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Nasal cavity taken drug system and combination of naloxone hydrochloride and preparation method

A technology for nasal administration of naloxone hydrochloride, which is applied in drug combinations, pharmaceutical formulations, respiratory diseases, etc., can solve the problems of affecting bioavailability, large first-pass effect of the liver, and poor user compliance, and achieve rapid absorption , controllable quality and stable performance

Inactive Publication Date: 2006-02-01
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the large first-pass effect of the liver, oral administration is ineffective. At present, there are two dosage forms in clinical use: injection and sublingual tablet. The injection is for intravenous and intramuscular injection. Professionals are required to administer the drug, and special environments and equipment are required. , the user's compliance is poor and inconvenient; buccal tablets are difficult to administer to critically ill or comatose patients, and the bioavailability is affected due to the loss of saliva when containing

Method used

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  • Nasal cavity taken drug system and combination of naloxone hydrochloride and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 Naloxone hydrochloride spray

[0024] Ingredient Amount

[0025] Naloxone Hydrochloride 80mg

[0026] Polyvinylpyrrolidone 0.5g

[0027] Laurazone 0.5ml

[0028] Propylene glycol 1.0g

[0029] Ethylparaben 0.1g

[0030] Distilled water to 100ml

[0031] Preparation method: Stir the above-mentioned amount of polyvinylpyrrolidone, naloxone hydrochloride, propylene glycol, laurozone and ethylparaben thoroughly 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

[0032] Embodiment 2 Naloxone hydrochloride spray

[0033] Naloxone Hydrochloride 80mg

[0034] Hydroxypropyl beta-cyclodextrin 2.5g

[0035] Ethylparaben 0.1g

[0036] Mannitol 0.5g

[0037] Macrogol 400 1.0ml

[0038] Distilled water to 100ml

[0039] Preparation method: Shake the above amount of naloxone hydrochloride, hydroxypropyl β-cyclodextrin, ethylparaben, mannitol and distilled water to dissolve, then add the above polyethylene glycol 400, and finally add distilled water to 100ml .

Embodiment 3

[0040] Embodiment 3 Naloxone hydrochloride spray

[0041] Naloxone Hydrochloride 160mg

[0042]Methyl beta-cyclodextrin 5g

[0043] Ethylparaben 0.1g

[0044] Polyvinyl alcohol 0.5g

[0045] Mannitol 2-4g

[0046] Distilled water to 100ml

[0047] Steaming method: add distilled water to the above amount of naloxone hydrochloride, methyl β-cyclodextrin, ethylparaben, polyvinyl alcohol, shake to dissolve all, and finally add distilled water to 100ml.

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Abstract

A nasal application system or composition of naloxone hydrochloride contains the naloxone hydrochloride or its free alkali or its other medicinal salts, absorption promoter, osmotic pressure regulator, antiseptic, and solvent or other medicinal auxiliaries. Its preparing process s also disclosed.

Description

field of invention [0001] The invention relates to a naloxone hydrochloride nasal cavity administration system or composition and a preparation method thereof. Specifically, the nasal cavity drug delivery system of the present invention includes naloxone hydrochloride or its free base or other pharmaceutically acceptable salts of naloxone, absorption accelerators, osmotic pressure regulators, preservatives, solvents or other pharmaceutical auxiliary materials. Background technique [0002] Naloxone Hydrochloride (Naloxone Hydrochloride) is a specific morphine receptor antagonist. Its affinity with opioid receptors is greater than that of morphine and enkephalin. It can competitively block and replace the binding of opioids and receptors, and clear opioid Drug intoxication symptoms, and can quickly induce withdrawal symptoms in opioid addicts. In 1961, Blumberg reported that naloxone can antagonize the analgesic and lethal effects of oxydimorphone in mice and the respiratory...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61P39/02A61P9/10A61P11/00A61P25/04
Inventor 高永良刘亚琴孙建绪李万华
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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