Thymalfasin compound and novel preparation method thereof

A thymus method and compound technology, applied in the field of medicine, can solve problems such as not being suitable for direct use, reducing the content of active ingredients of the drug, and high cost, and achieve the effect of improving clinical adverse reactions

Inactive Publication Date: 2012-08-01
灵康药业集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] It can be seen that the methods in the prior art have many steps and are not suitable for industrial production; or the yield is low, a large amount of raw materials are consumed, resulting in high costs, or toxic solvents are used, resulting in toxic residues of the drug, which affects the preparation products quality
[0007] In addition, although the highest purity of thymus fasin currently obtained can reach 99.6% or even higher, this can only be obtained through special purification methods. The purity of ...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: Refined thymus method

[0047] Take 10 g of Thymus Farsin crude product treated according to the method of CN 1390853A, and its HPLC purity is 94.52%. Dissolve it in 60ml of trifluoroacetic acid, stir to make it completely dissolved, add 20ml of pH 2.0 mixed buffer solution of sodium dihydrogen phosphate and ammonium acetate, then add 0.4g of activated carbon, stir and adsorb at 12°C for 15 minutes, filter to remove Remove gac, collect filtrate, concentrate under reduced pressure at 0.05-0.08Mpa;

[0048] Then the concentrated solution is added to the upper end of the preparative neutral alumina chromatographic column, the stationary phase filler is particle diameter 18-53 μm, ICN alluminaN neutral alumina with a pore diameter of 6nm, pH 7.5, with sodium dihydrogen phosphate buffer (dihydrogen phosphate 9.5 grams of sodium, add 1600 milliliters of water to dissolve, adjust pH to 4.0 with 1mol / L sodium hydroxide solution, add water to 2000ml)-acetonitrile (...

Embodiment 2

[0050] Example 2: Refined thymus method

[0051] Take 10g of Thymofaxin API (manufactured by Suzhou Tianma Pharmaceutical Group Tianji Biopharmaceutical Co., Ltd., batch number 0281011001), and its HPLC purity is 97.52% after testing. Dissolve it in 100ml of ethanol, stir to dissolve it completely, add 30ml of pH 3.0 mixed buffer solution of sodium dihydrogen phosphate and ammonium acetate, then add 0.5g of activated carbon, stir and adsorb at 10°C for 20 minutes, filter to remove the activated carbon , collect the filtrate, concentrate under reduced pressure at 0.05-0.07Mpa;

[0052] Then the concentrated solution is added to the upper end of the preparative neutral alumina chromatographic column, and the stationary phase filler is a particle diameter of 50-200 μm, a special neutral alumina for Baker column chromatography with a pore diameter of 6 nm, and sodium dihydrogen phosphate buffer solution (dihydrogen phosphate 9.5 grams of sodium, add 1600 milliliters of water to...

Embodiment 3

[0054] Example 3: Refined thymus method

[0055] Get 10g expired thymus method new bulk drug, its HPLC purity is 91.52% after testing. Dissolve it in 120ml of trifluoroacetic acid, stir to dissolve it completely, add 50ml of pH 3.5 mixed buffer solution of sodium dihydrogen phosphate and ammonium acetate, then add 0.8g of activated carbon, stir and adsorb at 5°C for 15 minutes, filter to remove Remove activated carbon, collect filtrate, concentrate under reduced pressure at 0.04-0.05Mpa;

[0056] Then the concentrated solution is added to the upper end of the preparative chromatographic column, the stationary phase filler is particle diameter 18-32 μm, ICN alluminaN neutral alumina with a pore diameter of 6nm, pH 7.2, with sodium dihydrogen phosphate buffer (9.5 grams of sodium dihydrogen phosphate, Add 1600 ml of water to dissolve, adjust pH to 4.0 with 1mol / L sodium hydroxide solution, add water to 2000ml)-acetonitrile (80:20) as mobile phase A, use sodium dihydrogen phos...

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PUM

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Abstract

The invention discloses a thymalfasin compound prepared by the following processing steps: dissolving a thymalfasin crude product in an alcohol solvent or trifluoroacetic acid, adding a buffer solution at the pH of 2.0-4.0, adding activated carbon to perform adsorption, filtering, collecting filtrate, and carrying out decompression concentration; utilizing a preparation type neutral alumina chromatographic column to perform separating purification to the concentrated solution, collecting eluent, sequentially using a plate frame and a filter membrane to perform filtration, utilizing an ultrafiltration membrane to perform ultrafiltration concentration of the filtrate, and obtaining secondary concentrated solution; slowing adding ethyl ether into the obtained concentrated solution, mixing, performing gradient cooling, precipitating thymalfasin, performing centrifuged washing to the precipitated thymalfasin, and obtaining the purified thymalfasin after drying through a solid drier. The thymalfasin obtained by the method is high in purity, toxic and side effects of prepared medicines for curing chronic hepatitis B and illness causing damage of various immunity functions in the using process are reduced, product quality of a preparation is improved, and the thymalfasin is suitable for industrial mass production.

Description

technical field [0001] The invention relates to a novel thymus compound and a new preparation method thereof, through which high-purity thymus farsin can be obtained, and belongs to the technical field of medicine. Background technique [0002] Thymosin α1 (Thymosin α1, also known as thymosin α1) is the main biologically active component of thymosin, an important immunomodulatory substance in the body, a polypeptide composed of 28 amino acids acetylated at the nitrogen end, calculated as a dry product, containing thymosin α1 (C 129 h 215 N 33 o 55 ) is not less than 95.0%. Studies have shown that thymus fasin promotes the development and differentiation of bone marrow stem cells into pro-lymphocytes and pro-lymphocytes; induces the differentiation and maturation of T lymphocytes, and further differentiates mature T cells into several different subgroups, such as killer cells and memory cells , effector cells, counseling T lymphocytes, etc., and produce various soluble m...

Claims

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Application Information

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IPC IPC(8): C07K14/575C07K1/22C07K1/16A61K38/22A61P1/16A61P37/02
Inventor 陶灵刚赵雁鸿
Owner 灵康药业集团股份有限公司
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