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.
1 . A method of treating pain not related to cancer, comprising: orally administering a dosage form comprising zoledronic acid, in an acid form or a salt form, to a human being in need of treatment with zoledronic acid, wherein the human being has fasted for at least one hour before the dosage form is orally administered and the human being fasts for at least one hour after the dosage form is orally administered; with the proviso that the bioavailability of zoledronic acid resulting from orally administering the dosage form is no more than 4%; wherein the dosage form contains no less than 40 mg of the zoledronic acid; and with the proviso that the bioavailability of zoledronic acid resulting from orally administering the dosage form is at least 1.1%.
2 . The method of claim 1 , with the proviso that the bioavailability of zoledronic acid resulting from orally administering the dosage form is no more than 3%.
3 . The method of claim 1 , wherein the dosage form contains about 50 mg to about 150 mg of the zoledronic acid in the salt form.
4 . The method of claim 1 , wherein the dosage form contains an amount of the zoledronic acid in the salt form that is about 50 mg, about 100 mg, or any amount between these values.
5 . The method of claim 1 , wherein the pain comprises arthritis pain.
6 . The method of claim 1 , wherein the pain comprises inflammatory pain.
7 . The method of claim 1 , wherein the dosage form further contains a binder, an excipient, a disintegrating agent, a lubricant, or a flavoring agent.
8 . The method of claim 7 , wherein the binder is gum tragacanth.
9 . The method of claim 7 , wherein the excipient is dicalcium phosphate.
10 . The method of claim 7 , wherein the disintegrating agent is corn starch.
11 . The method of claim 7 , wherein the lubricant is magnesium stearate.
12 . The method of claim 7 , wherein the flavoring agent is peppermint.
13 . The method of claim 1 , wherein the dosage form comprises a silicified microcrystalline cellulose.
14 . The method of claim 13 , wherein the silicified microcrystalline cellulose is about 40% (wt/wt) to about 50% (wt/wt) of the dosage form.
15 . The method of claim 1 , wherein the dosage form comprises a crosslinked polyvinylpyrrolidone.
16 . The method of claim 15 , wherein the crosslinked polyvinylpyrrolidone is about 1% (wt/wt) to about 5% (wt/wt) of the dosage form.
17 . The method of claim 1 , wherein the dosage form comprises a fumed silica.
18 . The method of claim 17 , wherein the fumed silica is about 0.1% (wt/wt) to about 1% (wt/wt) of the dosage form.
19 . The method of claim 11 , wherein the magnesium stearate is about 0.1% (wt/wt) to about 1% (wt/wt) of the dosage form.
20 . The method of claim 1 , wherein the dosage form does not contain a bioavailability-enhancing agent.