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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

Inactive Publication Date: 2008-01-23
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 WO95 / 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

[0050] The components of the invention are tetrodotoxin monomer with a purity >99%, acidic solvent carrier acetic acid-sodium acetate, function regulator chlorobutanol and stabilizer 4,9-anhydro-6-epitetrodotoxin.

[0051] In each component of the detoxification preparation, the content of tetrodotoxin is selected as 5 μg / ml. Acetic acid-sodium acetate is present at 8.4 mg / ml of acetic acid and 1.0 mg / ml of sodium acetate. The content of the function regulator chlorobutanol is 5 mg / ml; the content of lidocaine hydrochloride is 0.5 mg / ml. Tetrodotoxin derivatives are selected from 4,9-anhydro-6-epitetrodotoxin with a content of 10 μg / ml. Said tetrodotoxin monomer with a purity greater than 99% has a unimodal spectrogram in its spectrogram detected by fluorescence detection reversed-phase high performance liquid chromatography, and its elemental analysis of C, H, and N coincides with theoretical values ​​(Table 1). After adding 4,9-anhydro-6-epitetrodotoxin, its spectrum showe...

Embodiment 2

[0054] The components of the invention are tetrodotoxin monomer with a purity >99%, acidic solvent carrier acetic acid-sodium acetate, function regulators chlorobutanol and benzyl alcohol, and stabilizer 4,9-dehydrated tetrodotoxin.

[0055]In each component of the detoxification preparation, the content of tetrodotoxin is selected as 16 μg / ml. Acetic acid-sodium acetate was present at 10.3 mg / ml of acetic acid and 18.0 mg / ml of sodium acetate. The content of the function regulator chlorobutanol is 0.5 mg / ml, and that of benzyl alcohol is 4.0 mg / ml. The derivative of tetrodotoxin is 4,9-anhydrotetrodotoxin with a content of 4 μg / ml. During preparation, the tetrodotoxin monomer is directly dissolved into the acidic solvent carrier acetic acid-sodium acetate solution, and then dissolved into the function regulator chlorobutanol and benzyl alcohol and the stabilizer 4,9-dehydrated tetrodotoxin. At this time, the pH value of the preparation liquid is is 4.5. Filter through a 0....

Embodiment 3

[0057] Similar to Example 1, the components of the present invention are tetrodotoxin monomer with purity>99%, acidic solvent carrier citric acid-sodium citrate solution, function regulator benzyl alcohol, stabilizer 4,9-anhydro-6 - Table tetrodotoxin.

[0058] In each component of the detoxification preparation, the content of tetrodotoxin is selected to be 10 μg / ml. The content of citric acid-sodium citrate is 0.24 mg / ml of citric acid and 0.30 mg / ml of sodium citrate. Function modulator benzyl alcohol is 10mg / ml; lidocaine hydrochloride is 5.0mg / ml. The tetrodotoxin derivative is 4,9-anhydro-6-epitetrodotoxin with a content of 6.0 μg / ml. During preparation, 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-anhydro-6-epitetrodotoxin are dissolved , filtered through a 0.20 μm filter membrane, placed at room temp...

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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 present invention relates to a kind of medicine preparation that contains natural organic active ingredient, uses marine biotoxin nerve center sodium ion channel blocker as ice poison [amphetamine (amphetamine), methamphetamine (methamphetamine), 3, 4 sub Methyldioxymethamphetamine (MDMA, commonly known as: ecstasy, also known as XTC, Smurfs, Adam, love him to death, soul out of body, etc.)], heroin and other opioids (heroin, morphine, codeine, demerol , dihydroetorphine, opium, methadone, etc.), cannabis [including cannabis resin, cannabis oil, "Marijuana" (called "Ganja" in India, "Kib" in North Africa, and the Middle East) processed from cannabis stems and leaves "Bhang" and "Dagga" in South Africa), and "Hashish" processed from the top flowers and parts of the leaves of cannabis female plants] The preparation and application of drug detoxification preparations, especially involving the use of tetrodotoxin in an accurate quantity Monomer (purity&...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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