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Method for preparing tetrodotoxin

A technology for tetrodotoxin and preparations, which is applied in the field of tetrodotoxin preparations, can solve problems such as the inability to form high water solubility, and achieve the effects of good water solubility, stable quality and excellent stability

Inactive Publication Date: 2010-11-24
SHANGHAI YINIAN BIOTECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the absorption rate of nasal mucosa is affected by many factors
And the acid used in the examples of this patent is a buffering agent, and the number of moles of the acid used in the preparation shows that most of the TTX still has not formed a salt, that is, most of the TTX still cannot form a highly water-soluble solution, and cannot fundamentally solve the problem of its water solubility. question

Method used

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  • Method for preparing tetrodotoxin
  • Method for preparing tetrodotoxin
  • Method for preparing tetrodotoxin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] [embodiment 1] preparation of crude drug tetrodotoxin

[0053] Grind 100kg of pufferfish ovaries with a meat grinder, homogenate with a homogenizer, add 100 liters of 60% ethanol containing 3% acetic acid, stir and soak for 3 times, filter and centrifuge, take the filtrate for 4 times, and then filter under reduced pressure , the filtrate was passed through the D152 type weakly acidic cationic resin column, and the column was eluted with deionized water until the eluate was colorless, and then eluted with 10% acetic acid aqueous solution (elution rate 50ml / min). Detected by HPLC, enriched with venom, combined and concentrated under reduced pressure, the concentrated solution passed through a glucose gel LH-20 column, eluted with 50% ethanol solution containing 5% acetic acid, detected by HPLC, enriched with the eluate containing TTX, Combined and concentrated under reduced pressure, the concentrate was adjusted to pH = 8.0 with ammonia water, placed at a low temperature...

Embodiment 2

[0055] [embodiment 2] the preparation of bulk drug tetrodotoxin

[0056] 100kg of puffer fish ovary is minced with a meat grinder, homogenized with a homogenizer, added 120 liters of 50% methanol containing 5% acetic acid, stirred and soaked 6 times, filtered, centrifugally filtered, and the filtrate is taken 4 times, filtered under reduced pressure, The filtrate was passed through a D152 type weakly acidic cationic resin column, and the column was eluted with deionized water until the eluate was colorless, and then eluted with 10% acetic acid solution (elution rate 50ml / min). Detected by HPLC, enriched with venom, combined, concentrated under reduced pressure, the concentrated solution passed through a glucose gel LH-20 column, eluted with 50% ethanol containing 5% acetic acid, detected by HPLC, enriched with eluate containing TTX Combined and concentrated under reduced pressure, the concentrate was adjusted to pH 9.0 with ammonia water, placed at a low temperature of 10°C fo...

Embodiment 3

[0058] [embodiment 3] preparation of crude drug tetrodotoxin

[0059] Take 100 kg of puffer fish liver, mince it with a meat grinder, homogenize it with a homogenizer, add 110 liters of 60% ethanol containing 4% acetic acid, stir and soak for 4 times, filter, centrifugal filter, take the filtrate for 4 times, and then filter under reduced pressure , the filtrate was passed through the D152 type weakly acidic cationic resin column, and the column was eluted with deionized water until the eluate was colorless, and then eluted with 10% acetic acid aqueous solution (elution rate 50ml / min). Detected by HPLC, enriched with venom, combined and concentrated under reduced pressure, the concentrated solution passed through a glucose gel LH-20 column, eluted with 50% ethanol solution containing 5% acetic acid, detected by HPLC, enriched with the eluate containing TTX, Combined and concentrated under reduced pressure, the concentrate was adjusted to pH = 8.5 with ammonia water, placed at ...

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Abstract

The invention relates to a tetrodotoxin preparation for treating drug addiction and relieving pain. The preparation comprises small-dose tetrodotoxin serving as a medicinal active ingredient and a pharmaceutical permissible cosolvent or support agent, wherein the cosolvent is amino acid. The amino acid is used as the cosolvent, so the amino acid has the function of the cosolvent, increases the water solubility of the tetrodotoxin, and can also form highly water-soluble salt solution with the tetrodotoxin. The tetrodotoxin used in the invention is prepared by a specific method; and the purity of the prepared tetrodotoxin reaches 98 percent and the yield is high. The preparation consisting of the tetrodotoxin prepared by the method and the amino acid has the advantages of high water solubility, high stability, safety, reliability, stable quality, no need of preservation in a refrigerator at a specific temperature, storage life of more than two years at room temperature, capability of greatly saving the storage and transportation cost and facilitating medical use, obvious treatment effect, and cure rate of 100 percent when particularly used for physiological detoxification.

Description

[0001] This application is a divisional application of Chinese patent application 200810127045.X. [0002] Original application date: 2008-6-18 [0003] Original application number: 200810127045.X [0004] Invention name of the original application: a tetrodotoxin preparation for detoxification and analgesia technical field [0005] The invention belongs to the field of pharmaceutical preparations, in particular to a tetrodotoxin preparation for detoxification and analgesia. Background technique [0006] Tetrodotoxin (TTX) is a low molecular weight alkaloid extracted from the viscera of puffer fish. Due to its unique chemical structure, it is a specific blocker of sodium ion channels in cells. Therefore, it has an irreplaceable position as a biological reagent in the field of biological research. The pharmacological effects of tetrodotoxin in clinical medicine have been reported as early as the 1930s for the clinical intervention of alkaloid addiction. There are also co...

Claims

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Application Information

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IPC IPC(8): C07D491/22
Inventor 王开业
Owner SHANGHAI YINIAN BIOTECH
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