Effervescent alendronate formulation

• US 5,853,759 A
• Filed: 05/08/1997
• Issued: 12/29/1998
• Est. Priority Date: 05/17/1996
• Status: Expired due to Term

• Current Assignee: Merck Sharp & Dohme Corporation (Merck & Co., Inc.)
• Original Assignee: Merck & Co., Inc.
• Inventors: Katdare, Ashok V., Kramer, Kenneth A., Gardner, Colin R.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Spear, James M.
• Application Number:
  US08/848,460
• Time in Patent Office: 600 Days
• Field of Search: 424/466, 424/489
• US Class Current: 424/466
• CPC Class Codes: A61K 31/663 Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
• CPC Class Codes: A61K 31/675 having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• CPC Class Codes: A61K 9/0007 Effervescent A61K9/0065 takes precedence

Abstract

An effervescent formulation of alendronate contains an acid source, a carbonate source, a binder, a lubricant and optionally, flavoring agents, colorants and sweeteners.

Claims

1. A formulation comprising (in mg):

space="preserve" listing-type="tabular">______________________________________ Alendronate sodium 5-10 mg (in mg alendronic acid) citric acid 600-750 sodium bicarbonate 300-500 sodium carbonate 20-60 sodium benzoate 5-15 water 0-5. ______________________________________

2. A formulation according to claim 1, further comprising a flavoring agent or a colorant.

3. A formulation comprising (in mg):

space="preserve" listing-type="tabular">______________________________________ Alendronate sodium 5-10 (in mg alendronic acid) citric acid 450-650 sodium bicarbonate (total) 800-1150. ______________________________________

4. A formulation comprising (in mg):

space="preserve" listing-type="tabular">______________________________________ Alendronate sodium 2.5-10 (in mg alendronic acid) citric acid 400-800 sodium bicarbonate 1000-2000 sodium carbonate 20-80 sodium benzoate 25-175 xylitol 100-300. ______________________________________

5. A formulation made by the process of combining:

space="preserve" listing-type="tabular">______________________________________ Alendronate sodium 2.5-10 (in mg alendronic acid) citric acid 400-800 sodium bicarbonate 1000-2000 sodium carbonate 20-80 sodium benzoate 25-175 xylitol 100-300. ______________________________________