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CDL (corydalmine) medicine composition for preventing and treating opioid analgesic pain relieving tolerance

An opioid drug, the technology of Corydalin, which is applied in the field of the pharmaceutical composition of Corydalin for the prevention and treatment of opioid analgesics and analgesic tolerance, can solve the problems of unpredictable, synergistic and complicated drug effects, etc. problems, to achieve the effect of enhancing analgesic effect, strong analgesic effect, and reducing opioid tolerance

Inactive Publication Date: 2016-08-24
CHINA PHARM UNIV +1
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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 use of two different drugs for the same purpose is complex and unpredictable, and may produce synergistic, additive or even antagonistic effects.

Method used

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  • CDL (corydalmine) medicine composition for preventing and treating opioid analgesic pain relieving tolerance
  • CDL (corydalmine) medicine composition for preventing and treating opioid analgesic pain relieving tolerance
  • CDL (corydalmine) medicine composition for preventing and treating opioid analgesic pain relieving tolerance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1. Corydalamine (CDL) can alleviate opioid tolerance caused by chronic administration of morphine

[0026] (1) Test animals:

[0027] Healthy female ICR mice, clean grade, weighing 18-22 g, were provided by the Animal Center of Yangzhou University. 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.

[0028] (2) Test drugs and reagents:

[0029] Morphine hydrochloride was purchased from Shenyang No. 1 Pharmaceutical Factory

[0030] (3) Test method

[0031] Dosage and method of CDL administration: CDL was dissolved in sterile saline containing 1% DMSO, the doses were 1 μg / 10 μl, 3.3 μ / g 10 μl, 10 μg / 10 μl, and th...

Embodiment 2

[0037] Example 2, Corydalis chinensis (CDL) can reduce the expression levels of p-ERK, p-p38 and p-JNK proteins up-regulated by chronic morphine tolerance

[0038] (1) Test animals:

[0039] Healthy female ICR mice, clean grade, weighing 18-22 g, were provided by the Animal Center of Yangzhou University. 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.

[0040] (2) Test drugs and reagents:

[0041] Tris, TEMED, β-Mercaptoethanol, Glycine, Tween-20SDS, 30% Acrylamide / Bis, Ammonium Persulfate, GAPDH were purchased from sigma; Marker was purchased from Thermo; bromophenol blue, glycerin, Bovine SerumAlbumin were purchased from Su...

Embodiment 3

[0046] Example 3, Corydalis dammine (CDL) can inhibit astrocytes and microglial cells activated by chronic morphine tolerance

[0047] (1) Test animals:

[0048] Healthy female ICR mice, clean grade, weighing 18-22 g, were provided by the Animal Center of Yangzhou University. 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.

[0049] (2) Test drugs and reagents:

[0050] Tris, TEMED, β-Mercaptoethanol, Glycine, Tween-20SDS, 30% Acrylamide / Bis, Ammonium Persulfate, GAPDH were purchased from sigma; Marker was purchased from Thermo; bromophenol blue, glycerin, Bovine SerumAlbumin were purchased from Sunshine; methanol, chloride S...

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Abstract

The present invention discloses the new application of Corydalis CDL (CDL) in the field of analgesic drugs, and specifically discloses the application of CDL in the preparation of drugs for preventing or treating analgesic tolerance of opioid analgesic drugs. The corydalis dammine is used in combination with opioids, or used in compound preparations with opioids, which can enhance its analgesic effect and prevent or alleviate opioid tolerance in the course of chronic opioid treatment. This effect is achieved by inhibiting opioid-induced excessive activation of spinal cord microglial cells, and inhibiting opioid-induced excessive up-regulation of p-P38, p-ERK and p-JNK.

Description

technical field [0001] The invention belongs to the field of pharmacy. Generally speaking, the invention relates to a medicine for preventing and treating the analgesic tolerance of opioid analgesics and its composition. Pharmaceutically acceptable salts thereof are used as active ingredients of opioid analgesics for the prevention and treatment of analgesic tolerance and combinations thereof, involving the preparation of the drug and its composition with the ability to enhance the analgesic effect of opioids, delay or relieve Use in the medicine of 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. In 1995, the World Pain Society proposed that pain be listed as the fifth vital sign along with heart rate, blood pressure, respiration, and body temperature. Pain is one of the most common clinical ...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61K45/06A61P29/00
CPCA61K31/4375A61K45/06
Inventor 刘吉华余伯阳洪绯戴文玲
Owner CHINA PHARM UNIV
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