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Tetrodotoxin formulation for drug rehabilitation , pain ease

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, convenient medical use and high purity

Inactive Publication Date: 2008-12-10
SHANGHAI YINIAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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  • Tetrodotoxin formulation for drug rehabilitation , pain ease
  • Tetrodotoxin formulation for drug rehabilitation , pain ease
  • Tetrodotoxin formulation for drug rehabilitation , pain ease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] [Example 1] Preparation of bulk drug tetrodotoxin

[0049] 100kg of puffer fish ovaries were minced with a meat grinder, homogenized with a homogenizer, added with 100 liters of 60% ethanol containing 3% acetic acid, stirred and soaked for 3 times, filtered and centrifuged, and the filtrate was taken 4 times, and then filtered under reduced pressure. , the filtrate was passed through a D152 weakly acidic cation resin column, and the column was eluted with deionized water until the eluent was colorless, and then eluted with 10% acetic acid aqueous solution (elution rate 50ml / min). Detected by HPLC, the venom containing venom was enriched, combined and concentrated under reduced pressure, the concentrate was passed through a glucose gel LH-20 column, eluted with 50% ethanol containing 5% acetic acid, detected by HPLC, and the eluate containing TTX was enriched, Combined, concentrated under reduced pressure, the concentrate was adjusted to pH=8.0 with ammonia water, placed...

Embodiment 2

[0051] [Example 2] Preparation of bulk drug tetrodotoxin

[0052] 100kg of puffer fish ovaries were minced with a meat grinder, homogenized with a homogenizer, added with 120 liters of 50% methanol containing 5% acetic acid, stirred and soaked for 6 times, filtered and centrifuged, and the filtrate was taken 4 times, filtered under reduced pressure, The filtrate was passed through a D152 type weakly acidic cation resin column, and the column was eluted with deionized water until the eluate was colorless, and then eluted with 10% acetic acid (elution rate 50ml / min). Detected by HPLC, the venom containing venom was enriched, combined and concentrated under reduced pressure, the concentrate was passed through a glucose gel LH-20 column, eluted with 50% ethanol containing 5% acetic acid, detected by HPLC, and the eluate containing TTX was enriched Combined, concentrated under reduced pressure, the concentrate was adjusted to pH 9.0 with ammonia water, placed at a low temperature o...

Embodiment 3

[0054] [Example 3] Preparation of bulk drug tetrodotoxin

[0055] Take 100 kg of the liver of the puffer fish, mince it in 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 4 times of filtrate, and then filter under reduced pressure , the filtrate was passed through a D152 weakly acidic cation resin column, and the column was eluted with deionized water until the eluent was colorless, and then eluted with 10% acetic acid aqueous solution (elution rate 50ml / min). Detected by HPLC, the venom containing venom was enriched, combined and concentrated under reduced pressure, the concentrate was passed through a glucose gel LH-20 column, eluted with 50% ethanol containing 5% acetic acid, detected by HPLC, and the eluate containing TTX was enriched, Combined, concentrated under reduced pressure, the concentrate was adjusted to pH=8.5 with ammonia water, placed at a low ...

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Abstract

The present invention relates to a tetrodotoxin preparation used for drugs abstinence and analgesia. The preparation comprises small dose of tetrodotoxin that is taken as active ingredient of medicine and cosolvent or allowable supportting agent in pharmacy. The cosolvent is amino acid. In the present invention, the amino acid is taken as the cosolvent, which not only can act as the cosolvent for increasing solubility of the tetrodotoxin in water, but also can form highly water-soluble salting liquid with the tetrodotoxin. The tetrodotoxin used in the present invention is prepared by adopting the specific method of the present invention. The purity of the prepared tetrodotoxin is as high as 98 percent with high yield. The preparation formed by the tetrodotoxin prepared by adopting the method provided in the present invention and amino acid is not only good in water solubility, but also good in stability, safe, reliable, stable in quality. The preparation does not need to be preserved in the refrigerator at specific temperature. The preparation can be preserved for more than 2 years at room temperature, thus greatly saving storage and transportation cost and providing convenience for use in medical treatment. The cure effect is evident, and in particular when applied to physiologic de-toxin, the tetrodotoxin preparation has a cure rate reaching 100 percent.

Description

technical field [0001] The invention belongs to the field of medicinal preparations, and in particular relates to a tetrodotoxin preparation for detoxification and analgesia. Background technique [0002] Tetrodotoxin (TTX) is a low molecular weight alkaloid extracted from the guts of puffer fish. Due to its unique chemical structure, it is a specific blocker of cellular sodium ion channels. 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 mediation of alkaloid addiction. There have also been reports of analgesic treatment. Therefore, it plays a very important role in both biological research and medical clinical applications. [0003] Because TTX can block sodium ion channels in cells in very small amounts, but has no effect on potassium ion channels, it is highly metastatic, so it is a very us...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/529A61K47/26A61K47/16A61P25/36
Inventor 王开业
Owner SHANGHAI YINIAN BIOTECH
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