COMPOSITIONS FOR ORAL ADMINISTRATION OF ZOLEDRONIC ACID OR RELATED COMPOUNDS FOR TREATING DISEASE
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 arthritis.
1 . A method of treating arthritis comprising orally administering a zoledronic acid to a human being suffering from arthritis, wherein the zoledronic acid is in an acid form or a salt form, wherein the human being is fasted for at least 2 hours prior to receiving the zoledronic acid and the human being is fasted for at least 1 hour after receiving the zoledronic acid, wherein the zoledronic acid has a bioavailability that is 1.1% to about 4%, and wherein the human being experiences pain relief as a result of receiving the zoledronic acid.
2 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.3% to 3%.
3 . The method of claim 1 , wherein the human being receives about 0.18 moles of zoledronic acid with each administration of the zoledronic acid.
4 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.4% to 3%.
5 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.5% to 3%.
6 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.6% to 3%.
7 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.8% to 3%.
8 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.8% to 4%.
9 . The method of claim 1 , wherein the arthritis affects a knee, an elbow, a wrist, a shoulder, or a hip.
10 . The method of claim 1 , wherein each dose of the zoledronic acid is orally administered in a manner that provides an AUC 0-inf of zoledronic acid of about 100 ng·h/mL to about 200 ng·h/mL.
11 . The method of claim 1 , wherein the human being is fasted in a manner that maximizes bioavailability.
12 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is about 10 to about 15.
13 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is about 12 to about 15.
14 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is at least twice that of 1 mg of zoledronic acid administered intravenously.
15 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a 48 hour sustained plasma factor that is at least twice that of 1 mg of zoledronic acid administered intravenously.
16 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is at least 1.2 times that of 4 mg of zoledronic acid administered intravenously.
17 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a 48 hour sustained plasma factor that is at least twice that of 4 mg of zoledronic acid administered intravenously.
18 . A method of providing zoledronic acid to a human being comprising orally administering a zoledronic acid to a human being in need of treatment with zoledronic acid, wherein the zoledronic acid is in a salt form, wherein the human being is fasted for at least 2 hours prior to receiving the zoledronic acid and the human being is fasted for at least 1 hour after receiving the zoledronic acid, and wherein the zoledronic acid has a bioavailability that is 1.1% to about 4%.
19 . The method of claim 18 , wherein the zoledronic acid is orally administered in a dosage form that contains at least 20% zoledronic acid in a disodium salt form by weight.
20 . The method of claim 18 , wherein the zoledronic acid is orally administered in a dosage form that contains at least 30% zoledronic acid in a disodium salt form by weight.
21 . The method of claim 18 , wherein the zoledronic acid is orally administered in a dosage form that contains about 50 mg to about 100 mg of zoledronic acid in a disodium salt form.
22 . The method of claim 18 , wherein the zoledronic acid is orally administered in a dosage form that contains at least 40% zoledronic acid in a disodium salt form by weight.
23 . The method of claim 18 , wherein the zoledronic acid is orally administered in a dosage form that contains at least 50% zoledronic acid in a disodium salt form by weight.
24 . The method of claim 18 , wherein the zoledronic acid is orally administered in a dosage form that contains at least 60% zoledronic acid in a disodium salt form by weight.
25 . The method of claim 18 , wherein the zoledronic acid is orally administered once weekly.
26 . The method of claim 18 , wherein the salt form of the zoledronic acid has a water solubility that is about 5% to 50% by weight.
27 . The method of claim 18 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma factor that is about 10 to about 20.
28 . The method of claim 1 , wherein each dose of the zoledronic acid is orally administered in a manner that provides an AUC 0-inf of zoledronic acid of at least about 100 ng·h/mL.
29 . The method of claim 1 , wherein the zoledronic acid has a bioavailability that is 1.1% to 3%.
30 . The method of claim 1 , wherein the zoledronic acid has a bioavailability that is 1.1% to 2%.