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Mosquito repellent IR3535 loaded ethyl cellulose microparticles and preparation method thereof

A technology of ethyl cellulose and polyethyl cellulose, which is applied in the field of preparation of drug-loaded particles loaded with fat-soluble repellents, can solve the problems of short effective action time, bad smell, and easy absorption by the skin, etc. time, not easy to leak and deform, easy to use effect

Inactive Publication Date: 2014-03-12
SHANGHAI INST OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Compared with amide repellents, ester repellent Imonin has a good repellent effect, and its toxicity and environmental hazards are less than DEET, but it also has the problems of short effective time, easy absorption by skin and bad smell. , in order to avoid the above shortcomings, the mosquito repellent is wrapped and micronized with appropriate wall materials, thereby effectively reducing the direct contact between the mosquito repellent and the skin, reducing its transdermal absorption, and increasing the residue of the mosquito repellent on the skin time, to delay the release and evaporation of Imonin, in order to improve the mosquito repellent effect. Due to the special solubility of Imonin, there is no related report on its microparticle sustained-release preparation.

Method used

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  • Mosquito repellent IR3535 loaded ethyl cellulose microparticles and preparation method thereof
  • Mosquito repellent IR3535 loaded ethyl cellulose microparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] An ethyl cellulose microparticle loaded with mosquito repellent Imonin has a core-shell structure, the core of which is the mosquito repellent Imonin, and the shell is ethyl cellulose.

[0029] The above-mentioned preparation method of ethyl cellulose particles loaded with mosquito repellent Imonin specifically comprises the following steps:

[0030] (1) First, dissolve 0.8g of polyvinyl alcohol and 4.0g of emulsifier Tween80 in 80ml of deionized water at room temperature, and stir to fully dissolve it as the water phase;

[0031] The amount of polyvinyl alcohol, emulsifier Tween80 and water used is calculated by mass ratio, that is, polyvinyl alcohol: emulsifier Tween80: water is 0.8:4.0:80;

[0032] Then, 0.3g Immonine and 0.6g ethylcellulose, 2gspan-80 were dissolved in 20ml methyl acetate as the oil phase;

[0033] Among them, the amount of span-80, ethyl cellulose and imonin is calculated by mass ratio, that is, span-80: ethyl cellulose: imonin is 6.67: 2: 1;

[...

Embodiment 2

[0039] An ethyl cellulose microparticle loaded with mosquito repellent Imonin has a core-shell structure, the core of which is the mosquito repellent Imonin, and the shell is ethyl cellulose.

[0040] The above-mentioned preparation method of ethyl cellulose particles loaded with mosquito repellent Imonin specifically comprises the following steps:

[0041] (1) First, dissolve 1.5g of polyvinyl alcohol and 4.5g of emulsifier Tween80 in 80ml of deionized water at room temperature, and stir to fully dissolve it as the water phase;

[0042] The amount of polyvinyl alcohol, emulsifier Tween80 and water used is calculated by mass ratio, that is, polyvinyl alcohol: emulsifier Tween80: water is 1.5:4.5:80;

[0043] Then, 0.4g Immonine and 0.4g ethylcellulose, 1.5gspan-80 were dissolved in 20ml methyl acetate as the oil phase;

[0044] Among them, the amount of span-80, ethyl cellulose and imonin is calculated by mass ratio, that is, span-80: ethyl cellulose: imonin is 3.75: 1: 1;

...

Embodiment 3

[0050] An ethyl cellulose microparticle loaded with mosquito repellent Imonin has a core-shell structure, the core of which is the mosquito repellent Imonin, and the shell is ethyl cellulose.

[0051] The above-mentioned preparation method of ethyl cellulose particles loaded with mosquito repellent Imonin specifically comprises the following steps:

[0052] (1) First, dissolve 0.8g of polyvinyl alcohol and 3.0g of emulsifier Tween80 in 80ml of deionized water at room temperature, and stir to fully dissolve it as the water phase;

[0053] The amount of polyvinyl alcohol, emulsifier Tween80 and water used is calculated by mass ratio, that is, polyvinyl alcohol: emulsifier Tween80: water is 0.8:3:80;

[0054] Then, 0.6g Immonine and 0.3g ethylcellulose, 2.0gspan-80 were dissolved in 20ml methyl acetate as the oil phase;

[0055] Among them, the amount of span-80, ethyl cellulose and imonin is calculated by mass ratio, that is, span-80: ethyl cellulose: imonin is 6.67:1:2;

[00...

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Abstract

The invention discloses mosquito repellent IR3535 loaded ethyl cellulose microparticles and a preparation method thereof. The mosquito repellent IR3535 loaded ethyl cellulose microparticles have a core-shell structure in which the core is mosquito repellent IR3535 and the shell is ethyl cellulose; at 25 DEG C, the mean grain size of the mosquito repellent IR3535 loaded ethyl cellulose microparticles ranges from 500nm to 5873nm. The preparation method comprises the steps: dissolving polyvinyl alcohol and an emulsifier Tween80 in deionized water at the room temperature, and stirring so that the polyvinyl alcohol and the emulsifier Tween80 are dissolved into a water phase; dissolving the IR3535 and the ethyl cellulose and span-80 in methyl acetate to obtain a mixture as an oil phase; mixing the obtained oil phase with the water phase, homogenizing and emulsifying to obtain an emulsion; and continuing stirring at the room temperature, centrifuging after the methyl acetate volatilizes completely, thus finally, obtaining the mosquito repellent IR3535 loaded ethyl cellulose microparticles having an embedding rate ranging from 33.5% to 77.1%.

Description

technical field [0001] The invention relates to a drug-loaded particle for preparing a fat-soluble repellent, in particular to an ethyl cellulose particle loaded with a mosquito repellent Imonin and a preparation method thereof. Background technique [0002] Mosquitoes have had a huge impact on human health. Mosquito repellants are a class of substances that can make mosquitoes unable to identify and find their biting targets, so as to stay away from potential targets. With the improvement of health, environmental protection and ecological awareness, the development of mosquito repellants Research and application play an increasingly important role in daily chemical products. [0003] At present, the most widely used mosquito repellent on the market is DEET, but the repellent time of this mosquito repellent is directly related to the concentration of DEET, such as: 5-10% DEET preparation, mosquito repellent The duration of effect is 0.5-2h, and DEET with more than 20% is su...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/02A61K8/73A61K8/42A61K8/37A61Q17/02
Inventor 章苏宁
Owner SHANGHAI INST OF TECH
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