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Nalmefene hydrochloride compound and preparation method thereof

A technology of nalmefene and compound, which is applied in the field of nalmefene hydrochloride compound and its preparation, can solve problems such as toxicity, and achieve the effects of low cost, simplified quality inspection process, and easy operation

Active Publication Date: 2013-07-17
海思科制药(眉山)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Used chloroform and hexane in this method all belong to the second class solvent of ICH regulation, have certain toxicity, so there is above-mentioned problem equally

Method used

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  • Nalmefene hydrochloride compound and preparation method thereof
  • Nalmefene hydrochloride compound and preparation method thereof
  • Nalmefene hydrochloride compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Add 100.0g of nalmefene hydrochloride (HPLC content 95.16%) and 200.0ml of mixed solvent (ether: acetone: water = 4:1:1) into the three-necked flask, keep at 20-30°C, stir to dissolve nalmefene hydrochloride, Get nalmefene hydrochloride solution; add activated carbon, decolorize for 10-20 minutes, filter, wash the filter cake with a mixed solvent (ether: acetone: water = 4:1:1), collect the filtrate; naturally cool the filtrate to room temperature (15-25 ℃), so that the crystals were fully separated; the crystals were filtered with suction, and the filter cake was washed with water and dried to obtain 94.2 g of nalmefene hydrochloride. The HPLC analysis results are shown in Table 1. Powder diffraction pattern and TG-DTA differential thermal analysis see figure 1 and figure 2 .

Embodiment 2

[0026] Add 100.0g of nalmefene hydrochloride (HPLC content 95.16%) and 300.0ml of mixed solvent (ether: acetone: water = 3:1:1) into the three-necked flask, keep at 20-30°C, stir to dissolve nalmefene hydrochloride, Get nalmefene hydrochloride solution; add activated carbon, decolorize for 10-20 minutes, filter, wash the filter cake with a mixed solvent (ether: acetone: water = 3:1:1), collect the filtrate; naturally cool the filtrate to room temperature (15-25 ℃), so that the crystals were fully separated; the crystals were filtered with suction, and the filter cake was washed with water and dried to obtain 90.9 g of nalmefene hydrochloride. The HPLC analysis results are shown in Table 1. Powder diffraction pattern and TG-DTA differential thermal analysis see figure 1 and figure 2 .

Embodiment 3

[0028] Add 100.0g of nalmefene hydrochloride (HPLC content 95.16%) and 250.0ml of mixed solvent (ether: acetone: water = 5:1:1) into the three-necked flask, keep at 20-30°C, stir to dissolve nalmefene hydrochloride, Get nalmefene hydrochloride solution; add activated carbon, decolorize for 10-20 minutes, filter, wash the filter cake with a mixed solvent (ether: acetone: water = 5:1:1), collect the filtrate; naturally cool the filtrate to room temperature (15-25 ℃), so that the crystals were fully separated; the crystals were filtered with suction, and the filter cake was washed with water and dried to obtain 93.3 g of nalmefene hydrochloride. The HPLC analysis results are shown in Table 1. Powder diffraction pattern and TG-DTA differential thermal analysis see figure 1 and figure 2 .

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Abstract

The invention belongs to a technical field of medicines. Specifically, the invention relates to a nalmefene hydrochloride compound and a preparation method thereof. Nalmefene hydrochloride is a derivative of water-soluble naltrexone, and due to the chemical structure of 6-bit methylene of the nalmefene hydrochloride, the nalmefene hydrochloride has the characteristics of long action time, more medication ways, high bioavailability, less side effects, stronger physiological activity, easier biofilm penetration and the like, has different degrees of effects on keeping the normal functions of breathing, circulation, digestion, endocrine and nervous systems, and is applied to the antagonism of respiratory depression of narcotic analgesics, the treatment of heart failure and shock, the treatment of alcoholism and addiction, weight loss and the like. According to the invention, the drug stability is improved, and the medication safety is ensured.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a nalmefene hydrochloride compound and a preparation method thereof. Background technique [0002] Nalmefene hydrochloride was synthesized in 1975, CAS number: 58895‐64‐0, English name: Nalmefene hydrochloride; it is another new pure opioid receptor synthesized after naloxone (NAL) and naltrexone (NTX) antagonist. It can bind to opioid receptors μ, κ, and δ, and has the strongest binding effect on μ receptors. [0003] Nalmefene hydrochloride is a water-soluble derivative of naltrexone, its 6-methylene chemical structure makes it have a long action time, multiple drug routes, high bioavailability, less side effects, stronger physiological activity, and easier penetration Biofilm and other properties have varying degrees of effects on maintaining the normal functions of respiration, circulation, digestion, endocrine and nervous system. Currently, it has been used in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D489/08
Inventor 任东冯卫杨丽红
Owner 海思科制药(眉山)有限公司
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