Dosage forms for oral administration of zoledronic acid or related compounds for treating disease
View Patent ↗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.
1. A method of delivering zoledronic acid in the disodium salt form to the blood of a human being comprising: orally administering about 10 mg to about 300 mg of zoledronic acid in the disodium salt form to a human being in need of treatment with zoledronic acid; wherein the human being is instructed not to eat or drink for at least 1 hour before and at least 30 minutes after the zoledronic acid in the disodium salt form is administered, wherein the zoledronic acid in the disodium salt form is administered in a manner that results in an oral bioavailability of zoledronic acid in the human being of 1% to about 4%.
2. The method of claim 1 , wherein the zoledronic acid in the disodium salt form is administered in a manner that results in an oral bioavailability of zoledronic acid in the human being of 1.5% to about 3%.
3. The method of claim 1 , wherein the zoledronic acid in the disodium salt form is orally administered in a dosage form that contains at least 10% w/w zoledronic acid in the disodium salt form.
4. The method of claim 1 , wherein about 30 mg to about 150 mg of zoledronic acid in the disodium salt form is administered.
5. The method of claim 1 , wherein zoledronic acid in the disodium salt form is orally administered only once, or there is a period of about 24 hours to about 2 years between instances of oral administration of zoledronic acid in the disodium salt form.
6. The method of claim 1 , wherein there is a period of about 24 hours to about 7 days between instances of oral administration of zoledronic acid in the disodium salt form.
7. The method of claim 1 , wherein there is a period of about 7 days to about 14 days between instances of oral administration of zoledronic acid in the disodium salt form.
8. The method of claim 1 , wherein there is a period of about 14 days to about 28 days between instances of oral administration of zoledronic acid in the disodium salt form.
9. The method of claim 1 , wherein there is a period of at least one month between instances of oral administration of zoledronic acid in the disodium salt form.
10. The method of claim 1 , wherein zoledronic acid in the disodium salt form is orally administered only once.
11. The method of claim 1 , wherein zoledronic acid in the disodium salt form is administered once a month for only 3 months.
12. The method of claim 1 , wherein the zoledronic acid in the disodium salt form is administered in a manner that results in an oral bioavailability of zoledronic acid in the human being of 1.2% to about 3%.
13. The method of claim 1 , wherein about 25 mg to about 150 mg of zoledronic acid in the disodium salt form is orally administered.
14. The method of claim 1 , wherein about 200 mg to about 300 mg of zoledronic acid in the disodium salt form is orally administered.
15. The method of claim 1 , wherein the zoledronic acid in the disodium salt form is administered in a manner that results in an oral bioavailability of zoledronic acid in the human being of about 1.5% to about 2%.
16. The method of claim 1 , wherein the zoledronic acid in the disodium salt form is administered in a manner that results in an oral bioavailability of zoledronic acid in the human being of about 2% to about 3%.
17. The method of claim 1 , wherein the zoledronic acid in the disodium salt form is orally administered in a solid dosage form.
18. The method of claim 1 , wherein the zoledronic acid in the disodium salt form is orally administered in a solid dosage form that has a hardness of at least about 5 kPa.
19. The method of claim 1 , wherein the zoledronic acid in the disodium salt form is orally administered in a solid dosage form that contains about 50% w/w to about 90% w/w of zoledronic acid in the disodium salt form.
20. The method of claim 1 , wherein the zoledronic acid in the disodium salt form is administered in a manner that results in the zoledronic acid having a 24 hour sustained plasma factor of at least about 3.
21. The method of claim 1 , wherein the human being remains upright for at least one hour after oral administration of the zoledronic acid in the disodium salt form.
22. The method of claim 12 , wherein about 30 mg to about 150 mg of zoledronic acid in the disodium salt form is administered.
23. The method of claim 1 , wherein about 30 mg to about 100 mg of zoledronic acid in the disodium salt form is administered.
24. The method of claim 1 , wherein about 100 mg to about 300 mg of zoledronic acid in the disodium salt form is administered.
25. The method of claim 1 , wherein about 200 mg to about 300 mg of zoledronic acid in the disodium salt form is administered.