Acetylglutamine compound and pharmaceutical composition thereof

An acetoglutamine and compound technology, applied in the field of acetoglutamine compounds and pharmaceutical compositions thereof, can solve the problems of limiting the practical application of acetoglutamine preparations, reducing the yield of acetoglutamine, being unable to carry out industrialized production, etc., and achieving stable properties. , not easy to hydrolysis and oxidation, the effect of improving yield

Active Publication Date: 2011-12-14
周晓东
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the strict control of the process parameters not only increases the operating cost, but also has poor reproducibility of the operating process, so that the above method cannot be industrialized, which limits the practical application of acetylglutamine preparations
[0009] In addition, it is well known that activated carbon is required for decolorization during the preparation of injections. In the methods disclosed in the above-mentioned documents, activated carbon has a certain adsorption effect on acetylglutamine, thereby reducing the yield of acetylglutamine and improving pharmaceutical costs.

Method used

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  • Acetylglutamine compound and pharmaceutical composition thereof
  • Acetylglutamine compound and pharmaceutical composition thereof
  • Acetylglutamine compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] [Example 1] Preparation of Acetylglutamine Compound

[0054] 1) dissolving acetylglutamine powder in water to obtain solution 1;

[0055] 2) Under stirring, add ethanol dropwise to solution 1, the volume ratio of the amount of ethanol added to the water in solution 1 is 1:5-1:10 to obtain suspension 2;

[0056] 3) Suspension 2 is filtered, the filter cake is washed with ethanol, and dried to obtain the acetylglutamine compound.

[0057] The particle diameter of the prepared acetylglutamine compound is 170 μm, and the X-ray powder diffraction pattern (see figure 1 ) in the characteristic peaks at 2θ of 9.3, 11.2, 14.6, 17.0, 20.9 show. The melting point is 150-152°C.

Embodiment 2

[0058] [embodiment 2] the preparation of acetylglutamine compound

[0059] 1) Dissolve 120g of acetylglutamine powder in 20ml of water to obtain solution 1;

[0060] 2) Under stirring at 1200 rpm, add 70ml of ethanol dropwise to solution 1 at a rate of 1.5ml / min. During the dropwise addition, the temperature of solution 1 is controlled at 25°C to obtain suspension 2. After the addition of ethanol is completed, continue to stir the suspension for 24 Hour;

[0061] 3) Suspension 2 was filtered, the filter cake was washed with ethanol, and vacuum-dried under reduced pressure at 25° C. for 18 hours to obtain the acetylglutamine compound.

[0062] The obtained acetylglutamine compound has a particle size of 180 μm and a melting point of 150-152° C. The X-ray powder diffraction pattern obtained by Cu-K α-ray measurement is consistent with that of Example 1.

Embodiment 3

[0063] [Example 3] Preparation of Acetylglutamine Compound

[0064] 1) Dissolve 40g of acetylglutamine powder in 20ml of water to obtain solution 1;

[0065] 2) Under stirring at 1000 rpm, add 50ml of ethanol dropwise to solution 1 at a rate of 1.0ml / min. During the dropwise addition, the temperature of solution 1 is controlled at 30°C to obtain suspension 2. After the addition of ethanol is completed, continue to stir suspension 2 3.5 hours;

[0066] 3) Suspension 2 was filtered, the filter cake was washed with ethanol, and vacuum-dried under reduced pressure at 20° C. for 12 hours to obtain the acetylglutamine compound.

[0067] The obtained acetylglutamine compound has a particle size of 160 μm and a melting point of 151-153° C. The X-ray powder diffraction pattern obtained by Cu-K α-ray measurement is consistent with that of Example 1.

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Abstract

The invention discloses an aceglutamide compound. The aceglutamide compound is crystals; and characteristic peaks in an X-ray powder diffraction pattern measured by using Cu-K alpha rays are displayed as 9.3, 11.2, 14.6, 17.0 and 20.9 at 2 theta. The aceglutamide compound has the advantages of uniform particle size and steady characteristic, and cannot be hydrolyzed and oxidized easily, so that the aceglutamide compound can be used for preparing a medicinal composition. The invention also discloses the medicinal composition. The medicinal composition contains the aceglutamide compound and a pharmaceutically acceptable carrier, an excipient or a diluent; and the optimal formulation is freeze-dried powder injection or injection. The medicinal composition has the advantages of stable qualityand high yield, and the preparation process is simple, so that the period of validity of the medicine is prolonged, and the quality of the product is guaranteed.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an acetylglutamine compound and a pharmaceutical composition thereof. Background technique [0002] Acetyl glutamine, also known as acetate glutamine or amide glutaric acid amine acetate glutamine, chemical name: N-acetyl-L-glutamine, its physical and chemical properties are: white crystalline powder, odorless, tasteless, soluble In water, slightly soluble in ethanol. [0003] Acetylglutamine is a central nervous system stimulant, which can directly enter the central nervous system through the blood-brain barrier, participate in the information transmission of the central nervous system, improve nerve cell metabolism, increase cell vitality, maintain nerve stress ability, and improve brain function. Therefore, acetylglutamine can assist in the treatment of symptoms such as memory loss in the elderly, memory loss after cerebrovascular disease, and senile brain functi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C237/22C07C231/24A61K31/16A61P25/28
Inventor 周晓东
Owner 周晓东
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