Ornithine aspartate injection and preparation method thereof

A technology of ornithine aspartate and injection, which is applied in the field of medicine, can solve problems such as unclear impurities, high content of main impurities, and increased risk of adverse reactions in patients, and achieve an easy-to-control effect

Active Publication Date: 2013-02-20
SHANGHAI CHENPON PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is that the quality of the preparation is not easy to control due to factors such as the high main impurity content and unclear impurities of the existing injection, which increases the risk of adverse reactions when the patient takes the medicine. Therefore, the present invention provides a Ornithine Aspartate Injection

Method used

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  • Ornithine aspartate injection and preparation method thereof
  • Ornithine aspartate injection and preparation method thereof
  • Ornithine aspartate injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The preparation of embodiment 1 main impurity acetate

[0044] The reaction formula is as follows:

[0045]

[0046] Take an appropriate amount of ornithine acetate, and add concentrated ammonia to completely dissolve it. Reflux at 100°C for 25 hours, add an appropriate amount of concentrated ammonia water every 4 hours, follow and monitor the reaction by HPLC, until the ornithine peak area normalization method in HPLC accounts for about 0.5%. At 100°C, add 0.1% activated carbon and filter. The filtrate was rotary evaporated to dryness, added methanol, cooled to 0°C, and filtered to obtain the main impurity, acetate, off-white powder. Purity greater than 99.0% by HPLC analysis, such as figure 1 shown, t R (retention time)=7.643 is the main impurity peak. The chemical characteristics of the main impurity acetate are as follows:

[0047] Molecular formula: C 7 h 14 N 2 o 3 , Melting point: 127.9~130.9℃. IR(v max cm -1 ): 3411.5, 1675.9, 1558.2, 1407.8. 1 ...

Embodiment 2

[0049] Prepare Ornithine Aspartate Injection according to the following prescription:

[0050]

[0051]

[0052] Take 500.6g of ornithine aspartate, add 600mL of water for injection, stir to dissolve, add an appropriate amount of 1% acetic acid solution to adjust the pH to 5.7, add 0.1% activated carbon for needles, heat in a water bath at 40°C for 45 minutes, Filter through a 0.45 μm filter membrane, then rinse the activated carbon filter cake with a small amount of water for injection several times, and combine the collected filtrates. Dilute the filtrate to the 1000mL mark, accurately measure 10mL and pour it into a 10mL ampoule, seal, test, check for leaks, and sterilize at 115°C for 30 minutes. Take it out, cool it down to room temperature naturally, and make ornithine-aspartate injection.

[0053] Product testing: pH=5.75; after HPLC analysis and calculation, the content of main impurities is 0.10%, and the content of related substances is 0.21%. Such as figure...

Embodiment 3

[0055] Prepare Ornithine Aspartate Injection according to the following prescription:

[0056]

[0057] Take 100.2g of ornithine aspartic acid, add 600mL of water for injection, stir to dissolve, add an appropriate amount of 1% acetic acid solution to adjust the pH to 5.4, add 0.05% activated carbon for needles, heat in a water bath at 60°C for 30 minutes, and keep warm Filter through a 0.45 μm filter membrane, then rinse the activated carbon filter cake with a small amount of water for injection several times, and combine the collected filtrates. Dilute the filtrate to the 1000mL mark, accurately measure 10mL and pour it into a 10mL ampoule, seal, test, check for leaks, and sterilize at 121°C for 15 minutes. Take it out, cool it down to room temperature naturally, and make ornithine-aspartate injection.

[0058] Product testing: pH=5.50; after HPLC analysis and calculation, the content of main impurities is 0.07%, and the content of related substances is 0.15%

[0059] S...

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Abstract

The invention relates to an ornithine aspartate injection and a preparation method thereof. The injection contains ornithine aspartate, water for injection and acid-base adjusting agent, and has the pH value of 5.2-6.0 and the concentration of 0.01-1g / mL. The ornithine aspartate injection is prepared by dissolving the ornithine aspartate by the water for injection, adjusting the pH value by the acid-base adjusting agent, discoloring by activated carbon, leading the volume to be constant, split charging and sterilizing. The injection can be used for treating hepatic encephalopathy. The injection provided by the invention has the characteristics of being less in impurity content, easy in control of quality, safer in clinical application and the like.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a pharmaceutical preparation and a preparation method thereof, in particular to an ornithine-aspartate injection and a preparation method thereof. Background technique [0002] Ornithine aspartate was first used clinically in Germany in the 1970s. It was included in the German Pharmacopoeia in 1991 and was approved by the US FDA for the treatment of hepatic encephalopathy. Aspartic Acid Ornithine Injection is my country's first clinically used new drug with three effects of liver protection, detoxification and energy. Its main therapeutic ingredients are aspartic acid and ornithine. It is clinically used in acute, The treatment of chronic liver disease, including liver cirrhosis, fatty liver and elevated blood ammonia caused by hepatitis, is especially effective for hepatic encephalopathy. Currently commonly used dosage forms are powder injections, granules, and injections. Granules are par...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/198A61K9/08A61K47/04A61K47/12A61P25/00A61P1/16
Inventor 沈莹刘晓帆杜狄峥其他发明人请求不公开姓名
Owner SHANGHAI CHENPON PHARM TECH CO LTD
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