IP Library › Granted Patent US 10,881,626
Granted Patent B2
US 10,881,626 · App. 15/583,697 · Granted Jan 5, 2021

Controlled release oral pharmaceutical dosage forms comprising MGBG

Inventors: John McKearn (Saint Louis, MO); Jeremy Blitzer (San Francisco, CA)
Assignee: Pathologica LLC
A61K31/155A61K9/2054A61K9/2846A61K9/4808A61K9/4866A61K9/4891A61K9/5026A61K9/5047C07C211/13C07C243/16C07C251/12C07C251/78
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Quick Facts
Patent No.
US 10,881,626
App. No.
15/583,697
Granted
Jan 5, 2021
Kind
B2
Abstract

Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.

Claims (12)

1. A method of treating inflammation or an inflammatory condition, comprising the administration, to a patient in need thereof, a delayed-release oral pharmaceutical dosage form comprising methylglyoxal bis(guanylhydrazone) (MGBG) and an enteric coating.

2. The method as recited in claim 1 , wherein said delayed release oral pharmaceutical dosage form is an enterically-coated capsule comprising about 25 to about 350 mg MGBG.

3. The method as recited in claim 2 , wherein the administration of the enterically-coated capsule comprising MGBG results in a reduction of one or more gastrointestinal side effects when compared to a reference standard that is not enterically coated.

4. The method as recited in claim 3 , wherein said one or more gastrointestinal side effects is chosen from nausea, emesis, diarrhea, abdominal pain, oral mucositis, oral ulceration, pharyngitis, stomatitis, irritation of the gastric mucosa, and gastrointestinal ulceration.

5. The method as recited in claim 4 , wherein said gastrointestinal side effect is emesis.

6. The method as recited in claim 3 , wherein MGBG is administered at a dosage level which would result in dose-limiting side effects if administered as a non-enteric coated dosage form.

7. The method as recited in claim 1 , wherein the enteric coating begins to substantially dissolve, and drug release commences, in the duodenum.

8. The method as recited in claim 1 , wherein the enteric coating begins to substantially dissolve and drug release commences at about ½ or more hours after ingestion.

9. The method as recited in claim 1 , wherein the enteric coating begins to substantially dissolve and drug release commences at about 1 or more hours after ingestion.

10. The method as recited in claim 1 , wherein the enteric coating comprises a methacrylic acid/ethyl acrylate copolymer.

11. The method as recited in claim 1 , wherein the delayed release oral pharmaceutical dosage form is administered once per day.

12. The method as recited in claim 1 , wherein the delayed release oral pharmaceutical dosage form is administered twice per day.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 29, 2018
From: MCKEARN, JOHN; BLITZER, JEREMY
To: PATHOLOGICA LLC
Reel/Frame 046239/0261 →
Continuity (4)
Continuation 14480847 · Sep 9, 2014
Continuation 13354076 · Jan 19, 2012
Provisional Application 61434269 · Jan 19, 2011
Related Publication 20180050000A1 · Feb 22, 2018