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Goserelin purification method

A purification method and volume ratio technology are applied in the field of purification of goserelin, which can solve problems such as difficult to obtain medicine, and achieve the effects of simple and feasible operation, high yield and high purity.

Inactive Publication Date: 2013-01-09
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Existing technologies such as patent CN101759777A relate to content related to the purification of goserelin, but its process can only reach 98.5%, let alone less than 0.1% of simple impurities; as a new drug for the treatment of prostate cancer (it is listed in the European Pharmacopoeia EP stipulates that the simple impurity should be less than 0.5%. Considering factors such as its stability and validity period, its purification process must meet the standard of being able to obtain a simple impurity of less than 0.1%, otherwise it will be difficult to make a drug

Method used

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Experimental program
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Embodiment 1

[0027] 1. Pre-treatment: Dissolve the crude peptide with 20% acetic acid and 40% methanol aqueous solution at a concentration of 100g / L by volume, stir to dissolve the sample completely, filter it with a filter membrane, and collect the filtrate. Dilute the volume ratio of acetic acid and methanol in the crude peptide solution to below 20% with water for use.

[0028] 2. Purification:

[0029] Purification conditions: Chromatographic column: a chromatographic column with octadecylsilane bonded silica gel as the stationary phase, the diameter and length of the column: 5 cm × 25 cm. Mobile phase: A phase: 0.3% phosphoric acid aqueous solution (v / v), adjust the pH value to 6.5 with triethylamine; B phase: acetonitrile, flow rate: 50-100 ml / min, gradient: B%: 20% ~ 40%, Detection wavelength: 280 nm. The injection volume is 1.0-2.5g.

[0030] Purification process: Rinse the chromatographic column with acetonitrile with a volume ratio of more than 50%, and then equilibrate and lo...

Embodiment 2

[0033] 1. Pre-treatment: Dissolve the crude peptide with 5% acetic acid and 40% methanol aqueous solution at a concentration of 100g / L by volume, stir to dissolve the sample completely, filter it with a filter membrane, and collect the filtrate. Dilute the volume ratio of acetic acid and methanol in the crude peptide solution to below 20% with water for use.

[0034]2. Purification:

[0035] Purification conditions: Chromatographic column: a chromatographic column with octadecylsilane bonded silica gel as the stationary phase, the diameter and length of the column: 15 cm × 25 cm. Mobile phase: A phase: 0.2% sulfuric acid aqueous solution (v / v), adjust the pH value to 6.0 with ammonia water; B phase: acetonitrile, flow rate: 300-600 ml / min, gradient: B%: 20% ~ 40%, detection wavelength : 280 nm. The injection volume is 1.0-2.5g.

[0036] Purification process: Rinse the chromatographic column with acetonitrile with a volume ratio of more than 50%, and then equilibrate the sam...

Embodiment 3

[0039] 1. Pretreatment: Dissolve the crude peptide with 5% acetic acid and 15% methanol aqueous solution at a concentration of 100g / L by volume, stir to dissolve the sample completely, filter it with a filter membrane, and collect the filtrate. Dilute the volume ratio of acetic acid and methanol in the crude peptide solution to below 20% with water for use.

[0040] 2. Purification:

[0041] Purification conditions: Chromatographic column: a chromatographic column with octadecylsilane bonded silica gel as the stationary phase, the diameter and length of the column: 30 cm × 25 cm. Mobile phase: A phase: 0.1% phosphoric acid and 0.2% acetic acid aqueous solution (v / v), adjust the pH value to 6.5 with ammonia water; B phase: acetonitrile, flow rate: 2000-4000 ml / min, gradient: B%: 20%~40 %, detection wavelength: 280 nm. The injection volume is 80-200g.

[0042] Purification process: Rinse the chromatographic column with acetonitrile with a volume ratio of more than 50%, and th...

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Abstract

The invention provides a goserelin purification method including the steps: 1) dissolving crude peptide in water solution of acetic acid in the volume ratio of 5%-20% and methanol in the volume ratio of 15%-40% according to the concentration of 50g / L-100g / L so that crude peptide solution is obtained; 2) using octadecylsilane chemically-bonded silica as an immobile phase, performing sample injection for the crude peptide solution, using saline water solution with the volume by volume concentration of 0.1%-0.8% and the pH (potential of hydrogen) value of 4.0-7.5 as an A phase, using acetonitrile with the volume by volume concentration of 10%-50% as a B phase, and performing gradient elution so that goserelin is obtained; and 3) converting non-acetate of the goserelin to acetate by reversed-phase high-performance liquid chromatography. The goserelin purification method is simple to operate, high in yield and purity and beneficial to realization of industrialization.

Description

technical field [0001] The invention relates to a method for purifying polypeptides, in particular to a method for purifying goserelin. Background technique [0002] The molecular formula of goserelin is: Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH 2 , the chemical structural formula is: [0003] [0004] Goserelin has a good therapeutic effect on male prostate cancer and female breast cancer. At present, the commonly used tumor drugs are mainly chemical drugs. Due to the large response to chemotherapy, it is the general trend to find a suitable biological drug. At present, the better one is gonadotropin-releasing hormone analog (LHRH-a). Long-term and large-scale application of LHRH-a not only It will not cause excessive secretion of gonadotropin, but will inhibit the release of gonadotropin from the pituitary gland. LHRH-a will start to increase the testosterone produced by Leydig cells for about 3 to 5 months, and then decrease for 21 to 28 days to reach the...

Claims

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Application Information

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IPC IPC(8): C07K7/23C07K1/20
Inventor 赵忠卫潘俊锋马亚平袁建成
Owner HYBIO PHARMA
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