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Tetrodotoxin respiratory tract administration prepn. used for giving-up drug and easing pain

A technology of tetrodotoxin and respiratory tract, applied in the direction of non-central analgesics, medical preparations containing active ingredients, antipyretics, etc., can solve the problems of short duration, small side effects, and abnormal perception of patients, and achieve the goal of using Convenient, less toxic and side effects, quick effect

Inactive Publication Date: 2008-01-09
潘心富
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] (3) Pain relief for patients with advanced cancer, the effect is good, and there is no report of addiction
[0028] After injection of tetrodotoxin injection, some patients may have abnormal mouth and tongue sensation, head congestion, headache and other reactions, but the duration is not long
[0029] (3) In the patent No. USP5846975, CN1051706C and EP0750909A1, it is pointed out that the aminohydroquinazoline compounds represented by tetrodotoxin It and its derivatives have unprecedented detoxification effects in the field of detoxification, and they have no drug dependence and less toxic side effects, but the administration methods only include oral and subcutaneous muscle or intravenous injection

Method used

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  • Tetrodotoxin respiratory tract administration prepn. used for giving-up drug and easing pain
  • Tetrodotoxin respiratory tract administration prepn. used for giving-up drug and easing pain

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0059] This example is the preparation of tetrodotoxin bulk drug.

[0060] Concrete preparation method: cut 100kg of frozen puffer chrysanthemum ovaries with a knife, soak in 100 liters of ion-free water (hereinafter referred to as water), filter, filter in a centrifugal dryer, soak the dry residue in water again, and extract 4 Second-rate. The obtained filtrate was boiled on direct fire for 5 minutes, a large amount of protein coagulated, and the obtained coagulated protein was extracted twice with water, and then filtered. The combined filtrates are filtered with pulp, and the combined filtrates are the toxin stock solution, a total of 450 liters (the poison content is about 12.5 mg / l). This solution is added to 9 liters of n-butanol and placed in the refrigerator for replacement.

[0061] 10 liters of D152 type weakly acidic cation exchange resin (about 60 mesh) is pretreated by normal methods, and then converted into NH with 8% ammonia water 4 + Type, washed with water ...

Embodiment 2

[0079] This example is to confirm the chemical structure of the tetrodotoxin for preparing the tetrodotoxin bulk drug of the present invention

[0080] Appearance: white crystalline powder.

[0081] Solubility: easily soluble in acid water, insoluble in water, methanol, ethanol and other solvents.

[0082]Melting point: mp: 220-222°C. consistent with the reported values ​​in the literature.

[0083] Specific rotation [α] 15 D -8.64° (c 1.0, dilute AcOH).

[0084] Elemental analysis

[0085] Test instrument: CEST MOD.110 Elemental Analyzer

[0086] Determination of completeness of elements: the determination results only contain C, H, N, O

[0087] Determine the data list and compare with the reference substance or theoretical value (see Table 1 and Table 2)

[0088] Table 1 Elemental analysis results of samples

[0089] Elemental analysis

Percentage (%)

Average (%)

C

40.83, 40.85, 40.88

40.86

H

5.57, 5.5...

example 3-7

[0141] Example 3-7 prepares the respiratory tract administration solution preparation of following composition

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Abstract

A medicine in the form of aerosol or spray for dropping drug or antalgic purpose is prepared from tetrodotoxic citrate or tetrodonic acetate. Its advantages are applying it via respiratory tract, high effect up to 97% or more, high safety, and no addiction.

Description

technical field [0001] The present invention relates to the respiratory tract administration preparation of tetrodotoxin and its analogs for detoxification and analgesia. Background technique [0002] Tetrodotoxin (tetrodotoxin, TTX) is also known as dove toxin. Depending on the source, there are Fugu poison, Spheroidine, Maculotoxin, Gobytoxin, Tarichatoxin, etc. Molecular formula is C 11 h 17 N 3 o 8 , with a molecular weight of 319.28, is a perhydrogenated aminoquinazoline compound. [0003] Since ancient times, puffer fish have had an indissoluble bond with human beings, and statistics show that tens of thousands of people have died due to gluttony puffer fish poisoning. In the 19th century, some people used it to treat leprosy. Around the 1950s, the so-called "proprietary medicine" of the "water decoction" type was used for analgesia, sedation, and shock. This crude product with a purity of less than 1% has been tested for sale all over the world (Nippon Pharmace...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/529A61K9/12A61P25/36A61P25/04A61K35/56A61P25/00A61P25/30A61P29/00
CPCA61K9/0073A61P25/00A61P25/04A61P25/30A61P25/36A61P29/00
Inventor 潘心富刘助国黄致强
Owner 潘心富
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