Thermostable formulation of a21g human insulin

Patent metadata

Field	Value
Publication number	US-2025099551-A1
Application number	US-202418970153-A
Country	US
Kind code	A1
Filing date	Dec 5, 2024
Priority date	Jul 13, 2018
Publication date	Mar 27, 2025
Grant date	—

Abstract

A method for treating diabetes includes administering a composition in the form of an injectable aqueous solution, the pH of which is between 7.2 and 8.0 (7.2≤pH≤ 8.0) comprising at least A21G human insulin, to a patient in need thereof, wherein the composition is administered as a bolus before meals.

First claim

1 . A method for treating diabetes, comprising administering a composition in the form of an injectable aqueous solution, the pH of which is between 7.2 and 8.0 (7.2≤pH≤8.0) comprising at least A21G human insulin, to a patient in need thereof, wherein the composition is administered as a bolus before meals.

2 . The method according to claim 1 , wherein a concentration of A21G human insulin in the composition is between 40 and 1000 U/ml (40 U/mL≤concentration of A21G human insulin≤1000 U/mL).

3 . The method according to claim 2 , wherein the concentration of A21G human insulin is 100 U/mL.

4 . The method according to claim 2 , wherein the concentration of A21G human insulin is 300 U/mL.

5 . The method according to claim 1 , wherein the composition further includes zinc salt at a concentration of from 50 to 600 μM per 100 U/mL of A21G insulin.

6 . The method according to claim 1 , wherein the composition further comprises a phenolic preservative at a concentration of from 15 to 100 mM.

7 . The method according to claim 6 , wherein the phenolic preservative is phenol, and a concentration of the phenol in the composition is between 30 and 75 mM (30 mM≤phenol concentration≤75 mM).

8 . The method according to claim 1 , wherein the composition further comprises a surfactant chosen from polysorbates at a concentration between 4 and 20 μM (4 μM≤polysorbate concentration≤20 μM).

9 . The method according to claim 1 , wherein the composition further comprises arginine.

10 . The method according to claim 1 , wherein the composition further comprises trishydroxymethylaminomethane at a concentration between 2 and 100 mM (2 mM≤trishydroxymethylaminomethane concentration≤100 mM).

11 . A method for treating diabetes, comprising administering a composition in the form of an injectable aqueous solution, the pH of which is between 7.2 and 8.0 (7.2≤pH≤8.0) comprising at least A21G human insulin, to a patient in need thereof, wherein the composition is administered as prandial insulin.

12 . The method according to claim 11 , wherein a concentration of A21G human insulin in the composition is between 40 and 1000 U/ml (40 U/mL≤concentration of A21G human insulin≤1000 U/mL).

13 . The method according to claim 12 , wherein the concentration of A21G human insulin is 100 U/mL.

14 . The method according to claim 12 , wherein the concentration of A21G human insulin is 300 U/mL.

15 . The method according to claim 11 , wherein the composition further includes zinc salt at a concentration of from 50 to 600 μM per 100 U/mL of A21G insulin.

16 . The method according to claim 11 , wherein the composition further comprises a phenolic preservative at a concentration of from 15 to 100 mM.

17 . The method according to claim 16 , wherein the phenolic preservative is phenol, and a concentration of the phenol in the composition is between 30 and 75 mM (30 mM≤phenol concentration≤75 mM).

18 . The method according to claim 11 , wherein the composition further comprises a surfactant chosen from polysorbates at a concentration between 4 and 20 μM (4 μM≤polysorbate concentration≤20 μM).

19 . The method according to claim 11 , wherein the composition further comprises arginine.

20 . The method according to claim 11 , wherein the composition further comprises trishydroxymethylaminomethane at a concentration between 2 and 100 mM (2 mM≤trishydroxymethylaminomethane concentration≤100 mM).

Assignees

• Adocia

Inventors

• Chan You-Ping
• Di Lorenzo Fany

Classifications

• A61K47/26

  Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin · CPC title

• A61K47/183

  Amino acids, e.g. glycine, EDTA or aspartame · CPC title

• A61K47/18

  Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61K9/08

  Solutions {(composition of solutions A61K47/00)} · CPC title