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A technology of nasal administration and nalmefene, which is applied in antidote, drug combination, drug delivery, etc., can solve the problem of slow onset of action, and achieve stable performance and controllable quality
Inactive Publication Date: 2019-07-02
王旭宁
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[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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[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.
[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.
[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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Abstract
The invention provides a nalmefene hydrochloride intranasal preparation comprising nalmefene hydrochloride, nalmefene free alkali or pharmaceutically acceptable other medicinal salts and absorption enhancers of nalmefene. A lot of experiments indicate that medicines of the intranasal preparation are absorbed by nasal mucosa and enter blood circulation to play roles, and the preparation has the advantages of being stable in performance, controllable in quality and non-irritating to nasal mucosa. The provided intranasal preparation can be applied to overdose anesthesia in anti-shock operations,diagnosis of morphine drug poisoning and drug reliers and prevention or treatment of stress diseases such as acute alcoholism, cerebral infarction, neonatal asphyxia and drug poisoning.
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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