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Carbazochrome sodium sulfonate compound and medical composition thereof

A technology of sodium carbosulfonate and compounds, applied in the field of medicine, can solve problems such as high process requirements, increased addition, unstable pH value, etc., and achieve the effects of simple prescription process, improved stability, and improved safety and effectiveness

Active Publication Date: 2013-06-12
HUNAN WUZHOUTONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The feature of this application is that it discloses a new crystal form of sodium carbosulfonate. However, we found in the test that although the content stability of the sodium carbosulfonate compound prepared by this application has been improved, the insoluble particles are relatively high and unstable. Rapid increase and unstable pH
[0008] In the existing technical solutions represented by the above-mentioned technical solutions, in order to overcome the unstable problem of sodium carbosulfonate, relatively complicated preparation techniques are generally adopted or more excipients are added or new drug crystal forms are developed. These techniques generally The process requirements are high, the addition increases the cost and unsafe factors, or the quality improvement is not comprehensive, thus limiting the use of carbosulfonium sodium preparations

Method used

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  • Carbazochrome sodium sulfonate compound and medical composition thereof
  • Carbazochrome sodium sulfonate compound and medical composition thereof
  • Carbazochrome sodium sulfonate compound and medical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] ① Dissolve the crude sodium carbosulfonate in a mixed solution of water and methanol with a volume ratio of 15:1 at 65°C and a stirring speed of 100 rpm at a weight ratio of 1:6; Activated carbon with 2% crude product weight, stirred at 100 rpm for 20 minutes, filtered to remove carbon, and filtered the filtrate through a 0.22 μm filter membrane; ③ Cool down to 60 °C at 0.2 °C / min, and stir at a stirring speed of 150 rpm While adding ethanol with a weight of 1 / 20 of the mixture of middle water and methanol at a speed of 15ml / min, stir for 30 minutes; ① A mixed solution of ethanol, methanol and chloroform with a volume ratio of 4 times of the water and methanol mixture is 10:5:1; at the same time, the temperature is lowered to 8°C at 0.4°C / min, the stirring is stopped, and the temperature is cooled at a uniform speed of 0.2°C / min to Stand at 0°C for crystal growth for 12 hours, then filter; ⑤Wash the filter cake obtained by filtering in ④ twice with a mixed solution of e...

Embodiment 2

[0053] ① Dissolve the crude sodium carbosulfonate in a mixed solution of water and methanol with a volume ratio of 15:1 at 70°C and a stirring speed of 150 rev / min; Activated carbon with 2% crude product weight, stirred at 150 rpm for 20 minutes, filtered to remove carbon, and filtered the filtrate through a 0.22 μm filter membrane; ③ Cool down to 60 °C at 0.2 °C / min, and stir at a stirring speed of 150 rpm While adding ethanol with a weight of 1 / 20 of the mixture of middle water and methanol at a speed of 20ml / min, stir for 30 minutes; ① A mixed solution of ethanol, methanol and chloroform with a volume ratio of 8 times the mixture of water and methanol is 10:5:1; at the same time, cool down to 12°C at 0.8°C / min, stop stirring, and cool down to 0.5°C / min at a uniform speed Stand at 2°C for crystal growth for 12 hours, then filter; ⑤ Wash the filter cake obtained by filtering in ④ twice with a mixed solution of ethanol, methanol and chloroform at a volume ratio of 2 times the ...

Embodiment 3

[0056] prescription:

[0057] Carbosulfonium Sodium Compound 20g

[0058] Mannitol 60g

[0059] Water for injection 1000ml

[0060] Make 1000 pieces

[0061] Process:

[0062] 1. Add the prescribed amount of sodium carbosulfonate to 70% of the amount of water for injection, stir to dissolve at 65°C, add water for injection to 80%, then add mannitol according to the prescribed amount, stir to dissolve, add water for injection to the full amount, and stir evenly.

[0063] 2. Add 0.15% activated carbon to 1, stir for 20 minutes, decarbonize by filtration, and sterilize by filtration with a 0.22 μm filter membrane to detect intermediates.

[0064] 3. Freeze-drying:

[0065] ① Pre-freezing: put the filtrate in 2 subpackages into a half-stoppered freezer and place it in a pre-cooled freezer at -35°C, keep it for 2 hours, then cool it down to -45°C at a speed of 1.5°C / min, and keep it warm for 2 hours;

[0066] ②Sublimation: Turn on the vacuum device, control the vacuum degree ...

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Abstract

The invention relates to a carbazochrome sodium sulfonate compound which is a crystal. The characteristic peak in a map through X-ray powder diffraction determination is 12.5 degrees, 17.4 degrees, 19.8 degrees, 21.0 degrees, 21.5 degrees, 23.4 degrees, 26.2 degrees, 26.8 degrees, 27.7 degrees, 29.0 degrees, 3.01 degrees, 31.6 degrees, 32.1 degrees, 35.0 degrees, 38.5 degrees, 40.3 degrees and 51.9 degrees at 2theta+ / -0.2 degrees. The invention further provides a medical composition preparation containing the carbazochrome sodium sulfonate compound. The medical composition preparation is a freeze-dried powder injection, a water injection and a troche. The compound provided by the invention can be prepared in various medical forms and is extremely high in stability. The carbazochrome sodium sulfonate freeze-dried powder, water injection and troche preparations provided by the invention are simple in formulation and technology, the stability is remarkably improved, and the pharmaceutical safety and effectiveness are improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a sodium carbosulfonate compound and a pharmaceutical composition thereof. Background technique [0002] Sodium carbosulfonate, its chemical name is: chemical name: 1-methyl-6-oxo-2,3,5,6-tetrahydroindole-5-semicarbazone-2-sulfonic acid sodium salt three Hydrate. A new generation of vascular hemostatic drugs, is a very clinically valuable vascular strengthening agent. It is a derivative of carbacrol (Anluoxue), and a sodium sulfonate group is introduced into the molecular structure, which overcomes the shortcomings of carbacrol's low solubility and must be assisted by salicylic acid, thus producing obvious hemostasis Effect. Sodium carbosulfonate can increase the resistance of capillaries to injury, reduce the permeability of capillaries, and promote the retraction of broken capillaries to stop bleeding. [0003] It is clinically used for bleeding in the urinary system, upper...

Claims

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Application Information

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IPC IPC(8): C07D209/30A61K31/404A61P7/04
Inventor 李美林胡成忠马虹
Owner HUNAN WUZHOUTONG PHARMA
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