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Method for purifying semaglutide

A purification method and crude peptide technology, applied in the field of medicine and chemical industry, can solve the problems of affecting the purity and yield of the sample, poor solubility of the finished product, etc., and achieve the effect of good solubility of the finished product

Pending Publication Date: 2021-06-11
苏州天马医药集团天吉生物制药有限公司
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Problems solved by technology

[0003] There are many impurities in the crude product of solid-phase synthesis of semaglutide that affect the purity and yield of the sample. At present, there have been many studies on the purification of semaglutide, and the purity can reach more than 99%. However, the existing The solubility of the finished product obtained by the purification method is not good, and other means are needed to improve the solubility of the finished product in the subsequent research and application process

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  • Method for purifying semaglutide
  • Method for purifying semaglutide

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Embodiment 1

[0029] A method for purifying semaglutide, comprising the steps of:

[0030] (1) Dissolution: Dissolve the crude semaglutide peptide at 5 mmol / L in an acetonitrile aqueous solution with a volume ratio (v / v) of 10%-20%, to obtain an aqueous solution of semaglutide, heat it in a water bath at 45°C for 2 hours, and then use 0.45 Filter with μm mixed filter membrane, spare;

[0031] The applicant found that due to the characteristics of the structure and composition of semaglutide itself, during the synthesis and cleavage process, the protective group of tryptophan is easily removed incompletely, and double peaks will appear on the analytical instrument, which has a negative impact on the purification yield. After repeated exploration by the applicant, when the crude peptide is completely dissolved, heating it in a water bath at a constant temperature of 40-45°C for 1.5-2 hours has the best effect, and can completely remove the protecting group. If the temperature is too low, the...

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Abstract

The invention relates to a method for purifying semaglutide. The preparation method comprises the following steps: heating a semaglutide aqueous solution to remove a protecting group; carrying out primary purification on a semaglutide aqueous solution through a polymer filler, carrying out gradient elution by taking ammonium bicarbonate as a phase A and acetonitrile as a phase B, and collecting a main peak sample; carrying out secondary purification on the collected sample through octaalkylsilane bonded silica gel, carrying out gradient elution by taking an ammonium dihydrogen phosphate solution as a phase A and acetonitrile as a phase B, and collecting a main peak sample; finally, carrying out salt conversion on the collected sample through octaalkylsilane bonded silica gel, and carrying out isocratic elution by using an ammonium acetate aqueous solution as a phase A and acetonitrile as a phase B; and carrying out gradient elution by using a 40-50mg / L sodium hydroxide aqueous solution as a phase A and adding 15-25% of acetonitrile of the phase A as a phase B, collecting a main peak sample, and concentrating and freeze-drying to obtain a semaglutide finished product. According to the purification method, high purity can be achieved, the purity of a finished product reaches 99%, the single impurity content is smaller than 0.2%. Meanwhile, the solubility of the finished product is good, and the sample recovery rate can reach 100%.

Description

technical field [0001] The invention relates to the technical field of medicine and chemical industry, in particular to a method for purifying semaglutide. Background technique [0002] Semaglutide is a novel GLP-1 analogue administered subcutaneously once a week. Semaglutide is a long-acting GLP-1 analogue developed by Novo Nordisk for once-weekly injection. Semaglutide is modified with short-chain PEG, and its hydrophilicity is greatly enhanced. After PEG modification, it can not only bind tightly with albumin, cover the hydrolysis site of DPP-4 enzyme, but also reduce renal excretion, prolong the biological half-life and achieve the effect of long circulation. In December 2017, the FDA officially approved the once-weekly GLP-1 hypoglycemic drug semaglutide developed by Novo Nordisk for marketing. [0003] There are many impurities in the crude product of solid-phase synthesis of semaglutide that affect the purity and yield of the sample. At present, there have been man...

Claims

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Application Information

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IPC IPC(8): C07K14/605C07K1/16C07K1/06
CPCC07K14/605Y02P20/55
Inventor 谢宇沈杰王良友张璐黄金城宋亮
Owner 苏州天马医药集团天吉生物制药有限公司
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