Naloxone hydrochloride sublingual spraying drug delivery system or composition and its preparation method

A technology of naloxone hydrochloride tongue and naloxone hydrochloride, which is applied in the field of pharmacy, can solve the problems of large first-pass effect of the liver, influence on bioavailability, difficulty in medication for patients, etc., avoid the first-pass effect of the liver, and simple preparation process Feasible, avoiding the effects of non-compliance

Inactive Publication Date: 2007-10-24
BEIJING HUMANWELL JUNWEI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Naloxone has a rapid onset of action, reliable curative effect, and few side effects. However, due to the large first-pass effect of the liver, oral administration is ineffective. Currently, there are two dosage forms clinically used: injection and sublingual tablet. The injection is for intravenous and intramuscular injection. ...

Method used

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  • Naloxone hydrochloride sublingual spraying drug delivery system or composition and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 naloxone hydrochloride spray

[0031] Ingredients Dosage

[0032] Naloxone Hydrochloride 0.1g

[0033] Propylene glycol 1.0g

[0034] Mannitol 5.0g

[0035] Methyl-β-cyclodextrin 2.5g

[0036] Polyvinylpyrrolidone 0.5g

[0037] Sucrose 5.0g

[0038] Ethylparaben 0.05g

[0039] Preparation method: Mix the above amount of naloxone hydrochloride, propylene glycol, mannitol, methyl-β-cyclodextrin, polyvinylpyrrolidone, sucrose and ethylparaben fully to dissolve them all, and finally dilute to 100ml with distilled water , and the resulting solution was dispensed into a spray pump.

Embodiment 2

[0040] Embodiment 2 naloxone hydrochloride spray

[0041] Ingredients Dosage

[0042] Naloxone Hydrochloride 0.4g

[0043] Propylene glycol 1.0g

[0044] Mannitol 5.0g

[0045] Dimethyl-β-cyclodextrin 10g

[0046] Polyvinylpyrrolidone 0.5g

[0047] Sucrose 5.0g

[0048] Ethylparaben 0.05g

[0049] Preparation method: Mix the above-mentioned amount of naloxone hydrochloride, propylene glycol, mannitol, dimethyl-β-cyclodextrin, polyvinylpyrrolidone, sucrose and ethylparaben thoroughly to dissolve them all, and finally dilute with distilled water to 100ml, the resulting solution was dispensed into spray pumps.

Embodiment 3

[0050] Embodiment 3 naloxone hydrochloride spray

[0051] Ingredients Dosage

[0052] Naloxone Hydrochloride 0.8g

[0053] Dimethyl-β-cyclodextrin 10g

[0054] Sodium chloride 0.9g

[0055] Carbopol 1.0g

[0056] Glycerol 5.0g

[0057] Menthol 0.1g

[0058] Ethylparaben 0.05g

[0059] Preparation method: Mix the above amount of naloxone hydrochloride, dimethyl-β-cyclodextrin, sodium chloride, carbopol, glycerol, menthol and ethylparaben fully to dissolve them all, and finally use Distilled water was adjusted to 100ml, and the resulting solution was dispensed into spray pumps.

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PUM

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Abstract

The invention discloses a chlorhydric acid naloxone hypoglossal spraying drug delivery system or compound and the preparing method, belonging to pharmacology field. It is characterized in that: it is hypoglossal spraying agent, and the comprised components and their weight proportion are as follows: (1) chlorhydric acid naloxone or naloxone free alkali or naloxone medical salt: 0. 1-30%, (2) absorption promoter: 0. 5-10%; (3) osmotic pressure regulator: 0. 1 -5%; (4) bodying agent: 0. 5-30%; (5) corrigent: 0. 01-20%; (6) conservative 0. 01-0. 5%, (7) water: 45-95%. The invention is characterized by good adjustment, especially suitable for patient in comatose state; high biological utilization rate, convenient utilization. The product is characterized by stable performance, controllable quality and no stimulation to mouth mucosa.

Description

technical field [0001] The invention relates to a naloxone hydrochloride sublingual spray administration system or composition and a preparation method thereof, more precisely a sublingual spray containing naloxone hydrochloride and a preparation method thereof, belonging to the field of pharmacy. 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 could antagonize the analgesia and lethality of mice caused by oxydimorphone and the respiratory depression of rabbits, which was 7-10 times stronger than Nalorphine. Its structural formula is as follows: [0003] [0004] Molecular formula: C 19 h 21 N...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/485A61K47/10A61K47/40A61K47/34A61P25/30A61P25/32A61K47/32
Inventor 高永良刘长瑜李劲彤
Owner BEIJING HUMANWELL JUNWEI PHARM TECH CO LTD
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