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New application of ligustrazine in field of analgesic drugs

A technology of ligustrazine and its use, which is applied in the pharmaceutical field to achieve the effects of enriching sources, alleviating opioid tolerance, and delaying or alleviating opioid tolerance

Inactive Publication Date: 2015-07-01
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The inventor's previous research results and a small number of literature reports show that ligustrazine can inhibit the activation of microglial cells induced by lipopolysaccharide or cerebral ischemia, but the mechanism of microglial cell activation under this condition is different from that of opioid-induced microglial cell activation. The activation mechanisms are obviously different. Therefore, whether ligustrazine can also inhibit opioid-induced microglial activation and p-P38 up-regulation to enhance opioid analgesia and delay or reduce opioid tolerance is still unknown.

Method used

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  • New application of ligustrazine in field of analgesic drugs
  • New application of ligustrazine in field of analgesic drugs
  • New application of ligustrazine in field of analgesic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Ligustrazine can improve morphine tolerance, but does not affect the basic pain threshold of mice

[0042] a) Test animals:

[0043] Healthy male 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.

[0044] b) Test drugs and reagents:

[0045] Ligustrazine, with a purity of 98%, is commercially available. Morphine hydrochloride was purchased from Shenyang No. 1 Pharmaceutical Factory.

[0046] c) Test method:

[0047] Intraperitoneal injection of mice (i.p.): Insert the injection needle into the subcutaneous area of ​​the lower abdomen about 0.5 cm away from the linea a...

Embodiment 2

[0053] Example 2 Ligustrazine can significantly reduce the mRNA levels of inflammatory factors TNF-α and IL-1β in the spinal cord of chronic morphine-tolerant mice

[0054] a) Test animals:

[0055] Healthy male 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.

[0056] b) Test drugs:

[0057] Ligustrazine, with a purity of 98%, is commercially available. Morphine hydrochloride was purchased from Shenyang No. 1 Pharmaceutical Factory.

[0058] c) Test method:

[0059] Intraperitoneal injection of mice: Insert the injection needle into the subcutaneous at a place about 0.5 cm away from...

Embodiment 3

[0067] Example 3 Ligustrazine significantly inhibits the activation of spinal cord microglial cells in chronic morphine-tolerant mice

[0068] a) Test animals:

[0069]Healthy adult female ICR mice, clean grade, weighing 18-22g. 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.

[0070] b) Test drugs and reagents:

[0071] Ligustrazine, with a purity of 98%, is commercially available. Morphine hydrochloride was purchased from Shenyang No. 1 Pharmaceutical Factory.

[0072] c) Test method:

[0073] Dosage and method of administration of ligustrazine and morphine: Ligustrazine was dissolved in normal saline, the dosage was 60 ...

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Abstract

The invention discloses a new application of ligustrazine in the field of analgesic drugs, and particularly discloses an application of the ligustrazine in preparation of medicines for enhancing the analgesic effect of opioid agents, and delaying or relieving the opioid tolerance. The ligustrazine is matched with the opioid agents for use, or is prepared into a compound preparation together with the opioid agents for use; the analgesic time can be prolonged; the analgesic effect can be enhanced; the phenomenon of opioid tolerance caused in the treatment process of the chronic opioid agents can also be delayed or relieved; and the ligustrazine has the specific effects of inhibiting excessive activation of spinal microglia induced by the opioid agents through the ligustrazine and inhibiting realization of excessive increase p-P38 induced by opioid.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to the new use of ligustrazine 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 duratio...

Claims

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Application Information

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IPC IPC(8): A61K31/4965A61P25/04A61K31/485
Inventor 刘文涛潘彩龙韩园陈璐胡亮孔红蔡阳
Owner NANJING MEDICAL UNIV
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