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Nalmefene hydrochloride injection and preparation method thereof

A technology for nalmefene and injection, which is applied in the field of nalmefene hydrochloride injection and its preparation, can solve the problems of inability to achieve stable effects, safety, and effectiveness risks, and achieve the effects of improving stability and ensuring safety.

Active Publication Date: 2011-11-23
BEIJING SIHUAN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Chinese patent literature CN1895251A also discloses "stable nalmefene hydrochloride injection and preparation method", its core is adding inorganic antioxidants such as sodium bisulfite, sodium sulfite, pyrosulfite, vitamin C in the prescription, and adding certain The antioxidant synergist edetate disodium ethylenediaminetetraacetate disodium of a certain amount, but the stability test result that carries out by this prescription shows, can't reach the stabilizing effect of its instruction booklet, and relevant substance also has more obvious change (by 0.7% during the period of investigation) increased to 1.4%), and the pH change was also obvious (increased from 3.9 to about 5.3). Although the results did not exceed the standard, they were also close to the upper limit, and there were certain risks in the safety and effectiveness of the drug.

Method used

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  • Nalmefene hydrochloride injection and preparation method thereof
  • Nalmefene hydrochloride injection and preparation method thereof
  • Nalmefene hydrochloride injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Embodiment 1: This embodiment prepares 1000 nalmefene hydrochloride injections (specification: 1ml: 0.1mg),

[0025] Use the following ingredients:

[0026] Material name Feed amount

[0027] Nalmefene Hydrochloride 0.1108g (equivalent to Nalmefene 0.1g)

[0028] Sodium chloride 9g

[0029] tert-butylhydroxyanisole (BHA) 15mg

[0030] Add water for injection to 1000ml

[0031] Process steps: Take 15 mg of butyl hydroxyanisole (BHA) and 9 g of sodium chloride and add them to water for injection. After dissolving, adjust the pH to 3.8 with hydrochloric acid, add water for injection to 1000 ml, add 1.0 g of activated carbon, and decolorize at room temperature for 30 minutes After the decolorization is completed, filter with a 0.22 μm filter membrane, add 0.1108 g of nalmefene hydrochloride to the filtrate, stir and dissolve, filter with a 0.22 μm filter membrane, fill with nitrogen, and sterilize at 121 ° C for 20 minutes to obtain Nalmefene hydrochloride Fen injectio...

Embodiment 2

[0032] Embodiment 2: This embodiment prepares 1000 nalmefene hydrochloride injections (specification: 1ml: 0.1mg),

[0033] Use the following ingredients:

[0034] Material name Feed amount

[0035] Nalmefene Hydrochloride 0.1108g (equivalent to Nalmefene 0.1g)

[0036] Sodium chloride 9g

[0037] 2,6-di-tert-butyl-4-hydroxy-phenol (BHT) 60mg

[0038] Add water for injection to 1000ml

[0039] Process steps: Add 60mg of 2,6-di-tertiary hydroxy-p-cresol (BHT) and 9g of sodium chloride into water for injection, after dissolving, adjust the pH to 3.8 with hydrochloric acid, add water for injection to 1000ml, and add 1.0g of activated carbon , decolorize at room temperature for 30 minutes, filter with a 0.22 μm filter membrane after decolorization, add 0.1108 g of nalmefene hydrochloride to the filtrate, stir to dissolve, filter with a 0.22 μm filter membrane, fill with nitrogen, and sterilize with damp heat at 121°C for 20 minutes , to obtain nalmefene hydrochloride injectio...

Embodiment 3

[0040] Embodiment 3: This embodiment prepares 1000 nalmefene hydrochloride injections (specification: 1ml: 0.1mg), using the following ingredients:

[0041] Material name Feed amount

[0042] Nalmefene Hydrochloride 0.1108g (equivalent to Nalmefene 0.1g)

[0043] Sodium chloride 9g

[0044] Rosemary 20mg

[0045] Add water for injection to 1000ml

[0046] Process steps: Take 20mg of rosemary and 9g of sodium chloride and add them to water for injection. After dissolving, adjust the pH to 3.8 with hydrochloric acid, add water for injection to 1000ml, add 1.0g of activated carbon, and decolorize at room temperature for 30 minutes. Filter through a 0.22 μm filter, add 0.1108 g of nalmefene hydrochloride to the filtrate, stir to dissolve, filter with a 0.22 μm filter, fill with nitrogen and seal, and sterilize with damp heat at 121° C. for 20 minutes to obtain nalmefene hydrochloride injection.

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Abstract

The invention discloses a nalmefene hydrochloride injection, which is solution prepared from nalmefene hydrochloride and usable pharmaceutical excipients dissolved in injection water. The pharmaceutical excipients comprise an antioxidant and an osmotic pressure modifier. The nalmefene hydrochloride injection is characterized in that: the weight ratio of nalmefene to the antioxidant in the nalmefene hydrochloride is 1:0.1-1.0; and the antioxidant is mixed by one or more of tertiary butyl hydroxy anisole, 2,6-di-tert-butyl-4-methyl-phenol and rosemary. The injection is stable in property and ensures medication safety.

Description

technical field [0001] The invention relates to a pharmaceutical dosage form and a preparation method thereof, in particular to a nalmefene hydrochloride injection and a preparation method thereof. Background technique [0002] Nalmefene hydrochloride, synthesized in 1975, is another new pure opioid receptor antagonist synthesized after naloxone (NAL) and naltrexone (NTX). It can bind to opioid receptors μ, κ, and δ, and has the strongest binding effect on μ receptors. Nalmefene hydrochloride is a derivative of water-soluble NTX. The chemical structure of its 6-position methylene makes it show a long action time, multiple drug routes, high bioavailability, less side effects, stronger physiological activity, and easier penetration into biological Membrane and other properties have different effects on maintaining the normal functions of breathing, circulation, digestion, endocrine and nervous system. At present, it has been used in antagonism of narcotic analgesic respirator...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/485A61P9/04A61P25/30A61P3/04
Inventor 夏中宁舒军林恒庄太能
Owner BEIJING SIHUAN PHARMA
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