Naloxone hydrochloride compound with high purity

A technology for naloxone hydrochloride and crude naloxone hydrochloride, applied in the field of medicine, can solve the problems of affecting clinical application, poor purity, unqualified preparation quality, etc., and achieve the effects of low cost, improved purity, and optimized product quality

Inactive Publication Date: 2010-07-07
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There are many reports on the synthesis method of naloxone hydrochloride at home and abroad, but the purity is poor, resulting in substandard preparation quality, which affects clinical application

Method used

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  • Naloxone hydrochloride compound with high purity
  • Naloxone hydrochloride compound with high purity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The refining of embodiment 1 naloxone hydrochloride

[0029] (1) Dissolve 100g of crude naloxone hydrochloride in 1000ml of water, stir for 10 minutes, slowly add 5% sodium hydroxide solution until the pH value is 9.5, precipitate insoluble matter, stir for 20 minutes, filter, and dry under reduced pressure at 50°C , Denaloxone 75.3g;

[0030] (2) Naloxone 10g is packed into 200ml polyamide resin, at first carry out eluting with 10% aqueous ethanol (V / V), remove the first component that column elution separates, then use 80% aqueous ethanol ( V / V) further elutes again, obtains the second component, collects the second eluting component that separates most on the post;

[0031] (3) Add the collected components into 200ml of dichloromethane, add 0.3g of activated carbon, heat to 50°C, stir and adsorb for 15 minutes, filter for decarburization, and collect the filtrate;

[0032] (4) In the filtrate, the hydrochloric acid solution of 0.5mol / L is added dropwise to a pH val...

Embodiment 2

[0033] The refining of embodiment 2 naloxone hydrochloride

[0034] (1) Dissolve 100g of crude naloxone hydrochloride in 1000ml of water, stir for 10 minutes, slowly add 5% sodium hydroxide solution until the pH value is 9.5, precipitate insoluble matter, stir for 20 minutes, filter, and dry under reduced pressure at 50°C , Denaloxone 74.6g;

[0035] (2) Naloxone 15g is packed into 300ml polyamide resin, at first carry out eluting with 10% aqueous ethanol (V / V), remove the first component that column elution separates, then use 80% aqueous ethanol ( V / V) further elutes again, obtains the second component, collects the second eluting component that separates most on the post;

[0036] (3) Add the collected components into 300ml of dichloromethane, add 0.4g of activated carbon, heat to 40°C, stir and adsorb for 20 minutes, filter for decarburization, and collect the filtrate;

[0037] (4) in the filtrate, dropwise add the hydrochloric acid solution of 1.0mol / L to the pH value ...

Embodiment 3

[0038] The refining of embodiment 3 naloxone hydrochloride

[0039] (1) Dissolve 100g of crude naloxone hydrochloride in 1000ml of water, stir for 10 minutes, slowly add 5% sodium bicarbonate solution until the pH value is 10.0, precipitate insoluble matter, stir for 20 minutes, filter, and dry under reduced pressure at 50°C , Denaloxone 75.2g;

[0040] (2) Naloxone 15g is packed into 300ml polyamide resin, at first carry out eluting with 15% aqueous ethanol (V / V), remove the first component that column elution separates, then use 85% aqueous ethanol ( V / V) further elutes again, obtains the second component, collects the second eluting component that separates most on the post;

[0041] (3) Add the collected components into 300ml of dichloromethane, add 0.4g of activated carbon, heat to 40°C, stir and adsorb for 30 minutes, filter for decarburization, and collect the filtrate;

[0042](4) In the filtrate, add dropwise the hydrochloric acid solution of 2.0mol / L to the pH valu...

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Abstract

The invention relates to a naloxone hydrochloride compound, in particular to a naloxone hydrochloride compound with high purity obtained by a method, belonging to the technical field of medicine. By acid-base reaction, polyamide resin elution and activated carbon absorption, the purity of the naloxone hydrochloride is greatly improved, the product quality of preparation is optimized, and clinic pharmacy safety is ensured; and the method has the advantages of simple process, low cost and high yield, and is suitable for industrialized production.

Description

technical field [0001] The invention relates to a naloxone hydrochloride compound, through which high-purity naloxone hydrochloride can be obtained, and belongs to the technical field of medicine. Background technique [0002] Naloxone hydrochloride, chemical name: 17-allyl-4.5a-epoxy-3.14-dihydroxymorphinan-6-one hydrochloride dihydrate, molecular formula: C 19 h 21 NO 4 ·HCl·2H 2 O, molecular weight: 399.87, structural formula is as shown in following formula (I): [0003] [0004] Naloxone hydrochloride is an opioid receptor antagonist, which has almost no pharmacological activity, but can competitively antagonize various opioid receptors, and has a strong affinity for μ receptors. It is clinically used to relieve respiratory depression caused by opioid compound anesthetics after surgery, and to wake up patients, for opioid overdose, and for acute alcohol poisoning. [0005] There are many reports on the synthetic method of naloxone hydrochloride at home and abroa...

Claims

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Application Information

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IPC IPC(8): C07D491/107
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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