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Triptorelin purification preparation method

A technology of step 2, solution, which is applied in the field of purification and preparation of triptorelin, can solve the problems of difficult control, low purity of crude peptide, and low purification yield, and achieve the effects of improving efficiency, high product purity, and high reaction efficiency

Inactive Publication Date: 2015-07-08
苏州天马医药集团天吉生物制药有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The purpose of the present invention is to provide a purification preparation method of triptorelin, the purification preparation method solves the problems of low purity of crude peptide, low purification yield and difficult control in the production process of the current product, the conditions are relatively mild, and the reaction efficiency is high. High, high product purity, with reduced cost, reduced risk and pollution, improved efficiency, and very suitable for large-scale production

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  • Triptorelin purification preparation method

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Embodiment 1

[0018] Embodiment 1: a kind of purification preparation method of triptorelin, comprises the following steps:

[0019] Add 800mmol of crude peptide to pure water at 25°C to dissolve, place in a water bath for 100min, stir well until completely dissolved, the solution is light yellow, clear, and free of particles;

[0020] The solution was filtered through a 0.45 μm aqueous filter membrane to remove insoluble matter to obtain a filtrate, which was purified by a 15 cm diameter silica gel reversed-phase high performance liquid phase preparative column. Purification preparation mobile phase is, A phase: 0.2% phosphoric acid aqueous solution plus tetrabutyl ammonium hydrogen phosphate, B phase: acetonitrile. The detection wavelength of the prepared mobile phase is 230nm, the flow rate is 80mL / min, the elution gradient B is from 12 to 52%, 40 minutes, the loading amount is 15g, and the samples with a purity of ≥99.0% are collected, and then detected and quantified according to HPLC ...

Embodiment 2

[0021] Embodiment 2: a kind of purification preparation method of triptorelin, comprises the following steps:

[0022] Add 1000mmol of crude peptide to pure water at 27°C to dissolve it, place it in a water bath for 93 minutes, stir well until it is completely dissolved, and the solution is light yellow, clear, and free of particles;

[0023] The solution was filtered through a 0.45 μm aqueous filter membrane to remove insoluble matter to obtain a filtrate, which was purified by a 15 cm diameter silica gel reversed-phase high performance liquid phase preparative column. Purification preparation mobile phase is, A phase: 0.2% phosphoric acid aqueous solution plus tetrabutyl ammonium hydrogen phosphate, B phase: acetonitrile. The detection wavelength of the prepared mobile phase is 230nm, the flow rate is 400mL / min, the elution gradient B is from 12 to 52%, 40 minutes, the loading amount is 15g, and the samples with a purity of ≥99.0% are collected, and then detected and quantif...

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Abstract

The invention discloses a triptorelin purification preparation method. The triptorelin purification preparation method comprises the following steps of preparing a triptorelin crude peptide solution, dissolving the triptorelin crude peptide solution in a warm water bath, and carrying out gradient elution by octadecylsilane bonded silica gel as a stationary phase, a purification mobile phase A which comprises a phosphoric acid aqueous solution with content of 0.2% and tetrabutylammonium phosphate and a phase B which is acetonitrile and has a mass percentage concentration of 12-52% in gradient elution, wherein the phosphoric acid aqueous solution with content of 0.2% is prepared from 1L of pure water, 2mL of phosphoric acid and 1mL of tetrabutylammonium phosphate, a warm water temperature is in a range of 25-28 DEG C and water bath time is in a range of 1-1.5h. The triptorelin purification preparation method solves the problem that the existing product production method produces low-purity crude peptide, has a low purification yield and cannot be controlled easily, and has the advantages of mild conditions, high reaction efficiency, high product purity, low cost, low dangerousness and pollution, high efficiency and large scale production feasibility.

Description

technical field [0001] The invention relates to the field of chemical purification of polypeptide drugs, in particular to a method for purifying and preparing triptorelin. Background technique [0002] The amino acid sequence of triptorelin is: L-pyroglutamyl-L-histidyl-L-tryptophanyl-L-seryl-L-tyrosyl-D-tryptophanyl-L-leucine Acyl-L-arginyl-L-prolyl-glycylamide. [0003] Its structure is as follows: [0004] [0005] Triptorelin is a synthetic analogue of gonadotropin-releasing hormone. Its structural modification is to replace the sixth glycine in the natural molecular structure with D-tryptophan to make it more effective. and longer plasma half-life. Triptorelin is a synthetic gonadotropin-releasing hormone analog. Triptorelin mainly acts on the anterior lobe of the pituitary gland. In the early stage of high-dose application, it can cause a transient increase in the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). secretion decreased. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/23C07K1/20
Inventor 陈逸民高鲁孙锋王良友
Owner 苏州天马医药集团天吉生物制药有限公司
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