Purifying method of carperitide

Abstract

The invention provides a purifying method of carperitide. The purifying method comprises the following steps of: 1) dissolving a sample through 3 to 18% of an aqueous solution of an organic solvent based on volume by volume concentration, wherein the organic solvent has high polarity; preparing to obtain 100g / L of solution based on concentration; 2), getting octadecylsilane bonded silica gel as a stationary phase, getting 10 to 50mmol / L of sulfuric acid buffer salt in which 0.1 to 0.8% of perchloric acid is added based on a volume ratio as phase A, and getting acetonitrile as phase B, wherein volume ratio concentration of the phase B is 17 to 37%; feeding a solution prepared in step 1) to carry out gradient elution; and 3) transferring the carperitide sulfate into hydrochloride; carrying out a reverse phase HPLC (High Performance Liquid Chromatography) method; getting the octadecylsilane bonded silica gel as the stationary phase; carrying out the gradient elution; and drying to obtain the carperitide in a freezing way. The purifying method of the carperitide provided by the invention is stable and controllable in technology, high in yield, high in purity, wide in practical value and wide in application prospect.

Description

technical field [0001] The invention relates to a purification method of polypeptide medicine, in particular to a purification method of capecritide, and belongs to the field of medicinal chemistry. Background technique [0002] Acute heart failure (including acute exacerbation of chronic heart failure) Heart failure refers to a kind of overload cardiomyopathy caused by abnormal gene expression caused by insufficient energy, and finally caused by insufficient energy, myocardial ischemia, apoptosis of myocardial cells, myocardial The number of systolic units decreases, and this overload enters a vicious circle. [0003] Capecritide, trade name Caperitine, is a cycle regulating hormone composed of 28 amino acids, its molecular formula is: H-Ser-Leu-Arg-Arg-Ser-Ser-Cys-Phe-Gly-Gly -Arg-Met-Asp-Arg-IIe-Gly-Ala-Gln-Ser-Gly-Leu-Gly-Cys-Asn-Ser-Phe-Arg-Tyr-OH. As a polypeptide drug for the treatment of acute heart failure (including the exacerbation of chronic heart failure), cap...

AI Technical Summary

Problems solved by technology

This patent discloses a capecritide purification process using phosphate buffer purification and acetate conversion to salt, but in the process of purification with phosphate buffer salt, it is difficult to effectively control impurities, which in turn affects the purity and yield; During the salt process, it was found that the stability of capecritide hydrochloride was poor

[0005] The method of prior art CN102382188A is used to purify capecritide, the purity can only reach 98.5%, and the total yield is about 32.1%, which is difficult to achieve the purity of finished medicine and the yield of industrial production

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