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

A tetrodotoxin and respiratory technology, 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: 2003-12-03
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

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0059] This example is the preparation of tetrodotoxin raw materials.

[0060] Specific preparation method: Cut 100 kg of frozen Chrysanthemum fugu ovaries with a knife, soak in 100 liters of deionized water (hereinafter referred to as water), filter, filter in a centrifugal dryer, and soak the dried residue in water for a total of 4 Times. The obtained filtrate was boiled under direct fire for 5 minutes, and a large amount of protein was coagulated. The obtained coagulated protein was extracted twice with water and filtered by shaking. The combined filtrate is filtered with paper pulp, and the combined filtrate is the toxin stock solution, a total of 450 liters (toxin content is about 12.5 mg / l), and this solution is placed in a 9 liter n-butanol refrigerator for exchange.

[0061] 10 liters of D152 weakly acidic cation exchange resin (about 60 mesh) after normal pretreatment, use 8% ammonia water to convert to NH 4 + Type, the water is flushed to pH8, the toxin stock solution i...

Embodiment 2

[0078] This example is to confirm the chemical structure of the tetrodotoxin used in the preparation of the tetrodotoxin crude drug of the present invention

[0079] Appearance: white crystalline powder.

[0080] Solubility: easily soluble in acid water, insoluble in water, methanol, ethanol and other solvents.

[0081] Melting point: mp: 220-222°C. Consistent with the value reported in the literature.

[0082] Specific rotation [α] 15 D -8.64° (c 1.0, dilute AcOH).

[0083] Elemental analysis

[0084] Test instrument: CEST MOD.110 element analyzer

[0085] Completeness of measuring elements: the measuring result only contains C, H, N, O

[0086] Elemental analysis

Percentage content (%)

Average (%)

C

40.83， 40.85， 40.88

40.86

H

5.57， 5.58， 5.58

5.58

N

12.89， 12.86， 12.87

12.88

Elemental analysis

Percentage content (%)

Average (%)

C

...

example 3-7

[0122] Example 3-7 Preparation of respiratory tract administration solution formulations of the following compositions

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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 tetrodotoxin and its analogues used in the respiratory tract administration preparation for detoxification and analgesia. Background technique [0002] Tetrodotoxin (TTX) is also called puffer toxin. Due to different sources, there are Fugu poison, Spheroidine, Maculotoxin, Gobytoxin, Tari chatoxin, etc. The molecular formula is C 11 H 17 N 3 O 8 , Molecular weight 319.28, is a fully hydrogenated amino quinazoline compound. [0003] Since ancient times, puffer fish have forged an indissoluble bond with humans. Statistics show that tens of thousands of people have died of bulge poisoning due to bulimia. Someone used it to treat leprosy in the 19th century. Around the 1950s, the so-called "prepared medicine" of the "water decoction" type had been used for analgesia, sedation, and convulsion. This crude product with a purity of less than 1% has been tested worldwide (Japan Pharmaceutical Times: "Drug Name Search Dictionary" 197...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12A61K31/529A61K35/56A61P25/00A61P25/04A61P25/30A61P25/36A61P29/00
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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