Process for reducing the adverse taste and malodor associated with H.sub.2 -antagonists

• US 5,576,344 A
• Filed: 08/30/1994
• Issued: 11/19/1996
• Est. Priority Date: 08/30/1994
• Status: Expired due to Term

• Current Assignee: Wyeth (Pfizer Inc.)
• Original Assignee: American Home Products Corporation (Pfizer Inc.)
• Inventors: Patel, Kalpana, Sandler, Patricia L., Seabrook, Alexander, Mogavero, Annabelle
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): HOWARD, SHARON LEE
• Application Number:
  US08/300,494
• Time in Patent Office: 812 Days
• Field of Search: 424/467, 424/440, 424/484, 424/485, 514/819, 514/925, 514/922, 514/926, 514/421
• US Class Current: 514/427
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61K 31/425 Thiazoles
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00

Abstract

The present invention is directed to a process for reducing the adverse taste and malodor associated with the H₂ -antagonist nizatidine. The process involves forming an aqueous solution of the H₂ -antagonist, and subjecting said solution to elevated temperatures sufficient for a period sufficient to cause a reduction in the adverse taste and/or malodor of the H₂ -antagonist.

Claims

1. A process for reducing the adverse taste and malodor associated with an H₂ -antagonist selected from the group consisting of cimetidine, nizatidine and famotidine comprising

(a) forming an aqueous solution of the H₂ -antagonist, and

(b) subjecting said aqueous solution to elevated temperatures sufficient for a period sufficient to cause a reduction in the adverse taste and/or malodor of the H₂ -antagonist.

2. The process of claim 1 wherein the aqueous solution is elevated to a temperature ranging from about 80 degrees Centigrade and a temperature below which degradation of the H₂ -antagonist occurs.

3. The process of claim 1 wherein the aqueous solution is elevated to a temperature ranging from about 80 to about 120 degrees Centigrade.

4. The process of claim 3 wherein the aqueous solution is elevated to a temperature ranging from about 90 to about 110 degrees Centigrade.

5. The process of claim 3 wherein the aqueous solution is elevated to a temperature of about 100 degrees Centigrade.

6. The process of claim 1 wherein the H₂ -antagonist is nizatidine.

7. The process of claim 6 wherein the aqueous solution is elevated to a temperature ranging from about 80 to about 120 degrees Centigrade.

8. The process of claim 6 wherein the aqueous solution is elevated to a temperature ranging from about 90 to about 110 degrees Centigrade.

9. The process of claim 6 wherein the aqueous solution is elevated to a temperature of about 100 degrees Centigrade.

10. The process of claim 1 wherein the temperature of the aqueous solution is elevated for a period of time of between about 5 minutes and 2 hours.

11. The process of claim 10 wherein the temperature of the aqueous solution is elevated for a period of time of between about 15 minutes and 2 hours.

12. The process of claim 6 wherein the aqueous solution is elevated to a temperature of about 100 degrees. Centigrade for a period of time of about 30 minutes.