Effervescent compositions comprising bisphosphonates and methods related thereto

• US 7,488,496 B2
• Filed: 10/17/2002
• Issued: 02/10/2009
• Est. Priority Date: 03/06/2002
• Status: Expired due to Term

• Current Assignee: EffRx Pharmaceuticals SA
• Original Assignee: EFFRX, Inc. (EffRx Pharmaceuticals SA)
• Inventors: Rosen, Christer
• Primary Examiner(s): HUI, SAN MING R
• Application Number:
  US10/273,081
• Publication Number:
  US 20030175340A1
• Time in Patent Office: 2,308 Days
• Field of Search: 424/466, 524/103, 524/166, 514/108, 514/114, 514/103, 514/166
• US Class Current: 424/466
• 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 31/341 not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
• CPC Class Codes: A61K 31/4164 1,3-Diazoles
• CPC Class Codes: A61K 31/426 1,3-Thiazoles
• CPC Class Codes: A61K 31/4439 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole nicotine A61K31/465
• CPC Class Codes: A61K 31/66 Phosphorus compounds
• 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 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0007 Effervescent A61K9/0065 takes precedence
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61P 19/10 for osteoporosis

Abstract

The invention provides effervescent composition comprising a bisphosphonate, an acidic compound, an alkaline effervescing component, and optionally an anti-ulcer agent and methods of treating osteoporosis in a mammal using the effervescent compositions.

Claims

1. An effervescent composition comprising:

(a) 50 mg to 120 mg alendronate

(b) citric acid, and

(c) an alkaline effervescing component which is a carbonate salt or a bicarbonate salt, wherein the composition has a total weight of 3500 mg to about 6000 mg and when dissolved in water produces a solution having a buffered pH of about 4 to about 6.5 and has buffering capacity sufficient to mediate the pH of a patient'"'"'s stomach for at least 15 minutes.

2. The composition of claim 1, wherein the alkaline effervescing component comprises a carbonate salt and a bicarbonate salt.

3. The composition of claim 1, wherein the acid component and the alkaline effervescing component are at least partially reacted with each other during granulation with the bisphosphonate.

4. The composition of claim 1, further comprising a sweetener or flavorant.

5. The composition of claim 1, further comprising a solubilizing agent.

6. The composition of claim 5, wherein the solubilizing agent is selected from the group consisting of polyvinylpyrrolidones, polyethylene glycols, dextrans, and combinations thereof.