Preparation method of arginine aspirin and powder-injection of arginine aspirin

A technology of arginine aspirin and aspirin, applied in the direction of medical preparations containing active ingredients, anti-inflammatory agents, powder delivery, etc., can solve the problems of cumbersome steps, prolonged time, low crystallization temperature, etc., and achieve easy industrial production and reaction The effect of short process and high product quality

Active Publication Date: 2010-05-12
蚌埠丰原涂山制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] But the reaction temperature that method 1) adopts is too high, easily causes aspirin to hydrolyze rapidly in water, generates the free salicylic acid that is difficult to control, and the steps are particularly loaded down with trivial details, is unfavorable for suitability for industrialized production; method 2) is that aspirin is directly dissolved in aqueous ethanol In the process, it is also easy to cause rapid hydrolysis of aspirin in water to generate free salicylic acid that is difficult to control, and this reaction process is a drop-in process, which not only prolongs the time but also increases the required equipment in industrial production; in addition, the crystallization temperature is also high. Too low, increasing the production cost

Method used

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  • Preparation method of arginine aspirin and powder-injection of arginine aspirin
  • Preparation method of arginine aspirin and powder-injection of arginine aspirin
  • Preparation method of arginine aspirin and powder-injection of arginine aspirin

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Experimental program
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Effect test

Embodiment 1

[0027] Dissolve 40.0g of aspirin in 120ml of absolute ethanol, add 35.2g of arginine to react for 20 minutes at 40°C under agitation, then add 20ml of distilled water, and when the solution is clear, filter it aseptically and cool down to 29°C Insulated and stirred for 5 hours, then slowly cooled to 10°C for suction filtration, then fully washed twice with absolute ethanol, and vacuum-dried at 35°C for 6 hours to obtain 57.5 g of sterile arginine aspirin, with a total yield of about 75.2%. And the product quality fully complies with the national standard. Then the aspirin arginine aspirin powder for injection can be obtained by aseptic subpackaging.

[0028] The obtained arginine aspirin powder injection is detected, and the results are shown in Table 1:

[0029] The detection result of table 1 embodiment 1

[0030] Loss on drying

Embodiment 2

[0032] Dissolve 80g of aspirin in 400ml of absolute ethanol, add 77.3g of arginine at 30°C to react for 30 minutes under stirring conditions, then add 44ml of distilled water, after the solution is clarified, filter it aseptically, cool down to 25°C and keep stirring 6 hours, then slowly cool down to 8°C for suction filtration, then fully wash twice with absolute ethanol, and vacuum-dry at 35°C for 8 hours to obtain 122.2g of sterile arginine aspirin, with a total yield of about 77.7%, and the product The quality is in full compliance with national standards. Then the aspirin arginine aspirin powder for injection is obtained through aseptic subpackaging.

[0033] The obtained arginine aspirin powder injection is detected, and the results are shown in Table 2:

[0034] The detection result of table 2 embodiment 2

[0035] Loss on drying

Embodiment 3

[0037] Dissolve 60g of aspirin in 480ml of absolute ethanol, add 55.2g of arginine at 30°C to react for 40 minutes while stirring 8 hours, then slowly cool down to 5°C and filter with suction, then fully wash the crystals 3 times with absolute ethanol, and dry in vacuum at 30°C for 8 hours to obtain 93.3g of sterile arginine aspirin, with a total yield of about 81.0%, and Product quality is in full compliance with national standards. Then the aspirin arginine aspirin powder for injection is obtained through aseptic subpackaging. The obtained arginine aspirin powder injection is detected, and the results are shown in Table 3:

[0038] The detection result of table 3 embodiment 3

[0039] Loss on drying

[0040] Obviously, the content of free salicylic acid in the powder injection prepared by the method of the present invention is very low, the content of active ingredients is high, the weight loss on drying is low, and the stability is strong.

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Abstract

The invention relates to a preparation method of arginine aspirin and powder-injection of arginine aspirin. The preparation method of arginine aspirin comprises the following steps: 1) dissolving aspirin in absolute alcohol, adding arginine power at 30-40 DEG C to react; 2) adding distilled water to ensure the solution to be transparent, performing sterile filtration; 3) reducing temperature for crystallization, filtrating; and 4) drying to obtain sterile arginine aspirin, and then performing sterile subpackage of the sterile arginine aspirin to obtain the powder-injection of arginine aspirin. Compared with the prior art, the preparation method of the invention has short reaction process and simple operation, the reaction temperature is not high, the method is applicable to industrialized production; and the reaction yield is high, the product quality is good (especially the content of free salicylic acid is low), and the stability is good.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of arginine aspirin and its powder injection. Background technique [0002] Arginine aspirin is a double salt of aspirin and arginine, also known as aspirin arginine salt, which can inhibit cyclooxygenase, reduce the synthesis of prostaglandins, and has antipyretic, analgesic and anti-inflammatory effects. Arginine aspirin not only maintains the original efficacy of aspirin, but also changes its water-insoluble properties to make it have good water solubility, so that this old anti-rheumatic and analgesic drug can be made into injections, which not only reduces the dosage , and more rapid-acting, so far, arginine aspirin has become a new painkiller that is more convenient to use. [0003] At present, the production methods of domestic arginine aspirin mainly contain the following two kinds: [0004] 1) Dissolve arginine in water, add aspirin, stir to make...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C279/14C07C69/157A61K31/616A61K9/14A61P29/00
Inventor 候飞汪洪湖
Owner 蚌埠丰原涂山制药有限公司
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