Pharmaceutical composition comprising GLP-1 and GIP dual-receptor agonist and use thereof

Abstract

A pharmaceutical composition comprising a GLP-1 and GIP dual-receptor agonist and use thereof. Specifically, the pharmaceutical composition comprises the GLP-1 and GIP dual-receptor agonist, a stabilizer, a buffer salt, and a bacteriostatic agent. In the provided pharmaceutical composition, auxiliary materials such as the stabilizer, the buffer salt, and the bacteriostatic agent are selected and added, such that the polypeptide GLP-1 and GIP dual-receptor agonist serving as a pharmaceutical active ingredient has good solubility in a liquid formulation. Meanwhile, the problems of drug failure and the like caused by the polymerization of the agonist are avoided, and the pharmaceutical composition has good stability and antibacterial efficacy and meets the requirements of a multi-dose injection. The pharmaceutical composition exhibits an important application prospect in the prevention and treatment of metabolic disorder-related diseases such as diabetes or diabetic complications and obesity or obesity complications.

Claims

1. A pharmaceutical composition comprising a GLP-1 and GIP dual receptor agonist, comprising a GLP-1 and GIP dual receptor agonist, a stabilizer, a buffer salt, and an antibacterial agent; The GLP-1 and GIP dual receptor agonist is a compound as shown in Formula I or a pharmaceutically acceptable salt, ester, solvate, optical isomer, tautomer, isotope-labeled substance or prodrug thereof:

2. The pharmaceutical composition according to claim 1, characterized in that The pharmaceutical composition is a liquid preparation; Preferably, the pharmaceutical composition is an injection.

3. The pharmaceutical composition according to claim 1, characterized in that The concentration of the GLP-1 and GIP dual receptor agonist is 2 to 36 mg / mL; Preferably, the concentration of the GLP-1 and GIP dual receptor agonist is 5 to 30 mg / mL.

4. The pharmaceutical composition according to claim 1, characterized in that The antibacterial agent is phenol or m-cresol; Preferably, when the antibacterial agent is phenol, the concentration of the antibacterial agent is 5.3-5.5 mg / mL; When the antibacterial agent is m-cresol, the concentration of the antibacterial agent is 2.4-3.0 mg / mL.

5. The pharmaceutical composition according to claim 1, characterized in that The concentration of the stabilizer in the pharmaceutical composition is 10 to 20 mg / mL; the stabilizer is a polyol; Preferably, the stabilizer is propylene glycol, mannitol or glycerol; More preferably, the stabilizer is propylene glycol.

6. The pharmaceutical composition according to claim 1, characterized in that The buffer salt is selected from hydrogen phosphate, hydrogen phosphate hydrate, citrate, citrate hydrate, acetate or acetate hydrate; Preferably, the buffer salt is hydrogen phosphate hydrate, citrate hydrate or acetate hydrate.

7. The pharmaceutical composition according to claims 1-6, characterized in that The concentration of the buffer salt in the pharmaceutical composition is 7 to 23 mM; Preferably, the concentration of the buffer salt is 10 mM.

8. The pharmaceutical composition according to any one of claims 1 to 7, characterized in that The pH value of the pharmaceutical composition is 6.5 to 8.5; Preferably, the pH value of the pharmaceutical composition is 7.0 to 8.4; More preferably, the pH value of the pharmaceutical composition is 7.2 to 8.2; More preferably, the pH value of the pharmaceutical composition is 7.2-7.

6.

9. A method for preparing the pharmaceutical composition according to any one of claims 1 to 8, comprising the steps of: dissolving a stabilizer, a buffer salt, and an antibacterial agent in a solvent, adding a GLP-1 and GIP dual receptor agonist to prepare a solution, and adjusting the pH of the solution to a target value.

10. Use of the pharmaceutical composition according to any one of claims 1 to 8 in the preparation of a medicament for preventing and / or treating diseases related to metabolic disorders; Preferably, the metabolic disorder-related disease is diabetes, diabetic complications, obesity or obesity complications.

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