Methods for the safe administration of imidazole or imidazolium compounds

Patent metadata

Field	Value
Publication number	US-2016331679-A1
Application number	US-201615223487-A
Country	US
Kind code	A1
Filing date	Jul 29, 2016
Priority date	May 14, 2012
Publication date	Nov 17, 2016
Grant date	—

Abstract

Methods for the safe administration of imidazole or imidazolium compounds, and conditions that may be treated by these methods, are described herein.

First claim

What is claimed is:

1 . A method of safely and effectively delivering zoledronic acid to the blood of a human being through repeated oral administration comprising:
mixing zoledronic acid with a diluent, binder, an excipient, a disintegrating agent, a flavoring agent, or a lubricant to form a pharmaceutical composition containing at least 20% zoledronic acid by weight; wherein the pharmaceutical composition is in the form of a pill, tablet, or capsule, and containing about 0.15 millimoles to about 1.1 millimoles of zoledronic acid in the acid or a salt form; and wherein the pill, tablet, or capsule is orally administered to a human being at least twice a month and no more frequently than once a day.

2 . The method of claim 1 , wherein, about 0.15 millimoles to about 0.22 millimoles of zoledronic acid is orally administered weekly.

3 . The method of claim 2 , wherein the pill, tablet, or capsule containing zoledronic acid is orally administered for about 6 weeks.

4 . The method of claim 1 , wherein the pill, tablet, or capsule comprises more than about 30% zoledronic acid by weight.

5 . The method of claim 2 , wherein the pill, tablet, or capsule comprises more than about 30% zoledronic acid by weight.

6 . The method of claim 3 , wherein the pill, tablet, or capsule comprises more than about 30% zoledronic acid by weight.

7 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma level factor that is at least 1.5 times that of 4 mg of zoledronic acid administered intravenously.

8 . The method of claim 2 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma level factor that is at least 1.5 times that of 4 mg of zoledronic acid administered intravenously.

9 . The method of claim 3 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma level factor that is at least 1.5 times that of 4 mg of zoledronic acid administered intravenously.

10 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma level factor that is at least twice that of 4 mg of zoledronic acid administered intravenously.

11 . The method of claim 2 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma level factor that is at least twice that of 4 mg of zoledronic acid administered intravenously.

12 . The method of claim 3 , wherein the zoledronic acid is orally administered in a manner that results in a 24 hour sustained plasma level factor that is at least twice that of 4 mg of zoledronic acid administered intravenously.

13 . The method of claim 1 , wherein the zoledronic acid is orally administered in a manner that results in a 48 hour sustained plasma level factor that is at least twice that of 4 mg of zoledronic acid administered intravenously.

14 . The method of claim 2 , wherein the zoledronic acid is orally administered in a manner that results in a 48 hour sustained plasma level factor that is at least twice that of 4 mg of zoledronic acid administered intravenously.

15 . The method of claim 3 , wherein the zoledronic acid is orally administered in a manner that results in a 48 hour sustained plasma level factor that is at least twice that of 4 mg of zoledronic acid administered intravenously.

16 . The method of claim 1 , wherein zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.3% to 4%.

17 . The method of claim 2 , wherein zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.3% to 4%.

18 . The method of claim 3 , wherein zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.3% to 4%.

19 . The method of claim 1 , wherein zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.8% to 3%.

20 . The method of claim 2 , wherein zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.8% to 3%.

21 . The method of claim 3 , wherein zoledronic acid is orally administered in a manner that results in a bioavailability that is 1.8% to 3%.

22 . The method of claim 1 , wherein the zoledronic acid is orally administered in a dosage form that, other than a counter-ion to zoledronic acid, contains no agents which enhance the bioavailability of zoledronic acid.

23 . The method of claim 2 , wherein the zoledronic acid is orally administered in a dosage form that, other than a counter-ion to zoledronic acid, contains no agents which enhance the bioavailability of zoledronic acid.

24 . The method of claim 3 , wherein the zoledronic acid is orally administered in a dosage form that, other than a counter-ion to zoledronic acid, contains no agents which enhance the bioavailability of zoledronic acid.

25 . The method of claim 1 , wherein the human being is not suffering from a blood cancer.

26 . The method of claim 2 , wherein the human being is not suffering from a blood cancer.

27 . The method of claim 3 , wherein the human being is not suffering from a blood cancer.

28 . The method of claim 1 , wherein the zoledronic acid is orally administered in a solid dosage form having a binder.

29 . The method of claim 2 , wherein the zoledronic acid is orally administered in a solid dosage form having a binder.

30 . The method of claim 3 , wherein the zoledronic acid is orally administered in a solid dosage form having a binder.

Assignees

• Antecip Bioventures Ii Llc

Inventors

• Tabuteu Herriot

Classifications

• C07F9/58

  Pyridine rings · CPC title

• C07F9/6506

  having the nitrogen atoms in positions 1 and 3 · CPC title

• C07D233/60

  with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms · CPC title

• C07F9/3873

  containing nitrogen substituent, e.g. N.....H or N-hydrocarbon group which can be substituted by halogen or nitro(so), N.....O, N.....S, N.....C(=X)- (X =O, S), N.....N, N...C(=X)...N (X =O, S) · CPC title

• A61K9/2004

  Excipients; Inactive ingredients · CPC title