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Compositions Of Glp 1 Peptides And Preparation Thereof

Abstract: “COMPOSITIONS OF GLP-1 PEPTIDES AND PREPARATION THEREOF” The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine.

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Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
17 March 2020
Publication Number
13/2020
Publication Type
INA
Invention Field
BIOTECHNOLOGY
Status
Email
nncp-in@novonordisk.com
Parent Application

Applicants

Novo Nordisk A/S
Novo Allé, DK-2880 Bagsværd, Denmark

Inventors

1. HANSEN, Tue
NOVO NORDISK A/S, Novo Allé, DK-2880 Bagsværd, Denmark
2. ELIASEN, Helle
NOVO NORDISK A/S, Novo Allé, DK-2880 Bagsværd, Denmark
3. VILHELMSEN, Thomas
NOVO NORDISK A/S, Novo Allé, DK-2880 Bagsværd, Denmark

Specification

1. A process of producing a pharmaceutical composition comprising a salt of N-(8-(2-
hydroxybenzoyl)amino)caprylic acid and a GLP-1 peptide, wherein the process comprises
the steps:
a) mixing a GLP-1 peptide with a filler and/or a binder;
b) dry granulation of the mixture of step a;
c) mixing a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, optionally a lubricant and/or a filler;
d) dry granulation of the mixture of step c;
e) mixing the granules obtained in step b with the granules obtained in step d; and
f) optionally adding further lubricant,
wherein the mixture of step a does not comprise a salt of N-(8-(2-hydroxybenzoyl)amino) caprylic acid and wherein the mixture of step c does not comprise a GLP-1 peptide.
2. A process of producing a pharmaceutical composition comprising a salt of N-(8-(2-
hydroxybenzoyl)amino)caprylic acid and a GLP-1 peptide, wherein the process comprises
the steps:
a) mixing a GLP-1 peptide with a filler and/or a binder;
b) dry granulation of the mixture of step a;
c) mixing the granules obtained in step b with a composition comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid; and
d) optionally adding further lubricant,
wherein the mixture of step a does not comprise a salt of N-(8-(2-hydroxybenzoyl)amino) caprylic acid.
3. A process of producing a pharmaceutical composition comprising a salt of N-(8-(2-
hydroxybenzoyl)amino)caprylic acid and a GLP-1 peptide, wherein the process comprises
the steps:
a) mixing a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid with a lubricant and/or a filler;
b) dry granulation of the mixture of step a;
c) mixing the granules obtained in step b with a composition comprising a GLP-1 peptide; and

d) optionally adding further lubricant
wherein the mixture of step a does not comprise a GLP-1 peptide.
4 The process as claimed in claims 1-3, wherein said dry granulation is roller
compaction.
5. The process as claimed in claims 1-3, wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is SNAC.
6. The process as claimed in claims 1-3, wherein said GLP-1 peptide is semaglutide.
7. The process as claimed in claims 1-3, wherein said lubricant and/or said further lubricant is magnesium stearate.
8. The process as claimed in claims 1-3, wherein said filler is microcrystalline cellulose.
9. The process as claimed in claims 1-3, wherein said binder is povidone.
10. The process as claimed in claims 1-3, wherein said mixing step comprising mixing of a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid with a lubricant and/or a filler prior to dry granulation has a duration of at least 20 minutes, at least 30 minutes, or at least 40 minutes.
11. A process of producing a granule comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, wherein the process comprises the steps:

a) mixing a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (such as SNAC) with a lubricant and/or a filler; and
b) dry granulation of the mixture of step a.
12. A process of producing a granule comprising a salt of N-(8-(2-
hydroxybenzoyl)amino)caprylic acid, wherein the process comprises the steps:
a) mixing a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (such as
SNAC) with a lubricant and/or a filler; and
b) dry granulation of the mixture of step a,
wherein the mixture of step a does not comprise a GLP-1 peptide.

13. The process as claimed in claim 11-12, wherein the mixing step comprising mixing of a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid with a lubricant and/or a filler prior to dry granulation has a duration of at least 20 minutes.
14. The process as claimed in claims 11-13, wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is SNAC
15. The process as claimed in claim 11-14, wherein said lubricant is magnesium stearate.
16. A process of producing a granule comprising a GLP-1 peptide, wherein the process comprises the steps:

a) mixing a GLP-1 peptide, optionally a filler and/or a binder; and
b) roller compacting the mixture of step a.

17. The process as claimed in claims 11-16, wherein said filler is microcrystalline cellulose.
18. The process as claimed in claim 16, wherein said binder is povidone.
19. A granule obtained by the process as claimed in claims 11-12 or 16.

Documents

Application Documents

# Name Date
1 202048011367-STATEMENT OF UNDERTAKING (FORM 3) [17-03-2020(online)].pdf 2020-03-17
2 202048011367-SEQUENCE LISTING(PDF) [17-03-2020(online)].pdf 2020-03-17
3 202048011367-SEQUENCE LISTING [17-03-2020(online)].txt 2020-03-17
4 202048011367-PRIORITY DOCUMENTS [17-03-2020(online)].pdf 2020-03-17
5 202048011367-POWER OF AUTHORITY [17-03-2020(online)].pdf 2020-03-17
6 202048011367-FORM 18 [17-03-2020(online)].pdf 2020-03-17
7 202048011367-FORM 1 [17-03-2020(online)].pdf 2020-03-17
8 202048011367-DECLARATION OF INVENTORSHIP (FORM 5) [17-03-2020(online)].pdf 2020-03-17
9 202048011367-COMPLETE SPECIFICATION [17-03-2020(online)].pdf 2020-03-17
10 202048011367-Proof of Right [06-08-2020(online)].pdf 2020-08-06
11 202048011367-FORM 3 [16-09-2020(online)].pdf 2020-09-16
12 202048011367-FORM 3 [12-03-2021(online)].pdf 2021-03-12
13 202048011367-FORM 3 [08-09-2021(online)].pdf 2021-09-08
14 202048011367-FORM 3 [01-03-2022(online)].pdf 2022-03-01
15 202048011367-FORM 3 [29-08-2022(online)].pdf 2022-08-29
16 202048011367-FER.pdf 2022-11-30
17 202048011367-RELEVANT DOCUMENTS [15-12-2022(online)].pdf 2022-12-15
18 202048011367-POA [15-12-2022(online)].pdf 2022-12-15
19 202048011367-FORM 13 [15-12-2022(online)].pdf 2022-12-15
20 202048011367-PRE GRANT OPPOSITION FORM [14-02-2023(online)].pdf 2023-02-14
21 202048011367-PRE GRANT OPPOSITION DOCUMENT [14-02-2023(online)].pdf 2023-02-14
22 202048011367-OTHERS [14-02-2023(online)].pdf 2023-02-14
23 202048011367-Correspondence_Pre Grant Opposition_20-02-2023.pdf 2023-02-20
24 202048011367-Information under section 8(2) [28-02-2023(online)].pdf 2023-02-28
25 202048011367-Information under section 8(2) [28-02-2023(online)]-2.pdf 2023-02-28
26 202048011367-Information under section 8(2) [28-02-2023(online)]-1.pdf 2023-02-28
27 202048011367-FORM 3 [28-02-2023(online)].pdf 2023-02-28
28 202048011367-Information under section 8(2) [01-03-2023(online)].pdf 2023-03-01
29 202048011367-Information under section 8(2) [01-03-2023(online)]-1.pdf 2023-03-01
30 202048011367-FORM 4(ii) [24-05-2023(online)].pdf 2023-05-24
31 202048011367-OTHERS [29-06-2023(online)].pdf 2023-06-29
32 202048011367-FER_SER_REPLY [29-06-2023(online)].pdf 2023-06-29
33 202048011367-CLAIMS [29-06-2023(online)].pdf 2023-06-29
34 202048011367-Information under section 8(2) [25-08-2023(online)].pdf 2023-08-25
35 202048011367-FORM 3 [25-08-2023(online)].pdf 2023-08-25
36 PREGRANT OPPOSTION NOTICE-202048011367.pdf 2023-09-04
37 202048011367-FORM-26 [20-10-2023(online)].pdf 2023-10-20
38 202048011367-Written submissions and relevant documents [04-12-2023(online)].pdf 2023-12-04
39 202048011367-Annexure [04-12-2023(online)].pdf 2023-12-04
40 202048011367-Information under section 8(2) [23-02-2024(online)].pdf 2024-02-23
41 202048011367-FORM 3 [23-02-2024(online)].pdf 2024-02-23
42 202048011367-FORM-26 [22-03-2024(online)].pdf 2024-03-22
43 202048011367-Representation,including the statement and evidence [13-06-2025(online)].pdf 2025-06-13
46 202048011367-OTHERS [23-10-2025(online)].pdf 2025-10-23
47 202048011367-PRE-GRANT OPPOSITION NOTICE.pdf 2025-10-30

Search Strategy

1 SearchStrategyE_25-08-2022.pdf