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A technology of cetrorelix and salt transfer, applied in the field of biological drug preparation, can solve problems such as poor salt transfer effect and trifluoroacetic acid residue, and achieve the effects of low temperature and high replacement efficiency
Active Publication Date: 2021-01-22
KAIFENG MINGREN PHARMA
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Problems solved by technology
At present, the solution concentration commonly used in cetrorelix literature is to use a rotary evaporator to evaporate part of the solvent under vacuum conditions. The process often requires heating the cetrorelix solution, which may lead to thermal decomposition of cetrorelix to produce new Impurities
In addition, in the literature, acetic acid aqueous solution-acetonitrile system is used for salt conversion, the effect of salt conversion is poor, and there may be residual trifluoroacetic acid in the finished product
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Embodiment 1
[0031] The salt conversion method of Cetrorelix of the present invention, the detailed steps of described salt conversion method are as follows:
[0032] a. Transfer 32.0g of cetrorelix crude peptide into a beaker, put into a stirring bar, add 80ml of acetonitrile solution containing 0.1% trifluoroacetic acid, stir to dissolve it, then add 720ml of 0.1% trifluoroacetic acid aqueous solution, stir Until the solution is clear, the crude peptide solution is obtained; the obtained crude peptide solution is filtered through a 0.45 μm water filter membrane, and the filtrate is collected;
[0033] b. The filtrate obtained in step a is purified by reverse-phase chromatography using a chromatographic column, and the target peak eluent is collected to obtain a cetrorelix solution;
[0034] Adopt chromatographic column to carry out the condition in reversed-phase chromatographic purification process as follows:
[0035] Rinse the preparative column with filtered purified water for 5 min...
Embodiment 2
[0047] The salt conversion method of Cetrorelix of the present invention, the detailed steps of described salt conversion method are as follows:
[0048] a. Transfer 16.0 g of cetrorelix crude peptide into a beaker, put it into a stirring bar, add 80 ml of acetonitrile solution containing 0.1% trifluoroacetic acid, stir to dissolve it, then add 720 ml of 0.1% trifluoroacetic acid aqueous solution, and stir Until the solution is clear, the crude peptide solution is obtained; the obtained crude peptide solution is filtered through a 0.45 μm water filter membrane, and the filtrate is collected;
[0049] b. The filtrate obtained in step a is purified by reverse-phase chromatography using a chromatographic column, and the target peak eluent is collected to obtain a cetrorelix solution;
[0050] Adopt chromatographic column to carry out the condition in reversed-phase chromatographic purification process as follows:
[0051] Rinse the preparative column with filtered purified water...
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Abstract
The invention discloses a salt conversion method of cetrorelix. The method comprises the following steps of: firstly, preparing a crude peptide solution from cetrorelix crude peptide, filtering by adopting a water-based filter membrane, and collecting filtrate; carrying out reversed phase chromatography purification on the obtained filtrate, and collecting target peak eluent to obtain a cetrorelixsolution; concentrating the obtained solution by adopting a reverse osmosis membrane to obtain a concentrated solution; carrying out salt conversion on the obtained concentrated solution by adoptinga C18 reversed phase chromatographic column, replacing by adopting two systems in sequence in the salt conversion process, eluting by adopting an acetic acid solution methanol system, starting to collect the eluent after a main peak appears during elution, and stopping collecting after the main peak is completely ended to obtain a cetrorelix solution; and concentrating the obtained solution by adopting the reverse osmosis membrane, transferring the concentrated mixed solution into a freeze-drying disc, and putting the freeze-drying disc into a freeze dryer for freeze-drying to obtain a cetrorelix acetate finished product. By utilizing the method to carry out salt conversion on cetrorelix, the replacement efficiency is relatively high, and the obtained product is free of trifluoroacetic acid residues.
Description
[0001] 1. Technical field: [0002] The invention belongs to the technical field of biological drug preparation methods, in particular to a method for converting cetrorelix to salt. [0003] 2. Background technology: [0004] Cetrorelix, a synthetic 10-peptide, 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. It controls the stimulation of the ovaries, prevents the premature discharge of immature follicles, and aids in conception. And can be used to treat breast and cervical cancer, endometriosis, precocious puberty, uterine fibroids, ovarian androgen excess and premenstrual syndrome. [0005] Cetrorelix Amino Acid Sequence: [0006] AC-D-2-Nal-D-4-Cpa-D-3-Pal-Ser-Tyre-D-Cit-Leu-Arg-Pro-D-Ala-NH2 [0007] At present, the separation and purification method of cetrorelix has also been publicl...
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