being simethicone.

12. A method of claim 1, the antacid and the histamine H₂ -receptor antagonist being administered in a dosage form selected from a group consisting of liquid and solid dosage forms and mixtures thereof.

13. An oral pharmaceutical medication for providing immediate and sustained relief from pain, discomfort and/or symptoms associated with episodic heartburn in a human, said oral pharmaceutical medication consisting essentially of:

an antacid in an amount effective to substantially neutralize gastric acid;

a histamine H₂ -receptor antagonist in an amount effective to substantially inhibit or block gastric acid secretion; and

a pharmaceutically acceptable carrier;

said oral pharmaceutical medication providing immediate and sustained relief from pain, discomfort and/or symptoms associated with episodic heartburn in the human, said immediate and sustained relief lasting longer in duration than when the human is orally treated with only the antacid and being faster than and lasting at least about as long in duration as when the human is orally treated with only the histamine H₂ -receptor antagonist.

14. A pharmaceutical medication of claim 13, said oral pharmaceutical medication being in a liquid dosage form.

15. A pharmaceutical medication of claim 13, said oral pharmaceutical medication being in a solid dosage form.

16. A pharmaceutical medication of claim 13, said histamine H₂ -receptor antagonist being cimetidine.

17. A pharmaceutical medication of claim 16, said cimetidine being present in an amount of between about 200 mg and about 300 mg.

18. A pharmaceutical medication of claim 13, said histamine H₂ -receptor antagonist being ranitidine.

19. A pharmaceutical medication of claim 18, said ranitidine being present in an amount of between about 100 mg and about 150 mg.

20. A pharmaceutical medication of claim 13, said histamine H₂ -receptor antagonist being selected from a group consisting of famotidine and nizatidine.

21. A pharmaceutical medication of claim 13, said antacid being selected from a group consisting of aluminum hydroxide, calcium carbonate, magnesium hydroxide, sodium bicarbonate and mixtures thereof.

22. A pharmaceutical medication of claim 13, said antacid being a flavored antacid.

23. A pharmaceutical medication of claim 13, said antacid being a high potency antacid.

24. A pharmaceutical medication of claim 13, said oral medication further including an effective amount of an antiflatulent.

25. A pharmaceutical medication of claim 24, said antiflatulent being simethicone.

26. A pharmaceutical medication of claim 13, said antacid being aluminum hydroxide and magnesium hydroxide, and said histamine H₂ -receptor antagonist being cimetidine.

27. A pharmaceutical medication of claim 13, said antacid being aluminum hydroxide and magnesium hydroxide, and said histamine H₂ -receptor antagonist being ranitidine.