Osteoclast inhibitors such as zoledronic acid for low back pain treatment
View Patent ↗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 Modic changes type 1.
1. A method of treating a Modic change type I, comprising: orally administering zoledronic acid to a human being in need thereof, wherein about 100 mg to about 300 mg of the zoledronic acid is orally administered within a period of one month.
2. The method of claim 1 , wherein about 150 mg to about 250 mg of the zoledronic acid is orally administered within a period of one month.
3. The method of claim 1 , wherein about 50 mg to about 60 mg of the zoledronic acid in a disodium salt form is orally administered weekly.
4. The method of claim 3 , wherein the zoledronic acid is orally administered weekly for 6 weeks.
5. The method of claim 1 , wherein the zoledronic acid is orally administered weekly for one or two months.
6. The method of claim 2 , wherein about 50 mg of the zoledronic acid is orally administered weekly for 6 weeks.
7. The method of claim 1 , wherein the human being fasts for at least 1 hour before the zoledronic acid is orally administered, the human being fasts for at least 1 hour after the zoledronic acid is orally administered, and the bioavailability of zoledronic acid in the human being is 1.6% to 2.3%.
8. The method of claim 1 , wherein the Modic change type I is located at C1/2, C2/3, C3/4, C4/5, C5/6, or C6/7.
9. The method of claim 1 , wherein the Modic change type I is located at C7/T1, T1/2, T2/3, T3/4, T4/5, T5/6, T6/7, T7/8, T8/9, T9/10, T10/11, or T11/12.
10. The method of claim 1 , wherein the Modic change type I is located at T12/L1, L1/2, L2/3, L3/4, L4/5, or L5/S1.
11. The method of claim 1 , wherein the human being achieves a reduction in the size of the Modic change type I of at least about 5% relative to the baseline prior to administration of the zoledronic acid.
12. The method of claim 1 , wherein the human being has the Modic change type I at two or more levels.
13. The method of claim 2 , wherein the human being is fasted for at least 2 hours before the zoledronic acid is orally administered.
14. The method of claim 2 , wherein the human being is fasted for at least 30 minutes after the zoledronic acid is orally administered.
15. The method of claim 13 , wherein the human being is fasted for at least 1 hour after the zoledronic acid is orally administered.
16. The method of claim 15 , wherein the human being remains upright or sits upright for at least 30 minutes after the zoledronic acid is orally administered.
17. The method of claim 2 , wherein the human being is fasted for at least 4 hours before the zoledronic acid is orally administered.
18. The method of claim 1 , wherein the human being is fasted for at least 8 hours before the zoledronic acid is orally administered.
19. The method of claim 1 , wherein the size of the Modic change type I relative to the baseline prior to administration remains reduced for at least about 3 months after the zoledronic acid is orally administered.
20. The method of claim 1 , wherein the size of the Modic change type I relative to the baseline prior to administration is reduced at about 3 months after the zoledronic acid is orally administered.
21. The method of claim 1 , wherein the human being is suffering from low back pain.
22. A method of treating a Modic change type I, 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 week is about 30 mg to about 100 mg.
23. The method of claim 22 , wherein the total amount of the zoledronic acid that is orally administered to the human being within a period of one month is about 100 mg to about 500 mg.
24. The method of claim 22 , wherein the zoledronic acid is in an acid form.
25. The method of claim 22 , wherein the zoledronic acid is in a salt form.
26. The method of claim 22 , wherein the zoledronic acid is in a disodium salt form.
27. The method of claim 22 , wherein the zoledronic acid is orally administered in a dosage form that further comprises magnesium stearate.
28. The method of claim 22 , wherein the zoledronic acid is orally administered in a dosage form that further comprises microcrystalline cellulose.
29. The method of claim 22 , wherein the zoledronic acid is orally administered in a dosage form that further comprises a crosslinked polyvinylpyrrolidone.
30. The method of claim 22 , wherein the zoledronic acid is orally administered in a dosage form that further comprises fumed silica.