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Analgesic combination of sodium channel blockers with opioid antagonists

A technology of opioid receptors and derivatives, which can be used in the treatment of various diseases - especially in the application field of pain, and can solve the problems of drug resistance of analgesia, adverse reactions of patients, and limited pain relief.

Inactive Publication Date: 2008-03-26
WEX PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These drugs have limited efficacy, mainly manifested by limited pain relief and limited duration of treatment
In addition, patients often experience adverse reactions and develop resistance to the analgesic effects of these drugs

Method used

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  • Analgesic combination of sodium channel blockers with opioid antagonists
  • Analgesic combination of sodium channel blockers with opioid antagonists
  • Analgesic combination of sodium channel blockers with opioid antagonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0117] pain test

[0118] After mice were anesthetized, the sciatic nerve was exposed by blunt dissection, freeing it from the surrounding tissue. Subsequently, 4 ligatures (5-0 chrome gut, 1-2 mm apart) were performed on the sciatic nerve (Bennett and Xie, 1998). In order to obtain a satisfactory clipping effect, the standard developed by Bennett and Xie (1988) was used for operation.

[0119] In mice with ligated sciatic nerves, the mechanical pain threshold (expressed in grams (g)) was determined by the method of Randall and Selitto (1957) by gradually applying pressure to the injured innervated hind paw until retraction Foot reflexes and hissing (vocalization).

[0120]Test rats were first given naloxone or normal saline, and 15 minutes later subcutaneously injected TTX at a dose of 3 μg / kg. The administration concentration of naloxone was 0.5 mg / kg, and the rats in the control group were treated with placebo (0.09% NaCl) at the same time and environment. Each test mou...

Embodiment 2

[0124] Pain Trials Using Opioid Agonists

[0125] The treatment of the test rats was as in Example 1.

[0126] Inject morphine or saline 15 minutes before TTX. Thirty minutes after TTX injection, pressure thresholds were recorded every 30 minutes until 2 hours. The data at each time point are the mean±S.E.M of the pressure threshold of the test rats (one stress threshold per rat), as indicated in parentheses.

[0127] The concentration of morphine used was 3 mg / kg, the dose of TTX was 3 μg / kg, and the rats in the control group were treated with placebo (0.09% NaCl) at the same time and environment. Each rat received only one treatment (one compound, single dose) and was administered only once.

[0128] Data are reported as mean ± S.E.M. Non-parametric Kruskal-Wallis (1952) one-way analysis of variance (ANOVA) was used for analysis, and Mann-Whitney test was used for comparison between groups. The area under the curve (AUC) was calculated using the trapezoidal method. The...

Embodiment 3

[0131] The effect of TTX on μ-opioid receptors, especially the effect of TTX chronic in vivo administration on μ-opioid receptor signaling

[0132] The aim of the trial was to examine the effect of TTX on altered opioid receptor modulation, which is associated with opioid resistance / dependence. The test model is: ligand binding test and functional evaluation of subcellular fractions on rat brain tissue (Szucs and Coscia, 1992; Fabian et al., 2002). The effects of the drug on intracellular mu opioid receptors are described in detail.

[0133] Materials and methods

[0134] animal

[0135] Female Wistar rats, weighing about 200 g, were randomly assigned to different experimental groups, with 5 rats in each group. Rats were individually housed in small wire cages during drug treatment and maintained on a 12-h diurnal cycle, with free access to food and water during the test period. All drug treatments were completed within the same time period on the same day (7:00-8:00, 17:0...

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PUM

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Abstract

The present invention refers to a new combination of sodium channel blockers, especially Tetrodotoxin, and their derivatives with opioid antagonists, especially naloxone, according medicinal products for human and / or animal therapeutics and their use for the treatment of a variety of diseases, especially pain, preferably neuropathic pain.

Description

field of invention [0001] This invention relates to a novel combination preparation of a sodium channel blocker (especially tetrodotoxin) and its derivatives and an opioid receptor antagonist (especially naloxone), which is correspondingly used in the medical treatment of humans and / or animals Pharmaceutical products, and their use in the treatment of various diseases - especially pain, preferably neuropathic pain. Background of the invention [0002] The treatment of pain plays an important role in the field of medicine. There is a global need for new pain treatments. For several years, researchers have done a lot of work in the field of analgesics or basic research on pain in order to seek successful and satisfactory pain treatment methods, and have verified the specific treatment methods for pain in the medical field and the specific treatment methods for certain types of pain. Pain management methods are urgently needed. [0003] The International Association for the ...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/529A61K31/485A61P25/04A61P25/18A61P25/22A61P25/30
CPCA61K45/06A61K31/529A61K31/485A61P25/00A61P25/04A61P25/18A61P25/22A61P25/30A61P25/36A61K2300/00
Inventor H·H·布希曼A·费雷·格米斯M·哈蒙
Owner WEX PHARMA
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