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Application of combination of imrecoxib and tramadol in preparation of medicine for treating pain

A technology of tramadol and its use, which is applied in the field of the use of the combination of Erecoxib and tramadol in the preparation of drugs for the treatment of pain, and can solve the problems of increasing the risk of tramadol addiction

Pending Publication Date: 2020-12-01
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The high concentration of M1 in the body of patients after taking tramadol greatly increases the risk of addiction when taking tramadol

Method used

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  • Application of combination of imrecoxib and tramadol in preparation of medicine for treating pain
  • Application of combination of imrecoxib and tramadol in preparation of medicine for treating pain
  • Application of combination of imrecoxib and tramadol in preparation of medicine for treating pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1. To verify the effect of the combined use of Erecoxib and tramadol on the exposure (AUC) of O-desmethyl tramadol (M1) in healthy subjects compared with single-drug tramadol.

[0076] 1. Experimental drugs

[0077] Shumin (Germany Gruntel Co., Ltd., tramadol hydrochloride sustained-release tablets, specification 100 mg), tramadol hydrochloride, and erecoxib.

[0078] 2. Experimental method

[0079] The subjects were admitted to the clinical trial ward in the afternoon of the day before the test, had a uniform light diet in the evening, and then fasted without water for 10 hours overnight. At around 8:00 the next morning, they were orally administered tramadol hydrochloride 100 mg and Erecoxib 100 mg on an empty stomach. Composition or antiseptic. Except before taking the medicine and 1 hour after taking the medicine, you can drink water as needed at other times, and eat a standard meal 4 hours after the medicine (around 12:00). During hospitalization (36 hou...

Embodiment 2

[0087] Embodiment 2, mouse acetic acid writhing model analgesic efficacy test

[0088] Male ICR mice were used as experimental animals, and the analgesic efficacy test of mouse acetic acid writhing model was carried out. Specifically: 104 male ICR mice qualified for quarantine were randomly divided into blank control group, Erecoxib nanocrystal 5, 10, 15, 30 mg / kg group, and tramadol hydrochloride 2.5, 5, 10, 15 mg / kg group. group, Erecoxib nanocrystal and tramadol hydrochloride combined group 2.5+2.5mg / kg, 5+5mg / kg, 10+10mg / kg, 15+15mg / kg group, 8 rats in each group, administration volume Both are 10ml / kg, and the solvent is 0.5% CMC-Na. After a single intragastric administration for 30 minutes, mice in each group were intraperitoneally injected with 1.5% acetic acid solution 5ml / kg to establish a model. Immediately after modeling, the number of times of writhing in mice within 20 min was recorded, and the inhibition rate was calculated (Table 3).

[0089] The preparation ...

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Abstract

The invention relates to application of combination of imrecoxib and tramadol in preparation of a medicine for treating pain. Specifically, the invention relates to application of combination of irecoxib and tramadol or pharmaceutical salts of irecoxib and tramadol in preparation of a medicine for treating pain. Specific pain may be selected from acute pain, chronic pain, neuropathic pain, nociceptive pain, slight and severe to moderate pain, hyperalgesia, pain associated with central sensitization, allodynia or cancer pain, including diabetic neuropathy and osteoarthritis, and also includingrheumatoid arthritis, ankylosing spondylitis, sciatica and frozen shoulders.

Description

technical field [0001] A use of Erecoxib or its pharmaceutically acceptable salt in combination with tramadol or its pharmaceutically acceptable salt in preparing a medicine for treating pain. Background technique [0002] Erecoxib, the chemical name is 1-n-propyl-3-(4-methylphenyl)-4-(4-methylsulfonylphenyl)-2,5-dihydro-1H-2-pyrrolone , is a listed non-steroidal anti-inflammatory drug used to relieve the symptoms of bone and joint pain. It is a highly selective cyclooxygenase-2 (Cyclooxygenase-2, COX-2) inhibitor, which inhibits the production of prostaglandins, thereby Inhibit inflammation, relieve pain, high selectivity to COX-2 and reduce the risk of adverse drug reactions in the gastrointestinal tract, its structure is shown below, [0003] [0004] Tramadol is a synthetic centrally acting analgesic drug that is clinically used to treat moderate to severe pain. It acts by activating opioid receptors and enhancing the synaptic concentration of monoamine transmitters ...

Claims

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Application Information

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IPC IPC(8): A61K31/4015A61K31/137A61P29/00A61P25/00
CPCA61K31/137A61K31/4015A61P25/00A61P29/00A61K2300/00
Inventor 许大平罗涵廖成杨昌永张连山
Owner JIANGSU HENGRUI MEDICINE CO LTD
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