Abstract: The invention relates to pharmaceutical compositions comprising a peptide, such a GLP-1 peptide and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid. The invention further relates to processes for the preparation of such compositions, and their use in medicine.
1. A pharmaceutical composition comprising
a) 0.5-50 mg of a GLP-1 agonist and
5 b) 20-800 mg, such as 50-500 mg, of a salt of N-(8-(2-
hydroxybenzoyl)amino)caprylic acid and c) 0.6-20 mg, such as 1-10 mg, lubricant, wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid constitutes at least 90 w/w %, such as at least 95 w/w % of the excipients of the composition. 10
2. The pharmaceutical composition according to claim 1, wherein the lubricant is
magnesium stearate or glyceryl dibehenate.
3. The pharmaceutical composition according to claim 1 or claim 2 consisting of:
15 a) a GLP-1 agonist,
b) a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and
c) at least one lubricant.
4. The pharmaceutical composition according to any of the previous claims, wherein said
20 salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid constitutes at least 90 w/w % of the
composition.
5. The pharmaceutical composition according to any of the previous claims, wherein the
compositions comprises 1-8 mg, such as 2-5 mg or such as 2-3 mg magnesium stearate
25 per 100 mg of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid.
6. The pharmaceutical composition according to any of the previous claims wherein the
GLP-1 agonist is a GLP-1 peptide substituted with a fatty acid or a fatty diacid, such as a
GLP-1 agonist selected from the group consisting of: semaglutide, Ns26{2-[2-(2-{2-[2-(2-
30 {(S)-4-Carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butyrylamino}-
ethoxy)ethoxy]acetylamino}ethoxy)ethoxy]acetyl}, /\f57-{2-[2-(2-{2-[2-(2-{(S)-4-carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butyrylamino}ethoxy)ethoxy]acetylamino}-ethoxy)ethoxy]-acetyl}-[Aib8,Arg34,Lys37]GLP-1(7-37)-peptide (GLP-1 agonist B) and N£27-[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butanoyl]-
35 amino] ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]-acetyl], N£36-[2-[2-[2-[[2-[2-[2-[[(4S)-4-
carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butanoyl]amino]ethoxy]ethoxy]acetyl]-amino]ethoxy]ethoxy]acetyl]-[Aib8,Glu22,Arg26,Lys27, Glu30,Arg34,Lys36]-GLP-1-(7-37)-peptidyl-Glu-Gly (GLP-1 agonist C).
5 7. The pharmaceutical composition according to any of the previous claims, wherein the salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is sodium N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC).
8. The pharmaceutical composition according to any of the previous claims, wherein a dose
10 unit comprises;
a) 0.5-20 mg of semaglutide,
b) 50-400 mg of SNAC and
c) 1-10 mg lubricant.
15 9. The pharmaceutical composition according to any of the previous claims, wherein a dose unit comprises;
a) 1-10 mg of semaglutide,
b) 50-300 mg of SNAC and
c) 1-10 mg magnesium stearate. 20
10. The pharmaceutical composition according to any of the previous claims 1-6, wherein a
dose unit comprises;
a) 0.5-20 mg of the GLP-1 agonist C,
b) 50-400 mg of SNAC and 25 c) 1-10 mg lubricant.
11. The pharmaceutical composition according to any of the previous claims 1-6, wherein a
dose unit comprises;
a) 1-10 mg of the GLP-1 agonist C,
30 b) 50-300 mg of SNAC and
c) 1-10 mg magnesium stearate.
12. The pharmaceutical composition according to any of the previous claims, wherein the
composition is a solid composition, such as a tablet for oral administration.
35
13. A pharmaceutical composition according to any of the previous claims for use in
medicine.
14. A pharmaceutical composition according to any of the previous claims for use in a
5 method of treatment of diabetes and/or obesity.
15. A method of treatment of a subject in need thereof, wherein the method comprises
administering a therapeutically active amount of a composition according to any of the
previous claims to said subject.
| # | Name | Date |
|---|---|---|
| 1 | 202047035833-STATEMENT OF UNDERTAKING (FORM 3) [20-08-2020(online)].pdf | 2020-08-20 |
| 2 | 202047035833-SEQUENCE LISTING(PDF) [20-08-2020(online)].pdf | 2020-08-20 |
| 3 | 202047035833-SEQUENCE LISTING [20-08-2020(online)].txt | 2020-08-20 |
| 4 | 202047035833-PRIORITY DOCUMENTS [20-08-2020(online)].pdf | 2020-08-20 |
| 5 | 202047035833-POWER OF AUTHORITY [20-08-2020(online)].pdf | 2020-08-20 |
| 6 | 202047035833-FORM 1 [20-08-2020(online)].pdf | 2020-08-20 |
| 7 | 202047035833-DRAWINGS [20-08-2020(online)].pdf | 2020-08-20 |
| 8 | 202047035833-DECLARATION OF INVENTORSHIP (FORM 5) [20-08-2020(online)].pdf | 2020-08-20 |
| 9 | 202047035833-COMPLETE SPECIFICATION [20-08-2020(online)].pdf | 2020-08-20 |
| 10 | 202047035833-FORM 18 [21-08-2020(online)].pdf | 2020-08-21 |
| 11 | 202047035833-Proof of Right [27-08-2020(online)].pdf | 2020-08-27 |
| 12 | 202047035833-FORM 3 [22-02-2021(online)].pdf | 2021-02-22 |
| 13 | 202047035833-FORM 3 [12-08-2021(online)].pdf | 2021-08-12 |
| 14 | 202047035833.pdf | 2021-10-18 |
| 15 | 202047035833-FORM 3 [09-02-2022(online)].pdf | 2022-02-09 |
| 16 | 202047035833-FORM 3 [08-08-2022(online)].pdf | 2022-08-08 |
| 17 | 202047035833-RELEVANT DOCUMENTS [15-12-2022(online)].pdf | 2022-12-15 |
| 18 | 202047035833-POA [15-12-2022(online)].pdf | 2022-12-15 |
| 19 | 202047035833-FORM 13 [15-12-2022(online)].pdf | 2022-12-15 |
| 20 | 202047035833-FORM 3 [06-02-2023(online)].pdf | 2023-02-06 |
| 21 | 202047035833-FER.pdf | 2023-02-07 |
| 22 | 202047035833-FORM 4(ii) [02-08-2023(online)].pdf | 2023-08-02 |
| 23 | 202047035833-Information under section 8(2) [04-08-2023(online)].pdf | 2023-08-04 |
| 24 | 202047035833-FORM 3 [04-08-2023(online)].pdf | 2023-08-04 |
| 25 | 202047035833-FER_SER_REPLY [06-09-2023(online)].pdf | 2023-09-06 |
| 26 | 202047035833-COMPLETE SPECIFICATION [06-09-2023(online)].pdf | 2023-09-06 |
| 27 | 202047035833-CLAIMS [06-09-2023(online)].pdf | 2023-09-06 |
| 28 | 202047035833-FORM-26 [20-10-2023(online)].pdf | 2023-10-20 |
| 29 | 202047035833-Information under section 8(2) [02-02-2024(online)].pdf | 2024-02-02 |
| 30 | 202047035833-FORM 3 [02-02-2024(online)].pdf | 2024-02-02 |
| 31 | 202047035833-FORM-26 [22-03-2024(online)].pdf | 2024-03-22 |
| 32 | 202047035833-US(14)-HearingNotice-(HearingDate-01-05-2024).pdf | 2024-04-04 |
| 33 | 202047035833-PRE GRANT OPPOSITION FORM [05-04-2024(online)].pdf | 2024-04-05 |
| 34 | 202047035833-PRE GRANT OPPOSITION DOCUMENT [05-04-2024(online)].pdf | 2024-04-05 |
| 35 | 202047035833-Statement and Evidence [18-06-2024(online)].pdf | 2024-06-18 |
| 36 | 202047035833-PreGrant-HearingNotice-(HearingDate-22-08-2024)-1430.pdf | 2024-07-23 |
| 37 | 202047035833-REQUEST FOR ADJOURNMENT OF HEARING UNDER RULE 129A [14-08-2024(online)].pdf | 2024-08-14 |
| 38 | 202047035833-PreGrant-ExtendedHearingNotice-(HearingDate-25-09-2024)-1430.pdf | 2024-08-20 |
| 39 | 202047035833-REQUEST FOR ADJOURNMENT OF HEARING UNDER RULE 129A [19-09-2024(online)].pdf | 2024-09-19 |
| 40 | 202047035833-PreGrant-ExtendedHearingNotice-(HearingDate-25-10-2024)-1430.pdf | 2024-09-20 |
| 41 | 202047035833-Representation,including the statement and evidence [30-09-2024(online)].pdf | 2024-09-30 |
| 42 | 202047035833-RELEVANT DOCUMENTS [14-10-2024(online)].pdf | 2024-10-14 |
| 43 | 202047035833-POA [14-10-2024(online)].pdf | 2024-10-14 |
| 44 | 202047035833-FORM 13 [14-10-2024(online)].pdf | 2024-10-14 |
| 45 | 202047035833-REQUEST FOR ADJOURNMENT OF HEARING UNDER RULE 129A [21-10-2024(online)].pdf | 2024-10-21 |
| 46 | 202047035833-PreGrant-ExtendedHearingNotice-(HearingDate-22-11-2024)-1430.pdf | 2024-10-25 |
| 47 | 202047035833-PRE GRANT OPPOSITION FORM [01-11-2024(online)].pdf | 2024-11-01 |
| 48 | 202047035833-PRE GRANT OPPOSITION DOCUMENT [01-11-2024(online)].pdf | 2024-11-01 |
| 49 | 202047035833-OTHERS [01-11-2024(online)].pdf | 2024-11-01 |
| 50 | 202047035833-Response to office action [15-11-2024(online)].pdf | 2024-11-15 |
| 51 | 202047035833-Response to office action [18-11-2024(online)].pdf | 2024-11-18 |
| 52 | 202047035833-Statement and Evidence [10-01-2025(online)].pdf | 2025-01-10 |
| 53 | 202047035833-Response to office action [12-02-2025(online)].pdf | 2025-02-12 |
| 54 | 202047035833-PRE GRANT OPPOSITION FORM [11-06-2025(online)].pdf | 2025-06-11 |
| 55 | 202047035833-PRE GRANT OPPOSITION DOCUMENT [11-06-2025(online)].pdf | 2025-06-11 |
| 56 | 202047035833-OTHERS [11-06-2025(online)].pdf | 2025-06-11 |
| 57 | 202047035833-Statement and Evidence [15-09-2025(online)].pdf | 2025-09-15 |
| 58 | 202047035833-Response to office action [19-09-2025(online)].pdf | 2025-09-19 |
| 1 | SearchstrategyE_06-02-2023.pdf |
| 2 | IntellectualPropertyIndiaE_06-02-2023.pdf |