Separation and purification method of cetrorelix

A technology for separation and purification of cetrorelix, applied in the field of drug purification, can solve the problems of complicated operation, reduced yield, many process steps, etc., and achieve the effects of high purity, stable yield and less mobile phase

Active Publication Date: 2018-03-06
SUZHOU NANOMICRO TECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

CN201510332163.4 provides a synthetic method of cetrorelix, which describes separation and purification using C18 or C8 reverse-phase column chromatography, the mobile phase is 0.05%-0.5% aqueous solution of hydrochloric acid or phosphoric acid or trifluoroacetic acid and acetonitrile solution, After the peaks of the sample are merged, the salt is transferred, but this method has many steps, resulting in complicated operation and low yield

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  • Separation and purification method of cetrorelix
  • Separation and purification method of cetrorelix
  • Separation and purification method of cetrorelix

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Embodiment 1

[0029] Take the crude extract of cetrorelix with a purity of 95.46%, add 1% acetic acid, dissolve, add water, add acetonitrile, and the content of cetrorelix in the solution is 10 mg / mL. After the solution was clarified, it was filtered through a filter membrane with a pore size of 0.45 μm, and the filtrate was collected for later use. A chromatographic column of 4.6×250 mm was used, and UniSil C18 or C8 microspheres (manufactured by Suzhou Nawei Technology Co., Ltd.) were used as the packing material of the chromatographic column, and the packing volume was 4.2 ml. Perform pre-column pretreatment on the chromatographic column, first use a high-concentration organic phase to remove impurities, and then use an organic phase with a concentration lower than 20% to balance. Then 1% acetic acid aqueous solution (phase A) and acetonitrile (phase B) were used as mobile phases for gradient elution, and the flow rate was controlled at 1 ml / min. The gradient elution process is as follo...

Embodiment 2

[0032] Take the crude extract of cetrorelix with a purity of 95.46%, add 1% acetic acid, dissolve, add water, add acetonitrile, and the content of cetrorelix in the solution is 10 mg / mL. After the solution was clarified, it was filtered through a filter membrane with a pore size of 0.45 μm, and the filtrate was collected for later use. A chromatographic column of 4.6×250 mm was used, and UniSil C18 or C8 microspheres (manufactured by Suzhou Nawei Technology Co., Ltd.) were used as the packing material of the chromatographic column, and the packing volume was 4.2 ml. Pre-column pretreatment was performed on the chromatographic column, and 1% acetic acid aqueous solution (phase A) and acetonitrile (phase B) were used as mobile phases for gradient elution, and the flow rate was controlled at 1 ml / min. The gradient elution process is as follows: first wash with 10% phase B for 8 minutes, then elute with 23% phase B, collect the solution of the target peak in sections, summarize th...

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Abstract

The invention provides a method for efficiently separating and purifying cetrorelix. The method comprises the following steps: dissolving and filtering a crude cetrorelix extract; applying a filteredsolution to a chromatographic column with uniform-particle reverse-phase silica gel, and performing chromatography; eluting a target product by using an aqueous acetic acid solution and an organic solvent as a mobile phase; sectionally collecting solutions with target peaks, and combining component solutions which meet requirements. The method is used for deeply purifying the cetrorelix; by only one chromatographic purification step, a requirement that the any individual impurity content of the cetrorelix is lower than 0.1% can be met; the purification yield is high and stable; moreover, the separation method is simple and convenient and can be applied to large-scale production, and the production cost is greatly reduced.

Description

technical field [0001] The invention relates to the field of medicine purification, in particular to a method for efficiently separating and purifying cetrorelix. Background technique [0002] Cetrorelix is ​​a luteinizing hormone releasing hormone (LHRH) antagonist. LHRH can bind to membrane receptors of pituitary cells. Cetrorelix competes with endogenous LHRH for binding to these receptors, thereby controlling gonadotropin secretion. Cetrorelix can always rely on the secretion of sex hormones through the hypothalamus-pituitary-gonad pathway, so as to achieve the purpose of indirectly inhibiting cancer growth or preventing, alleviating, and treating other diseases. It can be used for the treatment of hormone-sensitive prostate cancer and breast cancer and Some benign gynecological conditions (endometriosis, fibroids and thinning of the endometrium). Compared with GNRH agonists, cetrorelix has the advantages of shorter course of treatment, fewer adverse reactions, and ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/23C07K1/16
CPCC07K7/23
Inventor 江必旺毕士峰邓杰
Owner SUZHOU NANOMICRO TECH CO LTD
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