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Novel active cytidine disodium triphosphate compound and pharmaceutical composition thereof

A technology of disodium cytidine triphosphate and disodium cytidine phosphate, which is applied in the field of medicine, can solve the problems of further improvement in stability, achieve the effects of improved stability, simple prescription, and guaranteed drug safety

Active Publication Date: 2012-10-31
南城第二医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The pH of the resulting product of the invention is acidic, and the stability needs to be further improved

Method used

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  • Novel active cytidine disodium triphosphate compound and pharmaceutical composition thereof
  • Novel active cytidine disodium triphosphate compound and pharmaceutical composition thereof
  • Novel active cytidine disodium triphosphate compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Preparation of cytidine triphosphate disodium compound

[0041] (1) Dissolve the crude product of cytidine disodium triphosphate in water to obtain a 0.25 g / ml aqueous solution of cytidine disodium triphosphate;

[0042] (2) Heat the aqueous solution of cytidine disodium triphosphate to 55°C, and add ethanol dropwise thereto at a stirring speed of 16rmp until the solution becomes turbid;

[0043] (3) Continue to stir into the solution and add a mixed solution of diethyl ether: chloroform whose volume is 4 times the weight of the crude product of cytidine triphosphate and whose volume ratio is 16:1; At the same time, the solution was cooled to 12°C at a rate of 3°C / min;

[0044] (4) Stop stirring, cool down the solution to 3°C within 25 min, let stand to grow crystals for 24 hours, filter, wash twice with 3 times the amount of ether, and dry to obtain the cytidine triphosphate disodium compound.

[0045] The described cytidine triphosphate disodium compound i...

Embodiment 2

[0046] Example 2 Preparation of cytidine triphosphate disodium compound

[0047] (1) Dissolve the crude product of cytidine disodium triphosphate in water to obtain a 0.05 g / ml aqueous solution of cytidine disodium triphosphate;

[0048] (2) Heat the aqueous solution of cytidine disodium triphosphate to 45°C, and add ethanol dropwise thereto at a stirring speed of 12 rpm until the solution becomes turbid;

[0049] (3) Stir and drop into the solution a mixed solution of diethyl ether: chloroform whose volume is twice the weight of the crude product of cytidine triphosphate and whose volume ratio is 12:1; the mixed solution is dripped at a constant speed within 10 minutes at a stirring speed of 5 rpm After the solution is added dropwise, the solution is cooled to 10°C at a rate of 2°C / min;

[0050] (4) Stop stirring, cool down the solution to 0°C within 20 minutes, let the crystal grow for 16 hours, filter, wash twice with 2 times the amount of ether, and dry to obtain the cytidi...

Embodiment 3

[0052] Example 3 Preparation of cytidine triphosphate disodium compound

[0053] (1) Dissolve the crude product of cytidine disodium triphosphate in water to obtain a 0.5 g / ml aqueous solution of cytidine disodium triphosphate;

[0054] (2) Heat the aqueous solution of cytidine disodium triphosphate to 60°C, and add ethanol dropwise thereto at a stirring speed of 20rmp until the solution becomes turbid;

[0055] (3) Continue to stir and add a mixed solution of diethyl ether: chloroform with a volume ratio of 20:1 whose volume is 6 times the weight of the crude cytidine disodium triphosphate; After the flow is added, the solution is cooled to 15°C at a speed of 4°C / min;

[0056] (4) Stop stirring, cool down the solution to 5°C within 35 minutes, let the crystal grow for 32 hours, filter, wash twice with 6 times the amount of ether, and dry to obtain the cytidine triphosphate disodium compound.

[0057] The described cytidine triphosphate disodium compound is measured by powde...

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Abstract

The invention relates to a novel active cytidine disodium triphosphate compound and a pharmaceutical composition thereof. The powder X-ray diffraction determination method indicates that the cytidine disodium triphosphate compound has feature diffraction peaks at 7.43 degrees, 9.88 degrees, 12.52 degrees, 14.92 degrees, 16.37 degrees, 19.58 degrees, 21.88 degrees, 23.57 degrees, 25.26 degrees, 30.69 degrees, 33.05 degrees and 34.32 degrees in the X-ray powder diffractogram represented as the diffraction angle 2theta+ / -0.2 degrees. The cytidine disodium triphosphate compound provided by the invention has obviously higher stability, and can not change after being stored for a long time, thereby greatly enhancing the medication security of the patient.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a new active cytidine triphosphate disodium compound and its pharmaceutical composition. Background technique [0002] Cytidine triphosphate disodium is a nucleotide derivative that participates in the synthesis and metabolism of phospholipids in the body. It can pass through the blood-cerebrospinal fluid barrier. It is the intermediate product and energy source of cephalin synthesis and nucleic acid metabolism. It can also improve the stability and reconstruction ability of the membrane structure of nerve cells, support the survival of nerve cells, delay cell aging and death, and improve the quality of nerve cells. Anti-injury ability, promote neurite outgrowth. This product can effectively prevent nerve cell injury or secondary death after ischemia, stabilize liver cell membrane, promote repair of liver cell after injury, nourish, promote regeneration and repair of myocardium and brain...

Claims

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Application Information

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IPC IPC(8): C07H19/20A61K9/19A61K31/7068A61P1/16A61P9/10A61P25/00
Inventor 夏智红
Owner 南城第二医院
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