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Drug addiction-stopping formulation and preparation thereof

A technology of preparations and modulators, applied in the field of detoxification preparations and their preparations, can solve problems such as unreviewed or resolved, affect the therapeutic effect, cannot determine the content or proportion, etc., to ensure safety and effectiveness, and reduce stimulation sensitivity Degree, the effect of ensuring stability

Active Publication Date: 2006-02-22
XIAMEN ZHAOYANG BIOLOGICAL ENG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The above inventions have played a positive role in promoting tetrodotoxin into clinical application research, but there are still unresolved key technical problems in terms of the accurate measurement of active ingredients in its preparations and the stability of effective doses for clinical use.
Wherein the publication number is W095 / 24903 patent disclosed detoxification dose and the poisoning dose of tetrodotoxin is close, example experimenter presents the poisoning symptom (tongue, mouth, lip complete numbness that part also includes upper and lower extremities) that tetrodotoxin induces. Numbness); in the patent No. 9611549454.5, the therapeutic dose of tetrodotoxin is 0.5-10.0 μg / 1-20ml, and the dose used in the example is injected intramuscularly or intravenously once a day, 20 μg each time, but it is obtained by the extraction process used Tetrodotoxin is not a pure product, but a mixture containing at least 2 to 3 derivatives. There are following problems in clinical use: the dose of tetrodotoxin cannot be accurately controlled, and the content or proportion of unseparated derivatives in the preparation cannot be determined , which will lead to uncertainty in the content of tetrodotoxin in the preparation, which not only affects the therapeutic effect, but also cannot guarantee the safety of medication; The dose-response needs to be further verified
However, how to ensure the accurate measurement of the main active ingredients of tetrodotoxin to ensure the safety of tetrodotoxin in clinical use, and the stability of tetrodotoxin as an active ingredient in the preservation process after the formulation of preparations have not been commented or resolved.

Method used

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  • Drug addiction-stopping formulation and preparation thereof
  • Drug addiction-stopping formulation and preparation thereof
  • Drug addiction-stopping formulation and preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0049] The components of the invention are tetrodotoxin monomer with a purity of more than 99%, acid vehicle carrier acetic acid-sodium acetate, function regulator chlorobutanol and stabilizer 4,9-dehydration-6-epi-tetrodotoxin.

[0050] In each component of the detoxification preparation, the content of tetrodotoxin was selected as 5 μg / ml. Acetic acid - The content of sodium acetate is 8.4 mg / ml acetic acid and 1.0 mg / ml sodium acetate. The content of the function regulator chlorobutanol is 5mg / ml; the content of lidocaine hydrochloride is 0.5mg / ml. Tetrodotoxin derivatives were selected from 4,9-anhydro-6-epi-tetrodotoxin, and the content was 10 μg / ml. Said tetrodotoxin monomer with a purity greater than 99% has a single peak spectrum detected by fluorescence detection reversed-phase high performance liquid chromatography, and the elemental analysis of C, H, and N agrees with the theoretical values ​​(Table 1). After the addition of 4,9 anhydro-6-epi-tetrodotoxin, its spe...

Embodiment 2

[0053] The components of the invention are tetrodotoxin monomer with a purity of more than 99%, acid vehicle carrier acetic acid-sodium acetate, function regulators chlorobutanol and benzyl alcohol, and stabilizer 4,9-dehydrated tetrodotoxin.

[0054]In each component of the detoxification preparation, the content of tetrodotoxin was selected as 16 μg / ml. Acetic acid - The content of sodium acetate is 10.3 mg / ml acetic acid and 18.0 mg / ml sodium acetate. The content of the function regulator chlorobutanol is 0.5 mg / ml, and the benzyl alcohol is 4.0 mg / ml. The tetrodotoxin derivative is 4,9-anhydrotetrodotoxin, and the content is 4 μg / ml. During the preparation, the tetrodotoxin monomer is directly dissolved into the acidic solvent carrier acetic acid-sodium acetate solution, and the functional regulators chlorobutanol and benzyl alcohol and the stabilizer 4,9-dehydrated tetrodotoxin are dissolved. At this time, the pH value of the preparation liquid is is 4.5. Filtered thro...

Embodiment 3

[0056] Similar to embodiment 1, the components of the present invention are tetrodotoxin monomer with a purity > 99%, acidic solvent carrier citric acid-sodium citrate solution, function regulator benzyl alcohol, stabilizer 4,9-dehydration-6 - Table tetrodotoxin.

[0057] In each component of the detoxification preparation, the content of tetrodotoxin was selected as 10 μg / ml. Citric Acid - The content of sodium citrate is 0.24 mg / ml of citric acid and 0.30 mg / ml of sodium citrate. The function regulator benzyl alcohol is 10mg / ml; lidocaine hydrochloride is 5.0mg / ml. The tetrodotoxin derivative was selected from 4,9-anhydro-6-epi-tetrodotoxin, and the content was 6.0 μg / ml. When preparing, the tetrodotoxin monomer is directly dissolved into the acidic solvent carrier citric acid-sodium citrate solution, the pH value is adjusted to 4.3, and the function regulator benzyl alcohol and the stabilizer 4,9-dehydration-6-epi-tetrodotoxin are dissolved. , filtered through a 0.20 μm ...

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Abstract

The invention relates to a drug rehabilitation preparation and method for preparation, wherein the preparation comprises predetermined amount of tetrodontoxin monomer as the main effective composition, right amount of auxiliary material carrier, function modifier and tetrodontoxin derivative as the stabilizer, the acidic dissolvent carrier is selected from acetic acid / sodium acetate, or citric acid / sodium citrate, or citric acid / disodium hydrogen phosphate, the function modifier is at least one selected from trichlorbutanolum, benzoic alcohol and lignocaine hydrochloride.

Description

technical field [0001] The invention relates to a medicinal preparation containing natural organic active ingredients, and uses marine biological toxin nerve center sodium ion channel blockers as ice drugs [amphetamine (amphetamine), methamphetamine (ice drug), 3, 4 subtypes] Methyldioxymethamphetamine (MDMA, commonly known as: ecstasy, also known as XTC, Smurfs, Adam, love him to die, out of body, etc.)], heroin and other opioids (heroin, morphine, codeine, doloretine , dihydroetorphine, opium, methadone, etc.), cannabis (including cannabis resin, cannabis oil, "Mary Warner" (called "Ganja" in India, "Kib" in North Africa, "Mary Warner") "Bhang" in South Africa, "Dagga" in South Africa), and "Hashish", which is processed from the top flowers and part of the leaves of the female cannabis plant] The preparation and application of drug detoxification preparations, especially involving tetrodotoxin in an accurate amount Monomer (purity > 99%) is used as main active ingredient...

Claims

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Application Information

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IPC IPC(8): A61K31/529A61P25/36
Inventor 易瑞灶许晨洪专张扬扬杨志文
Owner XIAMEN ZHAOYANG BIOLOGICAL ENG
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