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Drug combination for analgesia, anesthesia or drug rehabilitation

A drug and tetrodotoxin technology, applied in the direction of anesthetics, drug combinations, antipyretics, etc., to achieve the effect of improving therapeutic effect, improving bioavailability, inhibiting dependence and tolerance

Inactive Publication Date: 2015-02-18
赵继红 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, there is no use of open BBB hyperosmotic agents or BBB carriers at home and abroad to improve the permeability and bioavailability of tetrodotoxin and opioids to the blood-brain barrier, and at the same time use tetrodotoxin to transform opioids and cooperate with opioids to detoxify Synergistic Research and Reporting

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Preparation of a combined drug consisting of 4 μg / tube of TTX freeze-dried powder injection and pethidine water injection

[0044] The combined drug in this example consists of separately packaged tetrodotoxin freeze-dried powder injection and pethidine water injection.

[0045] The tetrodotoxin freeze-dried powder injection is composed of tetrodotoxin and 2-deoxy-d-glucose containing a buffer, the buffer is composed of citric acid and sodium citrate, and the weight ratio of tetrodotoxin to citric acid and sodium citrate is 1: 1.89:3.11, the weight ratio of tetrodotoxin to 2-deoxy-d-glucose is 1:5000, the content of tetrodotoxin in each tetrodotoxin freeze-dried powder injection is 4 μg, and the content of 2-deoxy-d-glucose is 20 mg.

[0046] The meperidine water injection is a commercially available meperidine water injection, produced by Qinghai Pharmaceutical Factory Co., Ltd., wherein the meperidine dose is the low dose (50mg / 1ml) specification indicated i...

Embodiment 2

[0054] Example 2 Preparation of a combined drug consisting of 4 μg / tube of TTX freeze-dried powder injection and morphine water injection

[0055] The combined medicine in this example consists of separately packaged tetrodotoxin freeze-dried powder injection and morphine water injection.

[0056] Tetrodotoxin freeze-dried powder injection is composed of tetrodotoxin and mannitol containing buffer, the buffer is composed of citric acid and sodium citrate, the weight ratio of tetrodotoxin to citric acid and sodium citrate is 1:1.89:3.11, tetrodotoxin The weight ratio of toxin to mannitol is 1:20000, the content of tetrodotoxin in each tube is 4 μg, and mannitol is 80 mg.

[0057] The morphine water injection is a commercially available morphine water injection, produced by Qinghai Pharmaceutical Factory Co., Ltd., wherein the morphine dosage adopts the low-dose (5mg / 0.5ml) or medium-dose (10mg / 1ml) specification indicated in the drug instruction sheet.

[0058] The preparation...

Embodiment 3

[0066] Example 3 Preparation of a combined drug consisting of 4 μg / tube of TTX freeze-dried powder injection and buprenorphine water injection

[0067] The combined drug in this example consists of separately packaged tetrodotoxin freeze-dried powder injection and buprenorphine water injection.

[0068] Tetrodotoxin freeze-dried powder injection is composed of tetrodotoxin and mannitol containing buffer, the buffer is composed of citric acid and sodium citrate, the weight ratio of tetrodotoxin to citric acid and sodium citrate is 1:1.89:3.11, tetrodotoxin The weight ratio of toxin to mannitol is 1:5000, the content of tetrodotoxin in each tube is 4 μg, and mannitol is 20 mg.

[0069] The buprenorphine aqueous injection is commercially available buprenorphine aqueous injection, produced by Qinghai Pharmaceutical Factory Co., Ltd., wherein the dosage of buprenorphine is the low dose (0.15mg / 1ml) specified in the drug instruction sheet.

[0070] The preparation method of the com...

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PUM

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Abstract

The invention provides a drug combination for analgesia, anesthesia or drug rehabilitation. The drug combination is composed of a tetrodotoxin injection and an opioid medical injection which are packaged separately. The tetrodotoxin injection is composed of tetrodotoxin containing a buffer agent and a high penetrating agent for opening of the blood-brain barrier (BBB) or a BBB carrier. The opioid medical injection is a commercially available injection containing an opioid receptor stimulant. In the drug combination for analgesia, anesthesia or drug rehabilitation, the BBB-opening high penetrating agent or the BBB carrier can raise BBB permeability and bioavailability of tetrodotoxin and the opioid medicine, and tetrodotoxin has a synergistic effect of de-addiction and synergism. Through cooperation of the three drugs, the drug therapeutic effect can be enhanced, duration of drug effect is prolonged, dosage of the opioid medicine is reduced, and tolerance and dependency of the opioid medicine are decreased or eliminated.

Description

technical field [0001] The invention relates to a combined medicine for analgesia, anesthesia or drug withdrawal, and belongs to the technical field of medicine preparation. Background technique [0002] Tetrodotoxin, the drug name is Tetrodotoxin, English Tetrodotoxin, referred to as TTX. Tetrodotoxin is a biologically active substance extracted from puffer fish viscera, which belongs to non-protein marine toxins, with a molecular formula of C11H17N3O8 and a molecular weight of 319.28. The appearance of tetrodotoxin is powdery crystal, insoluble in organic solvents, slightly soluble in water and ethanol, easily soluble in acidic aqueous solution, and decomposes rapidly in strong alkali or strong acid. Tetrodotoxin is relatively stable to heat, but it will gradually decompose when heated to 220°C, and it will be charred quickly when it exceeds 220°C. [0003] Studies have shown that the medicinal mechanism of tetrodotoxin lies in its ability to selectively block the nerve ...

Claims

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Application Information

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IPC IPC(8): A61K31/529A61K31/485A61K31/451A61K31/4468A61K31/137A61K31/135A61K47/26A61K47/22A61K47/18A61K47/12A61K47/10A61P29/00A61P23/00A61P25/36
CPCA61K31/529A61K31/137A61K31/4468A61K31/451A61K31/485A61K47/10A61K47/12A61K47/18A61K47/22A61K47/26A61K2300/00
Inventor 赵继红汤波澜赵琦吕晓平
Owner 赵继红
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