Liraglutide purifying method

Abstract

The invention discloses a liraglutide purifying method. The liraglutide purifying method comprises the following steps that 1, a liraglutide coarse product is pretreated to obtain a liraglutide crudepeptide water solution; 2, first-time HPLC purification for removing fragment impurities is performed; 3, a solvent is removed, and a first-step liraglutide sample solution is obtained; 4, second-timeHPLC purification for removing multi-Gly-sequence peptides, Gly-sequence-deleted peptides and epimers produced during synthesis is performed; 5, part of solvent is removed to obtain a second-step liraglutide sample solution, and a PH value is regulated to 6.5 so as to obtain a final liraglutide sample solution. The multi-Gly-sequence peptides, Gly-sequence-deleted peptides, epimers and other impurities produced during synthesis can be removed, and the purity and yield of liraglutide samples are improved.

Description

technical field

[0001] The invention relates to the field of peptide purification, in particular to a purification method for solid-phase synthesis of liraglutide. Background technique

[0002] Liraglutide, English name: Liraglutide.

[0003] The peptide sequence is:

[0004] H-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly--Gln-

[0005] Ala-Ala-Lys(Pal-γ-Glu)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH

[0006] Liraglutide is the first long-acting GLP-1 analogue developed by Novo Nordisk, Denmark. It is 97% homologous to human glucagon-like peptide-1 (GLP-1). Liraglutide has various effects such as lowering blood sugar, promoting regeneration of islet cells, and slightly prolonging gastric emptying, and has broad application prospects.

[0007] Liraglutide, as a new generation of incretin-based hypoglycemic drugs, not only has a long acting time, but also fully retains multiple physiological activities of natural GLP-1, which can safely and effectiv...

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