IP Library Granted Patent US 11,471,512
Granted Patent B2
US 11,471,512 · App. 16/801,227 · Granted Oct 18, 2022

Pharmaceutical compositions of a peptide

Inventors: Himanshu Bhattacharjee (Collegeville, PA); Suzanne M. D'Addio (Jamaica Plain, MA); Sachin Lohani (Annandale, NJ); Sachin Mittal (Bridgewater, NJ); Sergei Y. Pechenov (Gaithersburg, MD); Daniel Hong Yin (Exton, PA)
Assignee: Merck Sharp & Dohme LLC
A61K38/26A61K47/10A61K47/183A61K47/186A61K47/22A61K47/24A61K47/26
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Quick Facts
Patent No.
US 11,471,512
App. No.
16/801,227
Granted
Oct 18, 2022
Kind
B2
Abstract

Disclosed are pharmaceutical compositions comprising the peptide of SEQ ID No. 1, or a pharmaceutically acceptable salt or counterion thereof, methods of preparing such pharmaceutical compositions, and methods of treating diabetes and diabetes-related disorders with such pharmaceutical compositions.

Claims (120)

1. A pharmaceutical composition comprising:

1) about 0.1%-56% by weight of the peptide of SEQ ID NO. 1, or a pharmaceutically acceptable salt or counterion thereof;

2) about 9.6%-99.7% by weight of an anti-microbial agent,

3) about 0.1% -46% by weight of a buffer;

4) about 0.1% -38% by weight of an anti-oxidant; and

5) about 14% -88% by weight of a tonicity agent;

before constitution with a solvent, or a custom solvent, wherein

the anti-microbial agent is benzyl alcohol;

the buffer is L-histidine;

the tonicity agent is selected from:

1) propylene glycol, and

2) sucrose; and

the anti-oxidant is selected from:

1) L-methionine,

2) ethylenediamine tetra acetic acid or a salt and/or hydrate thereof, and

3) a combination of L-methionine and ethylenediamine tetra acetic acid, or a salt and/or hydrate thereof.

2. The pharmaceutical composition of claim 1 wherein

the tonicity agent is sucrose; and

the anti-oxidant is a combination of L-methionine and ethylenediamine tetra acetic acid, or a salt and/or hydrate thereof.

3. The pharmaceutical composition of claim 1 wherein the pharmaceutical composition is constituted with a solvent, or a custom solvent.

4. The pharmaceutical composition of claim 1 comprising:

1) about 0.6%-24%by weight of the peptide of SEQ ID No. 1, or a pharmaceutically acceptable salt or counterion thereof;

2) about 10.2%-98.8 by weight of an anti-microbial agent;

3) about 1.2%-43% by weight of a buffer;

4) about 0.1% -21% by weight of an anti-oxidant; and

5) about 34%-79% by weight of a tonicity agent,

before constitution with a solvent, or a custom solvent, wherein

the anti-microbial agent is benzyl alcohol;

the buffer is L-histidine;

the tonicity agent is selected from:

1) propylene glycol, and

2) sucrose; and

the anti-oxidant is selected from:

1) L-methionine,

2) ethylenediamine tetra acetic acid or a salt and/or hydrate thereof, and

a combination of L-methionine and ethylenediamine tetra acetic acid, or a salt and/or hydrate_thereof.

5. The pharmaceutical composition of claim 4 wherein

the tonicity agent is sucrose; and

the anti-oxidant is a combination of L-methionine and ethylenediamine tetra acetic acid, or a salt and/or hydrate thereof.

6. The pharmaceutical composition of claim 4 additionally comprising water.

7. The pharmaceutical composition of claim 1 comprising:

1) about 1.3%-17% by weight of the peptide of SEQ ID No. 1, or a pharmaceutically acceptable salt or counterion thereof;

2) about 22%-94% by weight of an anti-microbial agent;

3) about 5.6%-36% by weight of a buffer;

4) about 1.5-11% by weight of an anti-oxidant; and

5) about 42%-72% by weight of a tonicity agent,

before constitution with a solvent, or a custom solvent, wherein

the anti-microbial agent is benzyl alcohol;

the buffer is L-histidine;

the tonicity agent is selected from;

1) propylene glycol, and

2) sucrose; and

the anti-oxidant is selected from:

1) L-methionine,

2) ethylenediamine tetra acetic acid or a salt and/or hydrate thereof, and a combination of L-methionine and ethylenediamine tetra acetic acid or a salt and/or hydrate thereof.

8. The pharmaceutical composition of claim 7 wherein

the tonicity agent is sucrose; and

the anti-oxidant is a combination of L-methionine and ethylenediamine tetra acetic acid or a salt and/or hydrate thereof.

9. The pharmaceutical composition of claim 7 additionally comprising water.

10. The pharmaceutical composition of claim 1 comprising:

1) about 2%-4% by weight of the peptide of SEQ ID No. 1, or a pharmaceutically acceptable salt or counterion thereof;

2) about 28%-32% by weight of benzyl alcohol;

3) about 12%-14% by weight of L-histidine;

4) about 48%-52% by weight of sucrose;

5) about 2%-3% by weight of L-methionine; and

6) about 0.01%-0.5% by weight of ethylenediamine tetra acetic acid, or a salt and/or hydrate thereof,

before constitution with a solvent, or a custom solvent.

11. The pharmaceutical composition of claim 10 additionally comprising water.

12. A method of treating diabetes, a diabetes related disorder, obesity or an obesity related disorder, in a human in need thereof comprising administering to the human a pharmaceutical composition of claim 1 .

13. The pharmaceutical composition comprising:

1) about 0.01%-1% by weight of the peptide of SEQ ID NO. 1, or a pharmaceutically acceptable salt or counterion thereof;

2) about 0.8% -3% by weight of an anti-microbial agent;

3) about 0.01%-1.5% by weight of a buffer;

4) about 0.05%-0.5% by weight of an anti-oxidant; and

5) about 1%-6% by weight of a tonicity agent;

after constitution with a solvent, or a custom solvent,

wherein

the anti-microbial agent is benzyl alcohol;

the buffer is L-histidine;

the tonicity agent is selected from:

1) propylene glycol, and

2) sucrose; and

the anti-oxidant is selected from:

1) L-methionine,

2) ethylenediamine tetra acetic acid or a salt and/or hydrate thereof, and

3) a combination of L-methionine and ethylenediamine tetra acetic acid, or a salt and/or hydrate thereof.

14. The pharmaceutical composition of claim 13 wherein

the tonicity agent is sucrose; and

the anti-oxidant is a combination of L-methionine and ethylenediamine tetra acetic acid, or a salt and/or hydrate thereof.

15. The pharmaceutical composition of claim 14 wherein the solvent is water.

16. The pharmaceutical composition of claim 13 wherein the solvent is water.

17. The pharmaceutical composition of claim 13 comprising:

1) about 0.05%-0.4% by weight of the peptide of SEQ ID No. 1, or a pharmaceutically acceptable salt or counterion thereof;

2) about 1.3%-2.5% by weight of an anti-microbial agent;

3) about 0.1%-10.9% by weight of a buffer;

4) about 0.15%-0.3% by weight of an anti-oxidant; and

5) about 2%-5% by weight of a tonicity agent,

after constitution with a solvent, or a custom solvent,

wherein

the anti-microbial agent is benzyl alcohol;

the buffer is L-histidine;

the tonicity agent is selected from:

1) propylene glycol, and

2) sucrose; and

the anti-oxidant is selected from:

1) L-methionine,

2) ethylenediamine tetra acetic acid or a salt and/or hydrate thereof, and ps a combination of L-methionine and ethylenediamine tetra acetic acid, or a salt and/or hydrate thereof.

18. The pharmaceutical composition of claim 17 wherein

the tonicity agent is sucrose; and

the anti-oxidant is a combination of L-methionine and ethylenediamine tetra acetic acid, or a salt and/or hydrate thereof.

19. The pharmaceutical composition of claim 17 wherein the solvent is water.

20. The pharmaceutical composition of claim 13 comprising:

1) about 0.01%-2% by weight of the peptide of SEQ ID No. 1, or a pharmaceutically acceptable salt or counterion thereof;

2) about 1%-3% by weight of benzyl alcohol;

3) about 0.5%-1% by weight of L-histidine;

4) about 2%-4% by weight of sucrose;

5) about 0.01%-0.3% by weight of L-methionine; and

6) about 0.01%-0.3% by weight of ethylenediamine tetra acetic acid, or a salt and/or hydrate thereof,

after constitution with a solvent, or a custom solvent.

21. The pharmaceutical composition of claim 20 wherein the solvent is water.

Assignments (3)
MERGER Recorded Aug 25, 2022
From: MERCK SHARP & DOHME CORP
To: MERCK SHARP & DOHME LLC
Reel/Frame 060897/0573 →
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 Feb 26, 2020
From: BHATTACHARJEE, HIMANSHU; D'ADDIO, SUZANNE M.; LOHANI, SACHIN; MITTAL, SACHIN; PECHENOV, SERGEI Y.; YIN, DANIEL HONG
To: MERCK SHARP & DOHME CORP
Reel/Frame 052020/0042 →
Continuity (2)
Provisional Application 62812375 · Mar 1, 2019
Related Publication 20200276274A1 · Sep 3, 2020