IP Library Granted Patent US 9,833,463
Granted Patent B2
US 9,833,463 · App. 15/302,211 · Granted Dec 5, 2017

Sitagliptin tannate complex

Inventors: Wycliffe Omwancha (East Brunswick, NJ); Rubi Burlage (Florham Park, NJ)
Assignee: Merck Sharp & Dohme Corp.
A61K31/7032A61K9/0053A61K31/235A61K31/496A61K31/4985A61K45/06C07D487/04
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Quick Facts
Patent No.
US 9,833,463
App. No.
15/302,211
Granted
Dec 5, 2017
Kind
B2
Abstract

The present invention provides for a sitagliptin tannate complex or a pharmaceutical compositions or a pharmaceutically acceptable intermediates comprising said complex. This invention also relates to a processes to prepare the sitagliptin tannate complex as well as to methods of using the sitagliptin tannate complex to treat diabetes, obesity and high blood pressure.

Claims (15)

1. Sitagliptin tannate complex.

2. The sitagliptin tannate complex according to claim 1 , wherein the sitagliptin content is between about 25% and about 75% by weight.

3. The sitagliptin tannate complex according to claim 2 , wherein the sitagliptin content is between about 29 and about 33% by weight.

4. The sitagliptin tannate complex according to claim 1 , wherein the ratio of sitagliptin to tannic acid is about 3:1 to about 1:4 by weight.

5. The sitagliptin tannate complex according to claim 4 , wherein the ratio is about 2:1 by weight.

6. A pharmaceutical composition comprising a therapeutically effective amount of the sitagliptin tannate complex according to claim 1 and an inert carrier.

7. The pharmaceutical composition according to claim 6 that further comprises a therapeutically effective amount of an additional pharmaceutically active ingredient.

8. A pharmaceutical intermediate which comprises a therapeutically effective amount of a sitagliptin tannate complex according to claim 1 , a pharmaceutically acceptable polymer, and, optionally, one or more polyols, high intensity sweeteners, flavorants.

9. An oral dosage form which comprises the pharmaceutical intermediate according to claim 8 .

10. The oral dosage form according to claim 9 , which is in the form of a tablet, capsule, pellet or powder.

11. The oral dosage form according to claim 9 , which is in the form of a soft chew, medicated gum, chewable tablet, disintegrating tablet, syrup, sachet, oral film, gel or lyosphere.

12. The oral dosage form according to claim 9 , which has negligible release in the mouth and immediate release in the stomach.

13. The oral dosage form according to claim 12 , which is a soft chew, medicated gum, oral film, disintegrating tablet or syrup.

14. A method for treating, controlling, or preventing of one or more diseases for which an inhibitor of DPP-IV is indicated, comprising the administration a therapeutically effective amount of the sitagliptin tannate complex according to claim 1 to a patient in need thereof.

15. The method according to claim 14 , wherein the disease is type 2 diabetes, obesity or high blood pressure.

Assignments (2)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 6, 2016
From: OMWANCHA, WYCLIFFE; BURLAGE, RUBI
To: MERCK SHARP & DOHME CORP.
Reel/Frame 039954/0148 →
Continuity (2)
Provisional Application 61980641 · Apr 17, 2014
Related Publication 20170042922A1 · Feb 16, 2017