IP Library Granted Patent US 10,238,672
Granted Patent B2
US 10,238,672 · App. 15/997,470 · Granted Mar 26, 2019

Dosage forms for oral administration of zoledronic acid or related compounds for treating disease

Inventor: Herriot Tabuteau (New York, NY)
Assignee: ANTECIP BIOVENTURES II LLC
A61K31/663A61K9/0019A61K9/0053A61K9/0056A61K9/2004A61K31/573A61K31/675A61K45/06
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,238,672
App. No.
15/997,470
Granted
Mar 26, 2019
Kind
B2
Abstract

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.

Claims (30)

1. A method of delivering zoledronic acid to the blood of a human being, comprising: administering an oral dosage form comprising zoledronic acid in a salt form to the human being in need of treatment with zoledronic acid, wherein the human being fasts for at least 4 hours prior to receiving the oral dosage form and the human being fasts for at least 4 hours after receiving the oral dosage form, wherein the bioavailability of zoledronic acid in the oral dosage form is about 1.4% to about 2%, and wherein a weekly oral dose of about 30 mg to about 100 mg of the zoledronic acid in the salt form is orally administered to the human being, and the zoledronic acid in the salt form is administered for a total of about 1 month to about 2 months.

2. The method of claim 1 , wherein the oral dosage form contains about 0.2 moles of the zoledronic acid in the salt form.

3. The method of claim 2 , wherein the zoledronic acid is in a disodium salt form.

4. The method of claim 1 , wherein the oral dosage form is non-toxic.

5. The method of claim 1 , wherein the oral dosage form is well tolerated.

6. The method of claim 1 , wherein the human being is required to fast to maximize the bioavailability of the zoledronic acid in the oral dosage form.

7. A method of delivering zoledronic acid to the blood of a human being, comprising: administering an oral dosage form comprising zoledronic acid in a salt form to the human being in need of treatment with zoledronic acid, wherein the human being fasts for at least 4 hours prior to receiving the oral dosage form and the human being fasts for at least 4 hours after receiving the oral dosage form, wherein the bioavailability of zoledronic acid in the oral dosage form is about 1.4% to about 2%, and wherein about 50 mg/m 2 to about 200 mg/m 2 of the zoledronic acid in the salt form is orally administered to the human being within a month of about 28 days, and the zoledronic acid in the salt form is administered for a total of about 1 month to about 2 months.

8. The method of claim 7 , wherein the oral dosage form is administered approximately weekly in about equal doses.

9. The method of claim 8 , wherein the oral dosage form contains about 0.2 moles of the zoledronic acid in the salt form.

10. The method of claim 7 , wherein the oral dosage form is administered approximately bi-weekly in about equal doses.

11. The method of claim 7 , wherein the oral dosage form contains about 0.4 moles of the zoledronic acid in the salt form.

12. The method of claim 7 , wherein the oral dosage form is administered 2 or 3 times within the month of about 28 days in about equal doses.

13. The method of claim 7 , wherein the oral dosage form is administered daily.

14. The method of claim 7 , wherein the oral dosage form is administered once during the month of about 28 days.

15. The method of claim 7 , wherein the oral dosage form is administered 5 to 10 times during the month of about 28 days in about equal doses.

16. The method of claim 7 , wherein the oral dosage form contains about 0.6 moles of the zoledronic acid in the salt form.

17. The method of claim 7 , wherein the oral dosage form contains about 50 mg to about 150 mg of the zoledronic acid in the salt form.

18. The method of claim 7 , wherein the oral dosage form contains about 30 mg to about 100 mg of the zoledronic acid in the salt form.

19. The method of claim 7 , wherein the oral dosage form contains about 100 mg to about 150 mg of the zoledronic acid in the salt form.

20. A method of delivering zoledronic acid to the blood of a human being, comprising: administering an oral dosage form comprising zoledronic acid in an acid form to the human being in need of treatment with zoledronic acid, wherein the human being fasts for at least 4 hours prior to receiving the oral dosage form and the human being fasts for at least 4 hours after receiving the oral dosage form, wherein the bioavailability of zoledronic acid in the oral dosage form is about 1.4% to about 2%, and wherein a weekly oral dose of about 30 mg to about 100 mg of the zoledronic acid in the acid form is orally administered to the human being, and the zoledronic acid in the acid form is administered for a total of about 1 month to about 2 months.

21. The method of claim 20 , wherein the oral dosage form contains about 0.2 moles of the zoledronic acid in the acid form.

22. A method of delivering zoledronic acid to the blood of a human being, comprising: administering an oral dosage form comprising zoledronic acid in an acid form to the human being in need of treatment with zoledronic acid, wherein the human being fasts for at least 4 hours prior to receiving the oral dosage form and the human being fasts for at least 4 hours after receiving the oral dosage form, wherein the bioavailability of zoledronic acid in the oral dosage form is about 1.4% to about 2%, and wherein about 50 mg/m 2 to about 200 mg/m 2 of the zoledronic acid in the acid form is orally administered to the human being within a month of about 28 days, and the zoledronic acid in the acid form is administered for a total of about 1 month to about 2 months.

23. The method of claim 22 , wherein the oral dosage form is administered approximately weekly in about equal doses.

24. The method of claim 23 , wherein the oral dosage form contains about 0.2 moles of the zoledronic acid in the acid form.

25. The method of claim 22 , wherein the oral dosage form is administered approximately bi-weekly in about equal doses.

26. The method of claim 25 , wherein the oral dosage form contains about 0.4 moles of the zoledronic acid in the acid form.

27. The method of claim 22 , wherein the oral dosage form contains about 0.6 moles of the zoledronic acid in the acid form.

28. The method of claim 22 , wherein the oral dosage form contains about 50 mg to about 150 mg of the zoledronic acid in the acid form.

29. The method of claim 22 , wherein the oral dosage form contains about 30 mg to about 100 mg of the zoledronic acid in the acid form.

30. The method of claim 22 , wherein the oral dosage form contains about 100 mg to about 150 mg of the zoledronic acid in the acid form.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 11, 2018
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 046322/0265 →
Continuity (29)
Continuation 15808794 · Nov 9, 2017
Continuation In Part 15587108 · May 4, 2017
Continuation In Part 15349926 · Nov 11, 2016
Continuation 15217752 · Jul 22, 2016
Continuation 14967224 · Dec 11, 2015
Continuation 14604524 · Jan 23, 2015
Continuation In Part 14536526 · Nov 7, 2014
Continuation In Part 14446184 · Jul 29, 2014
Division 14288716 · May 28, 2014
Continuation In Part 14279229 · May 15, 2014
Continuation 14063979 · Oct 25, 2013
Continuation In Part 13894274 · May 14, 2013
Continuation In Part PCTUS2015032739 · May 27, 2015
Continuation PCTUS2014050427 · Aug 8, 2014
Continuation 14279241 · May 15, 2014
Provisional Application 61933608 · Jan 30, 2014
Provisional Application 61803721 · Mar 20, 2013
Provisional Application 61767647 · Feb 21, 2013
Provisional Application 61767676 · Feb 21, 2013
Provisional Application 61764563 · Feb 14, 2013
Provisional Application 61762225 · Feb 7, 2013
Provisional Application 61655541 · Jun 5, 2012
Provisional Application 61655527 · Jun 5, 2012
Provisional Application 61654383 · Jun 1, 2012
Provisional Application 61654292 · Jun 1, 2012
Provisional Application 61647478 · May 15, 2012
Provisional Application 61646538 · May 14, 2012
Provisional Application 62378140 · Aug 22, 2016
Related Publication 20180280415A1 · Oct 4, 2018