IP Library Granted Patent US 9,855,213
Granted Patent B2
US 9,855,213 · App. 15/599,319 · Granted Jan 2, 2018

Compositions for oral administration of zoledronic acid or related compounds for treating complex regional pain syndrome

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Quick Facts
Patent No.
US 9,855,213
App. No.
15/599,319
Granted
Jan 2, 2018
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 complex regional pain syndrome.

Claims (30)

1. A method of treating pain associated with complex regional pain syndrome comprising orally administering zoledronic acid to a human being in need thereof, wherein the amount of zoledronic acid orally administered to the human being within a period of about one month is about 200 mg to about 500 mg.

2. The method of claim 1 , wherein the zoledronic acid is in an acid form.

3. The method of claim 1 , wherein the zoledronic acid is in a salt form.

4. The method of claim 1 , wherein the zoledronic acid is orally administered in at least two consecutive doses that are at least about 1 week apart.

5. The method of claim 1 , wherein the AUC of zoledronic acid in the human being, measured over a period of one month, is about 100 ng·hr/mL to about 500 ng·hr/mL.

6. The method of claim 1 , wherein the complex regional pain syndrome was precipitated by a bone fracture.

7. The method of claim 1 , wherein the AUC of zoledronic acid in the human being, measured over a period of one month, is about 500 ng·hr/mL to about 700 ng·hr/mL.

8. The method of claim 1 , wherein the AUC of zoledronic acid in the human being, measured over a period of one month, is about 700 ng·hr/mL to about 1000 ng·hr/mL.

9. The method of claim 1 , wherein orally administering the zoledronic acid to the human being results in a C max of zoledronic acid of about 30 ng/mL to about 50 ng/mL.

10. The method of claim 1 , wherein orally administering the zoledronic acid to the human being results in a C max of zoledronic acid of about 50 ng/mL to about 80 ng/mL.

11. The method of claim 1 , wherein orally administering the zoledronic acid to the human being results in a C max of zoledronic acid of about 80 ng/mL to about 120 ng/mL.

12. The method of claim 1 , wherein orally administering the zoledronic acid to the human being results in a C max of zoledronic acid of about 120 ng/mL to about 200 ng/mL.

13. The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a bioavailability of zoledronic acid in a dosage form that is about 1.2% to about 1.5%.

14. The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a bioavailability of zoledronic acid that is about 1.5% to about 2.6%.

15. The method of claim 1 , wherein the complex regional pain syndrome is present in an area of the body that is free of other types of pain conditions.

16. The method of claim 1 , wherein, at the beginning of treatment, the human being has an average weekly pain intensity of at least 5 on the 0-10 numeric rating scale.

17. A method of treating pain associated with complex regional pain syndrome (CRPS) comprising orally administering a dosage form comprising zoledronic acid in an acid form or a salt form to a human being in need thereof, wherein the dosage form is orally administered in a manner that results in a bioavailability of zoledronic acid in the dosage form that is about 1.2% to about 3%.

18. The method of claim 17 , wherein a single oral administration of the dosage form results in an AUC for zoledronic acid of about 130 ng·hr/mL to about 160 ng·hr/mL.

19. The method of claim 17 , wherein a single oral administration of the dosage form results in an AUC for zoledronic acid of about 300 ng·hr/mL to about 350 ng·hr/mL.

20. The method of claim 17 , wherein a single oral administration of the dosage form results in an AUC for zoledronic acid of about 405 ng·hr/mL to about 450 ng·hr/mL.

21. The method of claim 17 , wherein orally administering zoledronic acid in the acid form or the salt form to the human being results in a C max of zoledronic acid of at least about 30 ng/mL.

22. The method of claim 17 , wherein orally administering zoledronic acid in the acid form or the salt form to the human being results in a C max of zoledronic acid of about 30 ng/mL to about 50 ng/mL.

23. The method of claim 17 , wherein orally administering zoledronic acid in the acid form or the salt form to the human being results in a C max of zoledronic acid of about 50 ng/mL to about 150 ng/mL.

24. The method of claim 17 , wherein orally administering zoledronic acid in the acid form or the salt form to the human being results in a C max of zoledronic acid of about 50 ng/mL to about 80 ng/mL.

25. The method of claim 17 , wherein orally administering zoledronic acid in the acid form or the salt form to the human being results in a C max of zoledronic acid of about 80 ng/mL to about 120 ng/mL.

26. The method of claim 17 , wherein orally administering zoledronic acid in the acid form or the salt form to the human being results in a C max of zoledronic acid of about 120 ng/mL to about 200 ng/mL.

27. The method of claim 17 , wherein the complex regional pain syndrome was precipitated by a bone fracture.

28. The method of claim 17 , wherein the complex regional pain syndrome is present in an area of the body that is free of other types of pain conditions.

29. The method of claim 17 , wherein the CRPS is CRPS Type I.

30. The method of claim 17 , wherein, at the beginning of treatment, the human being has an average weekly pain intensity of at least 5 on the 0-10 numeric rating scale.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 10, 2018
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 045034/0542 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 8, 2017
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 044777/0488 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 27, 2017
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 043719/0465 →