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 delivering zoledronic acid to the blood, comprising: orally administering a dosage form comprising zoledronic acid in 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 wherein 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 in the salt form; 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 a monthly dose of about 100 mg to about 600 mg of the zoledronic acid in the salt form is orally administered to the human being.
6 . The method of claim 5 , 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.
7 . The method of claim 1 , wherein the dosage form contains at least about 20% of the zoledronic acid in the salt form by weight.
8 . The method of claim 1 , wherein the zoledronic acid in the salt form has an aqueous solubility of about 10% (w/v) to about 15% (w/v).
9 . The method of claim 1 , wherein the dosage form further contains a binder, an excipient, a disintegrating agent, a lubricant, or a flavoring agent.
10 . 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%.
11 . The method of claim 10 , with the proviso that the bioavailability of zoledronic acid resulting from orally administering the dosage form is no more than 3%.
12 . The method of claim 10 , wherein the dosage form contains about 50 mg to about 150 mg of the zoledronic acid in the salt form.
13 . The method of claim 10 , 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.
14 . The method of claim 10 , wherein the pain comprises arthritis pain.
15 . The method of claim 10 , wherein the pain comprises inflammatory pain.
16 . A method of delivering zoledronic acid to the blood, comprising: orally administering a dosage form comprising zoledronic acid, in 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 wherein 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 as a property of the salt form, as measured in a reference dosage form, is no more than 4%, wherein the reference dosage form contains the zoledronic acid in the salt form and does not contain a bioavailability enhancer;
with the proviso that the dosage form contains no less than 40 mg of the zoledronic acid in the salt form; and
with the proviso that the bioavailability of zoledronic acid as a property of the salt form, as measured in the reference dosage form, is at least 1.1%.
17 . The method of claim 16 , with the proviso that the bioavailability of zoledronic acid, as measured in the reference dosage form that does not enhance bioavailability, is no more than 3%.
18 . The method of claim 16 , wherein the dosage form contains about 50 mg to about 150 mg of the zoledronic acid in the salt form.
19 . The method of claim 16 , 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.
20 . The method of claim 16 , wherein the dosage form contains at least about 20% of the zoledronic acid in the salt form by weight.
21 . The method of claim 16 , wherein the zoledronic acid in the salt form has an aqueous solubility of about 10% (w/v) to about 15% (w/v).
22 . The method of claim 16 , wherein the dosage form further contains a binder, an excipient, a disintegrating agent, a lubricant, or a flavoring agent.