Compositions for administration of zoledronic acid or related compounds for treating low back pain
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 chronic low back pain.
1. A method of treating chronic low back pain 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 bioavailability of zoledronic acid in the dosage form is about 1.8% to about 2.5%, as determined when orally administered to a human being who has fasted for eight hours.
2. The method of claim 1 , wherein the bioavailability of zoledronic acid in the dosage form is about 1.8% to 2.3%, as determined when orally administered to a human being who has fasted for eight hours.
3. The method of claim 1 , wherein a single oral administration of the dosage form to the human being results in an AUC for zoledronic acid of about 130 ng·hr/mL to about 160 ng·hr/mL.
4. The method of claim 1 , wherein the dosage form is orally administered three times within a period of six months.
5. The method of claim 1 , wherein the dosage form is orally administered six times within a period of six months.
6. The method of claim 1 , wherein, at the beginning of treatment, the human being has an average weekly pain intensity of at least 4 on the 0-10 numeric rating scale.
7. The method of claim 1 , wherein the human being has suffered from low back pain for at least 3 months.
8. The method of claim 1 , wherein a single oral administration of the dosage form to the human being results in an AUC for zoledronic acid of about 300 ng·hr/mL to about 350 ng·hr/mL.
9. The method of claim 1 , wherein a single oral administration of the dosage form to the human being results in an AUC for zoledronic acid of about 405 ng·hr/mL to about 450 ng·hr/mL.
10. The method of claim 1 , wherein orally administering the dosage form to the human being results in a C max of zoledronic acid of about 30 ng/mL to about 50 ng/mL.
11. The method of claim 1 , wherein orally administering the dosage form to the human being results in a C max of zoledronic acid of about 50 ng/mL to about 80 ng/mL.
12. The method of claim 1 , wherein orally administering the dosage form to the human being results in a C max of zoledronic acid of about 80 ng/mL to about 120 ng/mL.
13. The method of claim 1 , wherein an amount of a non-steroidal anti-inflammatory drug that is administered to the human being is reduced after the dosage form is orally administered.
14. The method of claim 1 , wherein the low back pain is associated with a type 1 Modic change.
15. The method of claim 1 , wherein the low back pain is associated with a type 2 Modic change.
16. A method of treating chronic low back pain 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 300 mg.
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 16 , wherein the zoledronic acid is in a disodium salt 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 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.
24. The method of claim 16 , 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.
25. The method of claim 16 , wherein the human being has suffered from low back pain for at least 2 months.
26. The method of claim 16 , wherein, at the beginning of treatment, the human being has an average weekly pain intensity of at least 4 on the 0-10 numeric rating scale.
27. 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.
28. The method of claim 16 , wherein the low back pain is associated with a Modic change.
29. The method of claim 16 , wherein the low back pain is associated with a type 1 Modic change.
30. The method of claim 16 , wherein the low back pain is associated with a type 2 Modic change.