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Carbazochrome sodium sulfonate compound and composition thereof

A technology of sodium carbosulfonate and compounds, applied in the field of medicine, to achieve the effect of reducing the possibility, simplifying the prescription, and improving the stability

Active Publication Date: 2012-10-10
江西璟瑞药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Patent application 200710191009.5 discloses a freeze-dried powder injection of sodium carbosulfonate and its preparation method, which is characterized by adding thiourea and / or sodium formaldehyde sulfoxylate, mannitol, excipients, etc. to solve the problem of sodium carbosulfonate However, due to the addition of non-pharmaceutical grade excipients in the prescription, unpredictable safety risks may occur in clinical injection use

Method used

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  • Carbazochrome sodium sulfonate compound and composition thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] The sodium carnosulfonate of the present invention is prepared by the following method:

[0052] (1) Take the crude sodium carnosulfonate, add water with a volume of 4.5 times the weight of the crude sodium carnosulfonate, stir, and gradually increase the temperature from room temperature to 80°C;

[0053] (2) After the crude sodium carbsulfonate is fully dissolved, add 0.3 times the amount of active carbon of the crude sodium sulfonate to decolorize and filter;

[0054] (3) Add dropwise to the filtrate a volume of 4.5 times the weight of the crude sodium carnosulfonate and a 16:1 ethanol:chloroform mixed solution; the mixed solution is dripped at a uniform speed within 16 minutes at a stirring speed of 12rpm, While dripping, the temperature of the filtrate was reduced to 12°C at a rate of 1°C / min;

[0055] (4) Stop stirring, cool the solution to 3°C within 10 minutes, leave it to stand for 24 hours, filter, wash twice with 6 times the amount of 70% ethanol aqueous solution, an...

Embodiment 2

[0058] (1) Take the crude sodium carnosulfonate, add water whose volume is 3 times the weight of the crude sodium carnosulfonate, stir, and gradually increase the temperature from room temperature to 75℃;

[0059] (2) After the crude sodium carbsulfonate is fully dissolved, add 0.2 times the amount of activated carbon of the crude sodium sulfonate to decolorize and filter;

[0060] (3) Add dropwise to the filtrate a mixture solution of ethanol:chloroform with a volume ratio of 3 times the weight of the crude sodium carnosulfonate and a volume ratio of 15:1; the mixed solution is dripped at a uniform speed within 8 minutes at a stirring speed of 8rpm, While dripping, the temperature of the filtrate was reduced to 10°C at a rate of 0.5°C / min;

[0061] (4) Stop stirring, cool the solution to 0°C within 5 minutes, leave it to stand for 18 hours, filter, wash twice with 4 times the amount of 60% ethanol aqueous solution, and dry to obtain the sodium calcinate. The yield was 82.9%, and th...

Embodiment 3

[0064] (1) Take the crude sodium carnosulfonate, add water with a volume of 6 times the weight of the crude sodium carnosulfonate, stir, and gradually increase the temperature from room temperature to 85°C;

[0065] (2) After the crude sodium carbsulfonate is fully dissolved, add 0.5 times the amount of active carbon of the crude sodium sulfonate to decolorize and filter;

[0066] (3) To the filtrate, add dropwise a volume of 6 times the weight of the crude sodium carnosulfonate to an ethanol:chloroform mixed solution with a volume ratio of 18:1; the mixed solution is dripped at a uniform speed within 24 minutes at a stirring speed of 16rpm, While dripping, cool the filtrate to 15℃ at a rate of 1.5℃ / min;

[0067] (4) Stop stirring, cool the solution to 5°C within 15 minutes, leave it to stand for 36 hours, filter, wash twice with 8 times the amount of 80% ethanol aqueous solution, and dry to obtain the sodium sulphonate. The yield was 83.4%, and the HPLC content was 99.76%.

[0068] ...

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Abstract

The invention relates to a carbazochrome sodium sulfonate compound and a composition thereof. The carbazochrome sodium sulfonate compound is measured by a powder X-ray diffraction measurement method; and the diffraction angle of 2 theta + / - 0.2 degrees can be used for showing that an X-ray powder diffraction pattern has characteristic diffraction peaks at the parts including 10.23 degrees, 12.12 degrees, 18.39 degrees, 22.32 degrees, 24.79 degrees, 26.23 degrees, 28.60 degrees, 30.25 degrees, 31.98 degrees, 33.32 degrees, 34.32 degrees and 36.02 degrees. The carbazochrome sodium sulfonate compound provided by the invention has the remarkably improved stability and does not change after being placed for a long time, so that the drug safety of patients can be greatly improved.

Description

Technical field [0001] The present invention relates to the field of medicine, in particular to a sodium carnosulfonate compound and a composition thereof. Background technique [0002] Carbazochrome Sodium Sulfonate is a chemical derivative of Adrenochrome. Its chemical name is: 1-methyl-6-oxo-2,3,5,6-tetrahydroindole-5-semicarbazone-2-sulfonic acid sodium salt trihydrate. Its structure was first reported in Japan in the 1970s. The main reason for its appearance was to improve the poor water solubility of Anluoxue and the adverse reactions that occurred when a large amount of salicylic acid was added to aid dissolution. These chemicals can reduce the permeability of capillaries and enhance the retraction of the broken ends of capillaries. They are often used for various bleeding caused by increased capillary permeability. At present, domestic medicine is clinically used for bleeding in urinary system, upper digestive tract, respiratory tract and obstetrics and gynecology disea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/30A61K31/404A61P7/04
Inventor 夏智红
Owner 江西璟瑞药业有限公司
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