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Nose cavity administering formulation of nalmefene

A technology of nasal administration and nalmefene, which is applied in drug combinations, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problems of slow onset of action and achieve stable performance and controllable quality

Active Publication Date: 2005-07-06
广东同德药业有限公司
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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, and the onset of effect is 30 minutes after administration. max 1.5 hours or more
However, intravenous and intramuscular injections must be operated by professional medical personnel.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: Nalmefene hydrochloride spray

[0034] Ingredient Amount

[0035] Nalmefene Hydrochloride 80mg

[0036] Polyvinylpyrrolidone 0.5g

[0037] Laurazone 0.5ml

[0038] Propylene glycol 1.0g

[0039] Ethylparaben 0.1g

[0040] Distilled water to 100ml

[0041] 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

[0042] Embodiment 2: Nalmefene hydrochloride spray

[0043] Ingredient Amount

[0044] Nalmefene Hydrochloride 80mg

[0045] Hydroxypropyl-β-cyclodextrin 2.5g

[0046] Ethylparaben 0.1g

[0047]Mannitol 0.5g

[0048] Macrogol 400 1.0ml

[0049] Distilled water to 100ml

[0050] 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

[0051] Embodiment 3: Nalmefene hydrochloride spray

[0052] Ingredient Amount

[0053] Nalmefene Hydrochloride 160mg

[0054] Methyl-beta-cyclodextrin 5g

[0055] Ethylparaben 0.1g

[0056] Polyvinyl alcohol 0.5g

[0057] Mannitol 2-4g

[0058] Distilled water to 100ml

[0059] 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.

[0060] pharmacological test

[0061] Experiment 1

[0062] Implementation Benefit 1 The blood drug concentration comparison test in the beagle dog body after Namefene Hydrochloride Nasal Spray provided by the invention and Nalmefene Hydrochloride Injection administration, the results are shown in Table 1,

[0063] Table 1: Comparative test of blood concentration of nalmefene hydrochloride spray nasal and injection in Beagle dogs

[0064] Time Blood concentration ng.ml-1

[0065] (min) N...

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PUM

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Abstract

The invention provides a nalmefene preparation to be administered through nasal cavity, which comprises nalmefene, namefene free alkali or other pharmaceutically acceptable medicinal salt of nalmefene and absorption promoting agent, a large number of tests have shown that, the nasal cavity administered medicinal preparation by the invention can make the medicament absorbed through the path of nasal mucosa, and enter into blood circulation for actions. The advantages of the preparation include stabilized performance, controlled quality and non-stimulation to nasal cavity.

Description

field of invention [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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61P9/04A61P11/00A61P25/32A61P43/00
Inventor 夏敏张同祥
Owner 广东同德药业有限公司
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