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Gamma-cytidine-5'-disodium triphosphate crystal compound, and preparation method and drug composition of crystal compound

A technology of disodium triphosphate and cytosine nucleoside, which is applied in the field of crystallization of γ-cytosine nucleoside-5'-disodium triphosphate, and can solve the problem of undiscovered crystallization of γ-cytosine nucleoside disodium triphosphate Compounds and other problems, to achieve the effect of high crystallinity, improved solubility and stability, and simple and easy-to-control operating conditions

Active Publication Date: 2015-04-01
宁辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the applicant has not found that the crystalline compound of disodium γ-cytidine-5'-triphosphate has been prepared

Method used

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  • Gamma-cytidine-5'-disodium triphosphate crystal compound, and preparation method and drug composition of crystal compound
  • Gamma-cytidine-5'-disodium triphosphate crystal compound, and preparation method and drug composition of crystal compound
  • Gamma-cytidine-5'-disodium triphosphate crystal compound, and preparation method and drug composition of crystal compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] 4.5 g of γ-cytidine-5'-disodium triphosphate was added to 23 g of N,N-dimethylformamide solvent, and the temperature was raised to 30°C to dissolve it to obtain a transparent solution. 80 g of acetonitrile was added dropwise with stirring, and crystals were formed. Cool to 5°C at 0.2°C / min and continue stirring for 1 h. The obtained suspension was vacuum filtered, and the filter cake was vacuum-dried at 40°C to obtain 4.12 g of γ-cytosine-5'-disodium triphosphate crystals.

[0027] The XRD pattern of the product is as follows figure 1 shown. Infrared absorption spectrum such as figure 2 shown.

Embodiment 2

[0029] 3.0 g of disodium γ-cytosine-5'-triphosphate was put into 18 g of acetamide solvent, heated to 40°C, and stirred to dissolve completely. 100 g of ethyl acetate was added under continuous stirring, then cooled to 0 °C at 0.2 °C / min, and then continued to be stirred for 1 h. The suspension was filtered, and the filter cake was vacuum-dried at 50°C to obtain 2.35 g of γ-cytosine-5'-disodium triphosphate crystals.

Embodiment 3

[0031] 5.0 g of disodium γ-cytosine-5'-triphosphate was put into 30 g of N,N-dimethylacetamide solvent, heated to 50°C, and stirred to dissolve completely. 120 g of ethyl acetate were added with continuous stirring. The temperature was lowered to 10°C at 0.3°C / min, and the resulting suspension was further stirred for 0.5h. The obtained suspension was filtered and dried under vacuum at 60°C to obtain 4.51 g of γ-cytosine-5'-triphosphate disodium crystals.

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Abstract

The invention relates to a gamma-cytidine-5'-disodium triphosphate crystal, and a preparation method, a drug composition, and a drug preparation of the crystal. The solubility and the stability of the crystal are better than those of a substance in the prior art, and the crystal is more beneficial for pharmacy and long-term storage. The preparation is particularly suitable for being prepared into an injection and a powder injection.

Description

technical field [0001] The invention belongs to the technical field of drug crystallization, and in particular relates to a crystal of gamma-cytidine-5'-triphosphate disodium, a preparation method thereof, a pharmaceutical composition and a pharmaceutical preparation. Background technique [0002] The structural formula of γ-cytidine-5'-triphosphate disodium is as follows, [0003] , [0004] It belongs to nucleotide derivatives, participates in the synthesis and metabolism of nucleic acid and phospholipids in the body, and promotes protein synthesis. It can also regulate and promote the synthesis and construction of nerve cells, glial cells and blood vessel wall cell membrane structures, and can resist nerve cell damage caused by excitatory amino acids and free radicals, thereby supporting survival, enhancing activity, delaying Death, improve the ability of cells to resist damage, regeneration and repair, promote the regeneration of neurite, and improve the function of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H19/10C07H1/06A61K31/7068A61P25/00A61P9/00A61P9/04A61P1/16
Inventor 宁辉
Owner 宁辉
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