Compositions for oral administration of zoledronic acid or related compounds for treating low back pain

Patent metadata

Field	Value
Publication number	US-9408860-B2
Application number	US-201514686551-A
Country	US
Kind code	B2
Filing date	Apr 14, 2015
Priority date	May 14, 2012
Publication date	Aug 9, 2016
Grant date	Aug 9, 2016

Abstract

Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions. The oral bioavailability of zoledronic acid can be enhanced by administering the zoledronic acid in the disodium salt form.

First claim

The invention claimed is:

1. A method of safely treating low back pain by an oral route comprising orally administering a safe and effective amount of zoledronic acid to a human being suffering from low back pain, wherein the human being receives about 80 mg to about 600 mg of the zoledronic acid within a period of two months, wherein the zoledronic acid is orally administered as 3 to 9 divided doses that are administered no more often than once a week, and wherein the human being experiences pain relief that lasts for a duration of at least 48 hours.

2. The method of claim 1 , wherein the human being receives about 80 mg to about 300 mg of the zoledronic acid in a period of one month or less.

3. The method of claim 1 , wherein the human being to which the zoledronic acid is administered does not eat food or drink beverage for at least 30 minutes after the zoledronic acid is orally administered.

4. The method of claim 2 , wherein the human being to which the zoledronic acid is administered does not eat food or drink beverage for at least 30 minutes after the zoledronic acid is orally administered.

5. The method of claim 1 , wherein the human being to which the zoledronic acid is administered does not eat food or drink beverage for at least 1 hour before the zoledronic acid is orally administered.

6. The method of claim 5 , wherein the zoledronic acid is administered in an oral dosage form that is at least 10% zoledronic acid by weight.

7. The method of claim 1 , wherein the zoledronic acid is orally administered for 1 to 2 months.

8. The method of claim 1 , wherein the zoledronic acid is orally administered weekly.

9. The method of claim 5 , wherein the zoledronic acid is orally administered weekly for 1 to 2 months.

10. The method of claim 9 , wherein about 10 mg to about 100mg of the zoledronic acid is orally administered weekly.

11. The method of claim 10 , wherein the zoledronic acid is administered in an oral dosage form that is at least 10% zoledronic acid by weight.

12. The method of claim 9 , wherein about 40 mg to about 50 mg of the zoledronic acid is orally administered weekly.

13. The method of claim 12 , wherein the zoledronic acid is administered in an oral dosage form that is at least 10% zoledronic acid by weight.

14. The method of claim 9 , wherein about 50 mg of the zoledronic acid is orally administered weekly.

15. The method of claim 14 , wherein the zoledronic acid is administered in an oral dosage form that is at least 10% zoledronic acid by weight.

16. The method of claim 9 , wherein about 50 mg to about 100 mg of the zoledronic acid is orally administered weekly.

17. The method of claim 16 , wherein the zoledronic acid is administered in an oral dosage form that is at least 10% zoledronic acid by weight.

18. The method of claim 1 , wherein the zoledronic acid is orally administered weekly for 1 to 2 months.

19. The method of claim 1 , wherein about 50 mg of the zoledronic acid is administered weekly for six consecutive weeks.

20. The method of claim 1 , wherein the zoledronic acid is orally administered as 3 to 6 divided doses.

21. The method of claim 1 , wherein the zoledronic acid is orally administered as 4 to 9 divided doses.

22. The method of claim 1 , wherein the zoledronic acid is administered in a solid dosage form having a hardness of about 5 kPa to about 20 kPa.

23. The method of claim 1 , wherein the human being remains upright or sits upright for at least 30 minutes after the zoledronic acid is orally administered.

24. The method of claim 1 , wherein the human being remains upright or sits upright for at least 1 hour after the zoledronic acid is orally administered.

25. The method of claim 1 , wherein the human being is fasted for at least 2 hours before the zoledronic acid is orally administered.

26. The method of claim 1 , wherein the human being is fasted for at least 4 hours before the zoledronic acid is orally administered.

27. The method of claim 1 , wherein the human being is fasted for at least 6 hours before the zoledronic acid is orally administered.

28. The method of claim 1 , wherein the human being is fasted for at least 8 hours before the zoledronic acid is orally administered.

29. The method of claim 1 , wherein the human being is fasted for at least 10 hours before the zoledronic acid is orally administered.

30. The method of claim 1 , wherein the human being is fasted for at least 12 hours before the zoledronic acid is orally administered.

Assignees

• Antecip Bioventures Ii Llc

Inventors

• Tabuteau Herriot

Classifications

• A61K9/2013

  Organic compounds, e.g. phospholipids, fats · CPC title

• A61K9/2009

  Inorganic compounds · CPC title

• A61K9/2027

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates · CPC title

• A61K9/2054

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title