Application of Artemisinin Compounds in the Preparation of Medicines for Treating Neuropathic Pain and/or Complications

An artemisinin and compound technology, which is applied in the application field of artemisinin compounds in the preparation of medicines for the treatment of neuropathic pain and/or complications, can solve the problem of increasing ataxia, confusion, abnormal thinking, and blurred vision. Difficulty in paying attention to ataxia, association with neuropathic pain, inability to infer drug efficacy, etc., to achieve the effect of drug safety, low drug resistance, and low toxicity and side effects

Active Publication Date: 2020-04-17
INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the use of high doses greatly increases the occurrence of side effects such as dizziness, drowsiness, ataxia, confusion, fatigue, abnormal thinking, blurred vision, movement disorders, dry mouth, edema, weight gain, and attention difficulties. , and had no significant effect on depression and other concurrent mental symptoms
Tricyclic antidepressants have strong side effects and severe cardiotoxicity, leading to clinical discontinuation rates as high as 15-20%
But first of all, the pathological mechanisms of neuropathic diseases and neuropathic pain are completely different, so it is difficult for those skilled in the art to associate neuropathic pain based on the effect of artemisinin drugs on neurodegenerative diseases.
Secondly, all the examples in this document are limited to the cellular level, and those skilled in the art cannot infer its drug efficacy in whole animals from the experimental effects at the cellular level, especially for neuropathic pain and its concurrent mental symptoms. A disorder whose pathology involves the entire nervous system

Method used

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  • Application of Artemisinin Compounds in the Preparation of Medicines for Treating Neuropathic Pain and/or Complications
  • Application of Artemisinin Compounds in the Preparation of Medicines for Treating Neuropathic Pain and/or Complications
  • Application of Artemisinin Compounds in the Preparation of Medicines for Treating Neuropathic Pain and/or Complications

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0055] Experimental example 1: Experimental preparation, model construction and detection method

[0056] 1. Experimental animals

[0057] Clean-grade 8-week-old adult male C57 / BL6 mice, weighing 24-26 g, were provided by Beijing Weitong Lihua Experimental Animal Technology Co., Ltd., animal certificate number SYXK-2010-0034.

[0058] 2. Experimental grouping

[0059] After adapting to the environment for 4 days, the mice were weighed and subjected to open-field testing, forced swimming testing and tail-suspension testing. The mice whose body weight was less than 23 grams, the time spent in the center field of the open-field test was less than 15 seconds, and the forced swimming time of more than 10 seconds were excluded. 160 seconds, or individuals whose immobility time is beyond 50-100 seconds by tail suspension, and then randomly divided into sham operation group, model SNL group, and medication group, each group in each parallel experiment is more than 12.

[0060] 3. Es...

experiment example 2

[0075] Experimental Example 2: Therapeutic Effects of Dihydroartemisinin on Mechanical Allodynia, Depression and Anxiety in Neuropathic Pain

[0076] 1. Drug preparation and dosing regimen

[0077] The day of modeling / sham operation is recorded as D0. In the drug group, the ratio of 40 mg / kg (artemisinin analogue or positive drug pregabalin / mouse body weight) was administered orally, and the volume of the drug solution was 150 μL; dihydroartemisinin or pregabalin was suspended in 150 μL beforehand The medicine solution was made from the oil; the sham operation group and the model SNL group used the same volume of edible oil instead of the medicine solution, and the administration time and route were the same as those of the drug treatment group.

[0078] In the early administration experiment, the drug was given by intragastric administration from the 4th day, which was recorded as D4(1). The intragastric administration was carried out at 5:00 p.m. every day for 14 consecuti...

experiment example 3

[0096] Experimental Example 3: Therapeutic Effects of Artesunate on Mechanical Allodynia, Depression and Anxiety in Neuropathic Pain

[0097] 1. Drug preparation

[0098] Artesunate was pre-suspended in 150 μL of 5% medical sodium bicarbonate injection to make a drug solution; the sham operation group and the model SNL group used 5% medical sodium bicarbonate injection as the solvent carrier.

[0099] 2. Observation indicators

[0100] The mechanical pain threshold was detected on D4, D7, D10, and D13 after modeling, and the detection time points were 1.5 hours, 3 hours, and 24 hours after intragastric administration.

[0101] Tail suspension test and open field test were carried out on D9 and D17 days after modeling, respectively.

[0102] 3. Experimental results

[0103] 3.1 Artesunate can increase mechanical pain threshold and reduce pain sensitivity

[0104] The test results of the influence of artesunate on the mechanical pain threshold are as follows: Figure 5 It s...

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Abstract

The invention relates to application of artemisinine compound to preparation of medicine for treating neuropathic pain and / or complications. The neuropathic pain belongs to refractory chronic pain. The safe and effective clinic preventive measures are lacked till now. The artemisinine medicine has the characteristics of low toxicity and high safety. The invention discloses the exact and obvious curative effect of the artemisinine medicine on the treatment of neuropathic pain and depression and anxiety symptoms induced by the pain for the first time.

Description

technical field [0001] This application relates to a new pharmaceutical application of artemisinin compounds, especially the pharmaceutical application in the preparation of drugs for treating neuropathic pain and / or its complications. Background technique [0002] Neuropathic pain is pain caused by primary damage or dysfunction of the nervous system. Epidemiological studies have shown that the prevalence of neuropathic pain is as high as 8%, and about 90 million patients in China are in urgent need of safe and effective targeted treatment. Due to the complex etiology, it is difficult to pay attention to neuropathic pain in the early stage of the disease. About 50% of the patients have developed serious mental symptoms such as major depression and anxiety before seeking medical treatment. It leads to persistent and repeated symptoms of pain sensitivity, seriously affects the quality of life of patients, and brings huge economic burden and pressure to patients and society. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/366A61K31/357A61P25/04A61P25/22A61P25/24A61P25/28
CPCA61K31/357A61K31/366
Inventor 林娜朱春燕毛志云许琼虹
Owner INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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