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Generated: August 21, 2017

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Title:Effervescent compositions comprising phosphonates and methods related thereto
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.
Inventor(s): Rosen; Christer (Epalinges, CH)
Assignee: EffRx Pharmaceuticals, S.A. (CH)
Filing Date:May 02, 2011
Application Number:13/099,226
Claims:1. An effervescent composition comprising: (a) 50 mg to 120 mg of a bisphosphonate (b) an acid component, 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 bisphosphonate is selected from the group consisting of etidronate, risedronate, ibandronate, alendronate, and combinations thereof.

3. The composition of claim 1, wherein the bisphosphonate is etidronate.

4. The composition of claim 1, wherein the bisphosphonate is alendronate.

5. The composition of claim 1, wherein the bisphosphonate is ibandronate.

6. The composition of claim 1, wherein the bisphosphonate is residronate.

7. The composition of claim 1, wherein the dissolved buffered solution is capable of mediating the pH of a patient's stomach for at least about 30 minutes or more.

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

9. 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.

10. A method for treating osteoporosis, comprising: administering to a patient in need thereof an effervescent composition comprising: (a) 50 mg to 120 mg of a bisphosphonate (b) acid component, 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.

11. The method of claim 10, wherein the bisphosphonate is selected from the group consisting of etidronate, risedronate, ibandronate and alendronate.

12. The method of claim 10, wherein the bisphosphonate is etidronate.

13. The method of claim 10, wherein the bisphosphonate is alendronate.

14. The method of claim 10, wherein the bisphosphonate is ibandronate.

15. The method of claim 10, wherein the bisphosphonate is residronate.

16. The method of claim 10, wherein the dissolved buffered solution is capable of mediating the pH of a patient's stomach for at least about 30 minutes or more.

17. The method of claim 10, wherein the alkaline effervescing component comprises a carbonate salt and a bicarbonate salt.
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