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N-acetylcysteine oral compound emulsion

A technology of acetylcysteine ​​and emulsifier, applied in the field of N-acetylcysteine ​​oral compound emulsion, to reduce burning sensation, improve medication compliance, and reduce the number of medications

Active Publication Date: 2015-07-22
广东百澳药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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But there is no research report on oral emulsion at home and abroad

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  • N-acetylcysteine oral compound emulsion

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Effect test

Embodiment 1

[0021] A kind of N-acetyl cysteine ​​oral compound emulsion, it is prepared according to the following method:

[0022] 1) dissolving N-acetylcysteine ​​and gum arabic in warm water at 70°C to obtain an inner aqueous phase with a weight concentration of N-acetylcysteine ​​of 40% and a weight concentration of gum arabic of 1.2%;

[0023] 2) dissolving glyceryl monostearate in liquid paraffin to obtain an oil phase whose weight concentration of glyceryl monostearate is 20%;

[0024] 3) According to the weight ratio of the inner water phase and the oil phase as 1:1.8, slowly add the oil phase into the inner water phase, and stir at 70°C to prepare the N-acetylcysteine-embedded oil hydrated colostrum;

[0025] 4) Dissolve the hydrophilic emulsifier and polyvinylpyrrolidone in warm water at 50°C to obtain an external aqueous phase in which the weight concentration of the hydrophilic emulsifier is 30% and the weight concentration of polyvinylpyrrolidone is 0.3%. Agent is Tween 80 ...

Embodiment 2

[0034] A kind of N-acetyl cysteine ​​oral compound emulsion, it is prepared according to the following method:

[0035] 1) dissolving N-acetylcysteine ​​and gum arabic in warm water at 80°C to obtain an inner aqueous phase with a weight concentration of N-acetylcysteine ​​of 30% and a weight concentration of gum arabic of 2%;

[0036] 2) dissolving glyceryl monostearate in liquid paraffin to obtain an oil phase whose weight concentration of glyceryl monostearate is 10%;

[0037] 3) According to the weight ratio of the inner water phase and the oil phase as 1:1, slowly add the oil phase into the inner water phase dropwise, and stir at 80°C to prepare the N-acetylcysteine-embedded oil hydrated colostrum;

[0038] 4) Dissolve the hydrophilic emulsifier and polyvinylpyrrolidone in warm water at 40°C to obtain an external aqueous phase in which the weight concentration of the hydrophilic emulsifier is 40% and the weight concentration of polyvinylpyrrolidone is 0.5%. Agent is Twee...

Embodiment 3

[0041] A kind of N-acetyl cysteine ​​oral compound emulsion, it is prepared according to the following method:

[0042] 1) dissolving N-acetylcysteine ​​and gum arabic in warm water at 70°C to obtain an inner aqueous phase with a weight concentration of N-acetylcysteine ​​of 50% and a weight concentration of gum arabic of 0.5%;

[0043] 2) dissolving glyceryl monostearate in liquid paraffin to obtain an oil phase whose weight concentration of glyceryl monostearate is 30%;

[0044] 3) According to the weight ratio of the inner water phase and the oil phase as 1:2, slowly drop the oil phase into the inner water phase, and stir at 70°C to obtain N-acetylcysteine-embedded oil hydrated colostrum;

[0045] 4) Dissolve the hydrophilic emulsifier and polyvinylpyrrolidone in warm water at 40°C to obtain an external aqueous phase in which the weight concentration of the hydrophilic emulsifier is 20% and the weight concentration of polyvinylpyrrolidone is 0.1%. The agent is Tween 80 an...

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Abstract

The invention discloses an N-acetylcysteine oral compound emulsion. The compound emulsion is prepared according to the following steps: 1), dissolving N-acetylcysteine and Arabic gum into warm water to obtain the inner water phase; 2), dissolving a lipophilic emulsifier into liquid paraffin to obtain the oil phase; 3), dropwise adding the oil phrase into the inner water phrase, and stirring to obtain a water-in-oil preliminary emulsion; 4), dissolving a hydrophilic emulsifier and polyvinylpyrrolidone into warm water to obtain the external water phrase; 5), mixing the water-in-oil preliminary emulsion with the external water phrase in proportion, and stirring to obtain the N-acetylcysteine embedded water-in-oil compound emulsion. The compound emulsion can improve the stability of N-acetylcysteine in the body, so that the initial effect time of the drug can be prolonged, and the frequency for taking the drug can be reduced; moreover, the compound emulsion can further cover the irritation of N-acetylcysteine, so that the burning sensation and the adverse reactions, such as choking, nausea, vomiting and ozostomia, during oral administration can be reduced, and the medication compliance can be improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations and relates to an oral compound emulsion of N-acetylcysteine. Background technique [0002] N-acetylcysteine ​​is an expectorant, which has the pharmacological effect of dissolving mucus. The appearance of acetylcysteine ​​is white crystalline powder; it has an odor similar to garlic, and it tastes sour; it has hygroscopicity. Its chemical name is N-acetyl-L-cysteine ​​and its molecular formula is C 5 h 9 NO 3 S, the relative molecular mass is 163.20. The initial listing of N-acetylcysteine ​​​​is an inhalation aerosol, which is a spray in the Chinese Pharmacopoeia, and a solution in the US Pharmacopoeia. [0003] N-acetylcysteine ​​was originally considered to be ineffective orally due to its low oral bioavailability, but after years of clinical research, it has been proved that oral administration is as effective as inhalation. Currently, there are tablets, chewable tablets, efferv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/198A61K47/36A61P11/10
Inventor 袁铭
Owner 广东百澳药业有限公司
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