Effervescent compositions comprising phosphonates and methods related thereto
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.
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.