Oral compositions of H2-antagonists

• US 5,622,980 A
• Filed: 02/02/1995
• Issued: 04/22/1997
• Est. Priority Date: 08/17/1993
• Status: Expired due to Fees

• Current Assignee: aaiPharma, Inc.
• Original Assignee: Applied Analytical Industries, Inc. (aaiPharma, Inc.)
• Inventors: Desai, Ashok J., Caldwell, Henry C.
• Primary Examiner(s): HENLEY III, RAYMOND J
• Application Number:
  US08/382,602
• Time in Patent Office: 810 Days
• Field of Search: 514/370, 514/400, 514/471, 424/683, 424/684, 424/43, 424/44, 424/687
• US Class Current: 514/370
• 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 31/341 not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61K 31/4164 1,3-Diazoles
• CPC Class Codes: A61K 31/425 Thiazoles
• CPC Class Codes: A61K 31/426 1,3-Thiazoles
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/143 with inorganic compounds

Abstract

The present invention provides a pharmaceutical composition for the oral administration of an H₂ -antagonist. The composition includes an H₂ -antagonist and a silicate taste-masking agent capable of forming an adsorbate complex with the H₂ -antagonist wherein the complex exhibits a non-bitter taste. The complex inhibits the release of the H₂ -antagonist in the oral cavity.

Claims

1. A pharmaceutical composition for the oral administration of a therapeutically effective amount of an H₂ -antagonist, wherein said composition exhibits a non-bitter taste, said composition consisting essentially of an H₂ -antagonist, a silicate taste-masking agent capable of forming an adsorbate complex with said H₂ -antagonist, wherein said complex inhibits the release of the H₂ -antagonist in the oral cavity, and between about 2.5 and about 10 percent based upon the weight of the composition of a dissociation agent capable of enhancing the release of said H₂ -antagonist from said adsorbate complex, wherein said dissociation agent comprises calcium carbonate.

2. The pharmaceutical composition according to claim 1, wherein said silicate taste-masking agent comprises magnesium aluminum silicate.

3. The pharmaceutical composition according to claim 1, wherein said H₂ -antagonist is in the form of a pharmaceutically acceptable salt.

4. The pharmaceutical composition according to claim 1, wherein said H₂ -antagonist is in the form of a free base.

5. The pharmaceutical composition according to claim 1 further including a flavoring agent.

6. The pharmaceutical composition according to claim 5, wherein said flavoring agent is selected from the group consisting of citric acid, maleic acid, tartaric acid, mannitol, xylitol, sugar, sorbitol, maltitol, and saccharin.

7. The pharmaceutical composition according to claim 1, wherein said H₂ -antagonist is selected from the group consisting of nizatidine, famotidine, ranitidine, and cimetidine.

8. The pharmaceutical composition according to claim 1, further including a pharmaceutically acceptable carrier.

9. The pharmaceutical composition according to claim 8 in the form of a chewable tablet.

10. The pharmaceutical composition according to claim 8 in the form of a lozenge.

11. The pharmaceutical composition according to claim 8 in the form of granules.

12. The pharmaceutical composition according to claim 1, wherein said calcium carbonate dissociation agent is present in an amount of about 5 percent based upon the weight of the composition.

13. A pharmaceutical composition for the oral administration of a therapeutically effective amount of an H₂ -antagonist, wherein said composition exhibits a non-bitter taste, said composition comprising a non-bitter tasting adsorbate complex of ranitidine hydrochloride and magnesium aluminum silicate, and a dissociation agent consisting of calcium carbonate.

14. A pharmaceutical composition for the oral administration of a therapeutically effective amount of an H₂ -antagonist, wherein said composition exhibits a non-bitter taste, said composition comprising a non-bitter tasting adsorbate complex of ranitidine hydrochloride and magnesium aluminum silicate, a dissociation agent consisting of calcium carbonate, and an a flavoring agent selected from the group consisting of citric acid and xylitol.

15. A method for enhancing the release of an H₂ -antagonist from an oral pharmaceutical formulation comprising an adsorbate complex, said adsorbate complex consisting essentially of a therapeutically effective amount of an H₂ -antagonist and a silicate taste-masking agent, said method comprising incorporating into said pharmaceutical formulation a dissociation agent that enhances the release of said H₂ -antagonist from said adsorbate complex, wherein said dissociation agent comprises calcium carbonate.