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Preparation method of tetrodotoxin ester
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A technology of tetrodotoxin and esterification, which is applied in the field of medicine, can solve problems such as restricting the clinical application of tetrodotoxin and having no significant curative effect, and achieve the effect of simple method, inhibition of dependence, and amplification of curative effect
Inactive Publication Date: 2019-09-20
江苏华豚药业有限公司
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[0005] The inventor believes that the main reason why tetrodotoxin has not become a new drug so far is not only that tetrodotoxin has no significant curative effect when used alone, but also that it is a highly toxic alkaloid, and its toxicity is equivalent to 1250 times that of potassiumcyanide. This restricts the clinical application of tetrodotoxin
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Embodiment 1
[0038] Example 1 Preparation method of tetrodotoxin ester
[0039] Take 20ml of glyceryl monooleate with a purity of ≥98%, put it in a 50ml beaker, heat it in a water bath, keep the temperature at 50-80°C, and stir it with a magnetic force. Take 5mg of pure tetrodotoxin, put it in a 2ml vial, add 9.45mg of citric acid, 15.55mg of sodium citrate, 1ml of pure water, let it stand until it is completely dissolved, draw it out with a small syringe, and drop into the stirring monooleic acid Glycerides were continuously stirred for 24 hours, and allowed to stand still to obtain 20 ml of tetrodotoxin monooleate (water evaporated), and the theoretical value of tetrodotoxin was 250 μg / ml.
Embodiment 2
[0040] Example 2 Preparation method of tetrodotoxin ester
[0041] Take 25ml of glyceryl linolenate with a purity of ≥98%, put it in a 50ml beaker, heat it in a water bath, keep the temperature at 50-80°C, and stir it with a magnetic force. Take 5mg of tetrodotoxin, put it in a 2ml vial, add 9.45mg of citric acid, 15.55mg of sodium citrate, 1ml of pure water, let it stand until it is completely dissolved, draw it out with a small syringe, and drop it into the stirring glyceryl linolenate , continuously stirred for 24 hours, and stood still to obtain 25 ml of tetrodotoxin linolenic acid ester (water evaporated), and the theoretical value of tetrodotoxin was 200 μg / ml.
Embodiment 3
[0042] Example 3 Preparation method of tetrodotoxin ester
[0043]Take 20ml of triolein with a purity of ≥98%, put it in a 50ml beaker, heat it in a water bath, keep the temperature at 50-70°C, and stir it with a magnetic force. Take 5mg of tetrodotoxin, put it in a 2ml vial, add 1ml of acetic acid with a concentration of 1%, heat slightly, shake until completely dissolved, draw it out with a small syringe, drop it into the stirring triolein, and stir continuously for 24 hours, After standing still, 20ml of tetrodotoxin trioleate was obtained (water evaporated), and the theoretical value of tetrodotoxin was 250μg / ml.
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technical field [0001] The invention relates to a preparation method of tetrodotoxin ester, which belongs to the field of medicine. The tetrodotoxin ester of the present invention is a new compound produced by dissolving tetrodotoxin into unsaturated fatty acid glyceride or saturated fatty acid glyceride after chemical reaction. This new compound does not have the toxicity of tetrodotoxin, and can be used to amplify the curative effect of shared drugs and suppress the dependence, tolerance and side effects of shared drugs. The invention overcomes the high toxicity of the tetrodotoxin when taken orally, and opens up a new way for the safe application of the tetrodotoxin. Background technique [0002] In 1909, Japanese scholar Yoshisumi Tahara extracted a crude toxin from puffer fish ovary, named Tetrodotoxin (TTX for short). In 1950, Japanese scientist Akira Yoko obtained the crystalline substance of tetrodotoxin and found that it is a non-proteintoxin with high toxicity a...
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