IP Library Granted Patent US 9,999,629
Granted Patent B2
US 9,999,629 · App. 15/801,049 · Granted Jun 19, 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 9,999,629
App. No.
15/801,049
Granted
Jun 19, 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 (34)

1. A method of safely and effectively treating complex regional pain syndrome by delivering zoledronic acid to the blood through repeated oral administration comprising: orally administering an oral dosage form to a human being suffering from complex regional pain syndrome at an interval of about 1 to 21 days;

wherein the oral dosage form is prepared by a method comprising:

mixing zoledronic acid with a diluent, binder, disintegrating agent, or lubricant to form a pharmaceutical composition; and

forming the pharmaceutical composition into the oral dosage form, wherein the oral dosage form contains at least 10% zoledronic acid by weight in a salt form or acid form;

wherein the amount of zoledronic acid, in the acid form or the salt form, in a single dose is about 100 mg to about 300 mg.

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

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

4. The method of claim 1 , wherein the complex regional pain syndrome is associated with an inciting event.

5. The method of claim 4 , wherein the inciting event is a bone fracture.

6. The method of claim 1 , wherein an area under the plasma concentration curve (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.

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 1000 ng·hr/mL.

8. The method of claim 1 , wherein the single dose of the zoledronic acid results in an AUC for zoledronic acid of about 130 ng·hr/mL to about 160 ng·hr/mL.

9. The method of claim 1 , wherein the single dose of the zoledronic acid results in an AUC for zoledronic acid of about 300 ng·hr/mL to about 350 ng·hr/mL.

10. The method of claim 1 , wherein the single dose of the zoledronic acid results in an AUC for zoledronic acid of about 405 ng·hr/mL to about 450 ng·hr/mL.

11. The method of claim 1 , wherein the zoledronic acid is administered at an interval of 13 to 16 days.

12. The method of claim 11 , wherein the zoledronic acid is administered 3 times.

13. The method of claim 12 , wherein the complex regional pain syndrome is associated with an inciting event, and the inciting event is a bone fracture.

14. The method of claim 13 , 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.

15. The method of claim 9 , wherein the complex regional pain syndrome is associated with an inciting event, and the inciting event is a bone fracture, and 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.

16. A method of safely and effectively treating complex regional pain syndrome by delivering zoledronic acid to the blood through repeated oral administration comprising: mixing zoledronic acid with a diluent, binder, disintegrating agent, or lubricant to form a pharmaceutical composition; and forming the pharmaceutical composition into a pill, tablet, or capsule containing at least 10% zoledronic acid by weight; wherein the amount of zoledronic acid in a single dose is about 100 mg to about 200 mg; and wherein the pill, tablet, or capsule is orally administered to a human being suffering from complex regional pain syndrome at an interval of 5 to 30 days.

17. The method of claim 16 , wherein the zoledronic acid is in an acid form.

18. The method of claim 16 , wherein the zoledronic acid is in a salt form.

19. The method of claim 18 , wherein the imidazole ring of zoledronic acid is in an imidazolium form.

20. The method of claim 16 , wherein the zoledronic acid is orally administered in at least two consecutive doses that are at least about 1 week apart.

21. The method of claim 16 , 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.

22. The method of claim 16 , 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 1000 ng·hr/mL.

23. The method of claim 16 , wherein the single dose of the zoledronic acid results in an AUC for zoledronic acid of about 130 ng·hr/mL to about 160 ng·hr/mL.

24. The method of claim 16 , wherein the single dose of the zoledronic acid results in an AUC for zoledronic acid of about 300 ng·hr/mL to about 350 ng·hr/mL.

25. The method of claim 16 , wherein the single dose of the zoledronic acid results in an AUC for zoledronic acid of about 405 ng·hr/mL to about 450 ng·hr/mL.

26. The method of claim 16 , wherein the zoledronic acid is orally administered in a dosage form that further comprises magnesium stearate.

27. The method of claim 16 , wherein the complex regional pain syndrome is associated with an inciting event, and the inciting event is a bone fracture.

28. The method of claim 16 , 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.

29. The method of claim 16 , wherein the zoledronic acid is orally administered three times within a period of six months.

30. The method of claim 29 , wherein the zoledronic acid is orally administered at an interval of about 2 weeks.

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 Nov 9, 2017
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 044086/0206 →