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Application of matrine in preparing opioid

A technology of opioids and matrine, which is applied in the field of preparation of drugs that enhance the analgesic effect of opioids, delay or reduce opioid tolerance, and can solve problems such as unpredictable, complicated drug effects, and drug effect synergy, and achieve relief. Adverse reactions, enhanced analgesic effect, effect of strong analgesic effect

Inactive Publication Date: 2015-09-30
JIANGSU TIANSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It should be pointed out that even the combined application of two different drugs for the same purpose is complex and unpredictable, and may produce synergistic, additive or even antagonistic effects.
Therefore, for those skilled in the art, unless the necessary experimental data are passed, it is difficult to simply establish the logic that matrine can enhance the analgesic effect of opioids or delay opioid tolerance based on the analgesic effect of matrine itself proposition
[0012] Whether matrine can also inhibit the activation of microglial cells induced by opioids to enhance opioid analgesia and delay or reduce opioid tolerance is still unknown.

Method used

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  • Application of matrine in preparing opioid
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  • Application of matrine in preparing opioid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 (acute analgesic effect enhancement experiment)

[0031] 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.

[0032] b) Test drugs and reagents:

[0033] Drug Matrine, 98% pure, commercially available. Morphine hydrochloride was purchased from Shenyang No. 1 Pharmaceutical Factory.

[0034] c) Test method:

[0035] Dosage and method of administration of matrine and morphine: matrine was dissolved in physiological saline, and the administration dose was 60 mg / kg, and the administration methods were all intragastric adminis...

Embodiment 2

[0040] Example 2 (Opioid Tolerance Alleviation Experiment)

[0041] a) Test animals:

[0042] 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.

[0043] b) Test drugs and reagents:

[0044] Drug Matrine, 98% pure, commercially available. Morphine hydrochloride was purchased from Shenyang No. 1 Pharmaceutical Factory.

[0045] c) Test method:

[0046] Dosage and method of administration of matrine: dissolve matrine with physiological saline, the dose is 60 mg / kg, and the administration method is intragastric administration.

[0047] ICR mice were randomly divided into fou...

Embodiment 3

[0051] Embodiment 3 (inhibition of inflammatory factor mRNA up-regulation experiment)

[0052] a) Test cells:

[0053] 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.

[0054] b) Test drugs and reagents:

[0055] Fetal bovine serum was purchased from Hyclone; DMEM and Trizol were purchased from Invitrogen; TaKaRa PrimeScript kit was purchased from Dalian Bao Biological Engineering Co., Ltd.

[0056] c) Test method:

[0057] Real-time quantitative PCR: the RNA of each group was extracted by Trizol method. SYBR Green Assay of TaKaRa PrimeScript kit was used for reverse transcription reaction. The reaction system was: 5×PrimeScript Buffer 2μl, Prime Script RT Enzyme 0.5μl, Oligo dT Primer 0.5μl,...

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Abstract

The invention discloses new application of matrine in the field of analgesic drugs, and particularly discloses application of matrine in preparing drugs enhancing the analgesic effect of opioid, and delaying or relieving opioid tolerance. The matrine is matched with the opioid for use, or the matrine and the opioid are prepared into compound preparations for use, the analgesia time of the opioid can be prolonged, the analgesic efficacy of the opioid can be enhanced, and the opioid tolerance phenomenon happening in the treating process of opioid slow in taking effect can also be delayed or relieved. Specifically, the effect is achieved in the mode that the matrine is used for inhibiting excessive activation, induced by the opioid, of spinal cord glial cells.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to the new application of matrine in the field of analgesic drugs, in particular to the application 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 sh...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61K45/06A61K31/485A61P25/04A61P29/00
Inventor 季浩刘文涛阚建伟窦长清刘佳
Owner JIANGSU TIANSHENG PHARMA
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