Pharmaceutical composition comprising a GLP-1 receptor agonist, a GIP / GLP-1 receptor agonist, and / or a GLP-1 / GIP / GCG receptor triple agonist.

Abstract

The present invention provides a pharmaceutical composition comprising one or more microparticles selected from GLP-1 receptor agonists, GIP / GLP-1 receptor agonists, and GLP-1 / GIP / GCG receptor triple agonists, and one or more pharmaceutically acceptable first carriers selected from the group consisting of a fluid oil containing a fatty acid ester, a surfactant, and a polyhydric alcohol. The pharmaceutical composition allows the microparticles to maintain stability for a long period in a suspension formulation, and the microparticles, after long-term storage, exhibit excellent dissolution properties. Furthermore, the pharmaceutical composition improves bioavailability and reduces the dosage.

Claims

1. Microparticles containing one or more selected from GLP-1 receptor agonists, GIP / GLP-1 receptor agonists, and GLP-1 / GIP / GCG receptor triple agonists, A pharmaceutical composition characterized by comprising one or more pharmaceutically acceptable first carriers selected from the group consisting of a fluid oil containing a fatty acid ester, a surfactant, and a polyhydric alcohol.

2. The pharmaceutical composition according to claim 1, characterized in that the fluid oil is one or more selected from coconut oil, palm oil, palm kernel oil, sesame oil, soybean oil, almond oil, rapeseed oil, corn oil, sunflower oil, peanut oil, olive oil, castor oil, safflower oil, cottonseed oil, and ethyl oleate.

3. The pharmaceutical composition according to claim 1, characterized in that the surfactant is one or more selected from poloxamer 188, poloxamer 407, polysorbate 20, polysorbate 60, polysorbate 80, polyoxyethylene oleyl ether, polyoxyethylene cetyl ether, polyoxyethylene stearyl ether, and polyoxyethylene lauryl ether.

4. The pharmaceutical composition according to claim 1, characterized in that the polyhydric alcohol is one or more selected from ethylene glycol, propylene glycol, polyethylene glycol, glycerol, erythritol, treitol, xylitol, ribitol, mannitol, sorbitol, and maltitol.

5. The pharmaceutical composition according to claim 4, characterized in that the polyhydric alcohol is ethylene glycol, propylene glycol, polyethylene glycol, or glycerol.

6. The pharmaceutical composition according to claim 1, characterized in that, based on 1 mL of the first carrier, one or more selected from GLP-1 receptor agonists, GIP / GLP-1 receptor agonists, and GLP-1 / GIP / GCG receptor triple agonists contained in fine particles are contained in a concentration range of 0.01 mg to 2,000 mg.

7. The pharmaceutical composition according to claim 1, characterized in that the GLP-1 receptor agonist, GIP / GLP-1 receptor agonist and / or GLP-1 / GIP / GCG receptor triple agonist is one or more selected from exenatide, liraglutide, lixisenatide, albiglutide, dulaglutide, semaglutide, tilzepatide, cotadutide, taspoglutide, letatoltide and pharmaceutically acceptable salts thereof.

8. The pharmaceutical composition according to claim 1, characterized in that one or more selected from the GLP-1 receptor agonist, GIP / GLP-1 receptor agonist, and GLP-1 / GIP / GCG receptor triple agonist are included in an amount of 3% to 50% by weight based on the total weight of the fine particles.

9. The pharmaceutical composition according to claim 1, characterized in that the fine particles further comprise a biocompatible polymer.

10. The pharmaceutical composition according to claim 9, characterized in that the biocompatible polymer is one or more selected from polylactic acid, polylactide, poly(lactic-co-glycolic acid), poly(lactide-co-glycolide) (PLGA), polyphosphazene, poly(iminocarbonate), polyphosphoester, polyanhydride, polyorthoester, copolymer of lactic acid and caprolactone, polycaprolactone, polyhydroxyvalerate, polyhydroxybutyrate, polyamino acid, and copolymer of lactic acid and amino acid.

11. The pharmaceutical composition according to claim 9, characterized in that the biocompatible polymer is contained in an amount of 50 to 97% by weight based on the total weight of the fine particles.

12. The pharmaceutical composition according to claim 1, further comprising one or more additives selected from buffers, isotonic agents, preservatives, and pH adjusters.

13. The pharmaceutical composition according to claim 9, characterized in that the fine particles contain one or more selected from the GLP-1 receptor agonist, GIP / GLP-1 receptor agonist, and GLP-1 / GIP / GCG receptor triple agonist and the biocompatible polymer in a weight ratio of 1:1 to 50.

14. The pharmaceutical composition according to claim 1, characterized in that the fine particles are maintained in a stable state for six months or more.

15. The pharmaceutical composition according to claim 1, characterized in that the pharmaceutical composition is an injectable preparation.

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