Nalmefene hydrochloride nasal medicine administration preparation

A technology of nasal administration and nalmefene, which is applied in the direction of anti-toxins, pharmaceutical formulas, drug combinations, etc., can solve the problems of slow onset of action and achieve stable performance and controllable quality

Inactive Publication Date: 2017-02-01
威海恒基伟业信息科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Practice has also proved that although the nalmefene hydrochloride injection and oral preparations used clinically have a certain therapeutic effect, the onset of effect is slow,

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: Nalmefene hydrochloride spray

[0035] Ingredients

[0036] Nalmefene Hydrochloride 80mg

[0037] Polyvinylpyrrolidone 0.5g

[0038] Laurazone 0.5ml

[0039] Propylene glycol 1.0g

[0040] Ethylparaben 0.1g

[0041] Distilled water to 100ml

[0042] Preparation method: fully stir the above-mentioned amount of polyvinylpyrrolidone, nalmefene hydrochloride, propylene glycol, and lauryl nitrogen statistical ethylparaben to dissolve them all, and finally add distilled water to 100ml. The obtained solution is distributed in a spray pump or a quantitative drop pump.

Embodiment 2

[0043] Embodiment 2: Nalmefene hydrochloride spray

[0044] Ingredients

[0045] Nalmefene Hydrochloride 80mg

[0046] Hydroxypropyl-β-cyclodextrin 2.5g

[0047] Ethylparaben 0.1g

[0048] Mannitol 0.5g

[0049] Polyethylene glycol 4001.0ml

[0050] Distilled water to 100ml

[0051] Preparation method: shake the above amount of nalmefene hydrochloride, hydroxypropyl-β-cyclodextrin, ethylparaben, mannitol and distilled water to dissolve, add the above polyethylene glycol 400, and finally add distilled water to 100ml.

Embodiment 3

[0052] Embodiment 3: Nalmefene hydrochloride spray

[0053] Ingredients

[0054] Nalmefene Hydrochloride 160mg

[0055] Methyl-β-cyclodextrin 5g

[0056] Ethylparaben 0.1g

[0057] Polyvinyl alcohol 0.5g

[0058] Mannitol 2-4g

[0059] Distilled water to 100ml

[0060] Preparation method: add distilled water to the above amount of nalmefene hydrochloride, methyl-β-cyclodextrin, ethylparaben, polyvinyl alcohol, shake to dissolve all, and finally add distilled water to 100ml.

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PUM

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Abstract

The invention provides a nalmefene nasal medicine administration preparation, which is prepared from nalmefene hydrochloride, nalmefene free alkali or pharmaceutically acceptable other nalmefene pharmaceutical salts and sorbefacients. A great number of experiments show that the nasal medicine administration preparation provided by the invention realizes the medicine absorption through a tunica mucosa nasi path, and the medicine enters blood circulation to achieve the effect; the advantages of stable performance, quality controllability and no stimulation on the tunica mucosa nasi can be realized. The nasal medicine administration preparation provided by the invention belongs to the intranasal medicine administration preparation capable of being used for shock resistance, overdose anesthesia rescue in an operation, morphine medicine poisoning and drug dependence person diagnosis, and prevention or treatment on stress diseases of acute alcoholism, cerebral infarction, neonatal asphyxia, drug poisoning and the like.

Description

technical field [0001] The invention relates to a preparation for nasal cavity administration, in particular to a preparation for nasal cavity administration of nalmefene hydrochloride. Background technique [0002] Nalmefene hydrochloride (nalmefene hydrochloride) is an opioid antagonist, created by the American Ivax / Ohmeda company, and listed in the United States in 1995. It is another new pure opioid receptor antagonist synthesized after naloxone (NALOXONE) and naltrexone (Naltrexone). It can bind to opioid receptors μ, κ, and δ, and has the strongest binding effect on μ receptors. [0003] Nalmefene hydrochloride is a pure opioid receptor antagonist and a derivative of water-soluble naltrexone. Its 6-methylene chemical structure makes it exhibit stronger physiological activity and easier penetration of biological membranes. Its plasma elimination half-life (t 1 / 2 ) is 8.2-8.9h, and similar compound naltrexone (F=5%-20%, t 1 / 2 =2-5h) and naltrexone (F=0%-5%, t 1 / 2 =1...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/485A61K47/40A61P25/36A61P9/10A61P9/02A61P25/32A61P11/00A61P39/02A61P25/30
CPCA61K9/12A61K9/0043A61K31/485A61K47/40
Inventor 蔡颖
Owner 威海恒基伟业信息科技发展有限公司
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