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Application of stilbene glycoside to preparing analgesic medicine

A stilbene glycoside and drug technology, which is applied in the field of drugs for delaying or alleviating opioid tolerance, preparing and enhancing the analgesic effect of opioid drugs, and achieving the effects of enhancing application space, reducing opioid tolerance, and enriching sources.

Inactive Publication Date: 2015-11-11
JIANGSU TIANSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] At present, there is no report about the use of stilbene glycosides in drugs that enhance the analgesic effect of opioids, nor is there any report about the use of stilbene glycosides in drugs that delay or reduce opioid tolerance
Whether stilbene glycosides can also inhibit the activation of microglial cells induced by opioids to exert their effects of enhancing opioid analgesia and delaying or alleviating opioid tolerance is still unknown

Method used

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  • Application of stilbene glycoside to preparing analgesic medicine
  • Application of stilbene glycoside to preparing analgesic medicine
  • Application of stilbene glycoside to preparing analgesic medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 (acute analgesic effect enhancement experiment)

[0030] a) Experimental animals: healthy adult female ICR mice, clean grade, weighing 18-22 g. The experimental animals were raised in an independent environment with 12h-12h alternation of day and night, the room temperature was maintained at 24±2°C, water and food were free to drink, and the experiment was carried out after 1 week of adaptation to the environment. All handling of animals followed the requirements of the Ethics Committee of the International Association for the Study of Pain.

[0031] b) Test drugs and reagents:

[0032] The drug stilbene glycoside, with a purity of 98%, is commercially available. Morphine hydrochloride was purchased from Shenyang No. 1 Pharmaceutical Factory.

[0033] c) Test method:

[0034] Dosage and method of administration of stilbene glycosides and morphine: stilbene glycosides were dissolved in physiological saline, and the administration dose was 60 mg / kg, and t...

Embodiment 2

[0039] Example 2 (Opioid Tolerance Alleviation Experiment)

[0040] a) Test animals:

[0041] Female ICR mice, clean grade, weighing 18-22 g. The experimental animals were raised in an independent environment with 12h to 12h alternation of day and night, the room temperature was maintained at 24±2°C, and they had free access to water and food. Experiments were carried out after 1 week of adaptation to the environment. All handling of animals followed the requirements of the Ethics Committee of the International Association for the Study of Pain.

[0042] b) Test drugs and reagents:

[0043] The drug stilbene glycoside, with a purity of 98%, is commercially available. Morphine hydrochloride was purchased from Shenyang No. 1 Pharmaceutical Factory.

[0044] c) Test method:

[0045] Dosage and method of administration of stilbene glycosides: stilbene glycosides are dissolved in physiological saline, the dose is 60 mg / kg, and the administration method is intragastric administ...

Embodiment 3

[0050] Embodiment 3 (inhibition of inflammatory factor mRNA up-regulation experiment)

[0051] a) Test cells:

[0052] BV2 microglial cells were cultured in DMEM medium containing 10% fetal bovine serum, 5% CO2, and cultured in a constant temperature incubator at 37°C. It can be subcultured when it covers 80% of the bottom of the culture bottle. 24 hours before the experiment, the medium was replaced with 0.5% fetal bovine serum high glucose DMEM.

[0053] b) Test drugs and reagents:

[0054] Fetal bovine serum was purchased from Hyclone; DMEM and Trizol were purchased from Invitrogen; TaKaRaPrimeScript kit was purchased from Dalian Bao Biological Engineering Co., Ltd.

[0055] c) Test method:

[0056] Real-time quantitative PCR: the RNA of each group was extracted by Trizol method. The reverse transcription reaction uses SYBRGreenAssay of TaKaRaPrimeScript kit, the reaction system is: 5×PrimeScriptBuffer2μl, PrimeScriptRTEnzyme0.5μl, OligodTPrimer0.5μl, Random6mers0.5μl,...

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PUM

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Abstract

The invention discloses novel application of stilbene glycoside to the field of analgesic medicine, and particularly discloses application of stilbene glycoside to preparing medicine for enhancing analgesic effects of opioid medicine and delaying or relieving opioid tolerance. The application has the advantages that the stilbene glycoside is used with the opioid medicine, or compound preparations are made of the stilbene glycoside and the opioid medicine, so that the analgesic time can be prolonged, the analgesic efficacy can be enhanced, and opioid tolerance during chronic opioid medicine treatment procedures can be delayed or relieved; excessive activation of spinal glial cells induced by the opioid medicine is particularly suppressed by the stilbene glycoside, so that effects can be realized.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to the new use of stilbene glycoside in the field of analgesic drugs, in particular to the use in the preparation of drugs for enhancing the analgesic effect of opioids and delaying or alleviating opioid tolerance. Background technique [0002] Pain is a complex physiological and psychological activity, including the pain sensation caused by noxious stimuli acting on the body, and the body's pain response to noxious stimuli. Pain can be used as a warning that the body is injured, causing a series of defensive protective reactions of the body, but some acute or long-term severe pain is an unbearable torture to the body. Pain is one of the most common clinical symptoms, and it is also an important problem that medical workers need to solve urgently. [0003] In terms of the course of the disease, pain can be divided into acute pain and chronic pain. Acute pain is pain that is new and of short d...

Claims

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Application Information

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IPC IPC(8): A61K31/7032A61P29/00A61P25/04A61P25/30A61K31/4468A61K31/137A61K31/135A61K31/485A61K31/445
Inventor 季浩刘文涛阚建伟窦长清刘佳
Owner JIANGSU TIANSHENG PHARMA
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