IP Library Granted Patent US 11,654,152
Granted Patent B2
US 11,654,152 · App. 16/452,910 · Granted May 23, 2023

Compositions for oral administration of zoledronic acid or related compounds for treating disease

Inventor: Herriot Tabuteau (New York, NY)
Assignee: ANTECIP BIOVENTURES II LLC
A61K31/675A61K9/0053A61K9/20A61K9/2004A61K9/28A61K31/663A61K45/06A61K47/12C07F9/6506A61K9/0095
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Quick Facts
Patent No.
US 11,654,152
App. No.
16/452,910
Granted
May 23, 2023
Kind
B2
Abstract

Oral dosage forms of osteoclast inhibitors, such as zoledronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as arthritis.

Claims (30)

1. A method of treating arthritis comprising orally administering a zoledronic acid to a human being suffering from arthritis, wherein the zoledronic acid is in a salt form, wherein the human being is fasted for at least 2 hours prior to receiving the salt form of zoledronic acid and the human being is fasted for at least 1 hour after receiving the salt form of zoledronic acid, wherein the salt form of zoledronic acid has a bioavailability that is 1.1% to about 4%, and wherein the human being experiences pain relief as a result of receiving the zoledronic acid.

2. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.3% to 3%.

3. The method of claim 1 , wherein the human being receives about 0.18 moles of zoledronic acid with each administration of the salt form of zoledronic acid.

4. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.4% to 3%.

5. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.5% to 3%.

6. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.6% to 3%.

7. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.8% to 3%.

8. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.8% to 4%.

9. The method of claim 1 , wherein the arthritis affects a knee, an elbow, a wrist, a shoulder, or a hip.

10. The method of claim 1 , wherein each dose of the salt form of zoledronic acid is orally administered in a manner that provides an AUC 0-inf of zoledronic acid of about 100 ng·h/mL to about 200 ng·h/mL.

11. The method of claim 1 , wherein the human being is fasted in a manner that maximizes bioavailability.

12. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is about 10 to about 15.

13. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is about 12 to about 15.

14. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is at least twice that of 1 mg of zoledronic acid administered intravenously.

15. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a 48 hour sustained plasma factor that is at least twice that of 1 mg of zoledronic acid administered intravenously.

16. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is at least 1.2 times that of 4 mg of zoledronic acid administered intravenously.

17. The method of claim 1 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a 48 hour sustained plasma factor that is at least twice that of 4 mg of zoledronic acid administered intravenously.

18. A method of providing zoledronic acid to a human being comprising orally administering a salt form of zoledronic acid to a human being in need of treatment with zoledronic acid, wherein the human being is fasted for at least 2 hours prior to receiving the salt form of zoledronic acid and the human being is fasted for at least 1 hour after receiving the salt form of zoledronic acid, and wherein the salt form of zoledronic acid has a bioavailability that is 1.1% to about 4%.

19. The method of claim 18 , wherein the salt form of zoledronic acid is orally administered in a dosage form that contains at least 20% zoledronic acid in a disodium salt form by weight.

20. The method of claim 18 , wherein the salt form of zoledronic acid is orally administered in a dosage form that contains at least 30% zoledronic acid in a disodium salt form by weight.

21. The method of claim 18 , wherein the salt form of zoledronic acid is orally administered in a dosage form that contains about 50 mg to about 100 mg of zoledronic acid in a disodium salt form.

22. The method of claim 18 , wherein the salt form of zoledronic acid is orally administered in a dosage form that contains at least 40% zoledronic acid in a disodium salt form by weight.

23. The method of claim 18 , wherein the salt form of zoledronic acid is orally administered in a dosage form that contains at least 50% zoledronic acid in a disodium salt form by weight.

24. The method of claim 18 , wherein the salt form of zoledronic acid is orally administered in a dosage form that contains at least 60% zoledronic acid in a disodium salt form by weight.

25. The method of claim 18 , wherein the salt form of zoledronic acid is orally administered once weekly.

26. The method of claim 18 , wherein the salt form of the zoledronic acid has a water solubility that is about 5% to 50% by weight.

27. The method of claim 18 , wherein the salt form of zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is about 10 to about 20.

28. The method of claim 1 , wherein each dose of the salt form of zoledronic acid is orally administered in a manner that provides an AUC 0-inf of zoledronic acid of at least about 100 ng·h/mL.

29. The method of claim 1 , wherein the salt form of zoledronic acid has a bioavailability that is 1.1% to 3%.

30. The method of claim 1 , wherein the salt form of zoledronic acid has a bioavailability that is 1.1% to 2%.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 3, 2019
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 050617/0402 →