Niclosamide ethanolamine salt self-emulsifying microemulsion and preparation method thereof

A technology of niclosamide ethanolamine salt and self-emulsification, which is applied in biocides, molluscicides, biocides, etc., can solve the problems of not involving the use of self-microemulsification technology, actual effect and insufficient cost of realization, and achieve formula The method is simple and feasible, it is convenient for large-scale industrial production, and the effect of increasing solubility

Active Publication Date: 2019-07-26
镇江市疾病预防控制中心 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that the above-mentioned patent involves the improvement of the dosage form of niclosamide ethanolamine salt, in order to achieve the purpose of improving drug solubility and water dispersibility, and convenient use, but there are deficiencies in actual effect and realization cost, and it does not involve the use of self-microemulsification technology to achieve the above objectives

Method used

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  • Niclosamide ethanolamine salt self-emulsifying microemulsion and preparation method thereof
  • Niclosamide ethanolamine salt self-emulsifying microemulsion and preparation method thereof
  • Niclosamide ethanolamine salt self-emulsifying microemulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] (1) Weigh 1.2 g Tween 20 and 0.6 g PEG 200, and mix them evenly under the action of magnetic stirring.

[0029] (2) Add 0.2 g of ethyl butyrate to the mixed emulsifier prepared in step (1), and mix uniformly under the action of magnetic stirring to obtain a blank self-emulsifying microemulsion.

[0030] (3) Finally, add 0.1 g of the niclosamide ethanolamine salt raw material, and stir at 100°C in a water bath until a uniform and transparent solution is formed to obtain the niclosamide ethanolamine salt self-emulsifying microemulsion.

Embodiment 2

[0032] The niclosamide ethanolamine salt self-emulsifying microemulsion prepared in Example 1 was subjected to content measurement, stability investigation, morphology, and particle size distribution measurement to further illustrate the effect of the present invention.

[0033] (1) Assay accurately weigh an appropriate amount of the test substance into a 5mL volumetric flask, dilute to the mark with methanol, vortex and mix well, filter with a 0.22μm microporous membrane, take 10μL of the continuous filtrate for HPLC determination, and calculate The content of niclosamide ethanolamine salt is 45 mg / g.

[0034] (2) Determination of cold storage and hot storage stability. According to GB / T 19137-2003 and GB / T 19136-2003, the storage stability under cold and hot conditions was measured. Take appropriate amount of niclosamide ethanolamine salt self-emulsifying microemulsion and store it at (-20±2)℃ and (54±2)℃ for 7d and 14d respectively, observe whether there is any change in appeara...

Embodiment 3

[0041] Example 3 Indoor immersion and killing experiment on snails

[0042] Refer to the requirements of "Oncomelania molluscicide efficacy test method and evaluation (NY / T 1617-2008) for pesticide registration". The niclosamide ethanolamine salt self-emulsifying microemulsion (NSM) is formulated with dechlorinated tap water to an effective concentration (calculated as niclosamide ethanolamine salt) of 0.020mg / L, 0.034mg / L, 0.058mg / L, 0.100 mg / L, 0.171mg / L, 0.292mg / L and 0.500mg / L liquid medicine. Take 500ml of each medicine solution of each concentration, pour it into a 500ml beaker, and put 3 portions of a screw bag containing 20 snails in each beaker, and make them completely immersed in the medicine solution. In the control group, 50% niclosamide ethanolamine salt wettable powder (WPN) and 25% niclosamide ethanolamine salt suspension (SCN) were operated in the same way, and dechlorinated water was set up as a blank control group.

[0043] The LC50 values ​​of NSM, WPN, and SC...

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Abstract

The invention relates to the technical field of pharmacy and particularly relates to a pesticide niclosamide ethanolamine self-emulsifying micro-emulsion for killing oncomelania and a preparation method thereof. The niclosamide ethanolamine self-emulsifying micro-emulsion provided by the invention is prepared from niclosamide ethanolamine, an oil phase, an emulsifying agent and an auxiliary emulsifying agent, wherein the mass ratio of all the components is that the niclosamide ethanolamine to the oil phase to the emulsifying agent to the auxiliary emulsifying agent is 1 to (1-15) to (5-30) to (5-20). The niclosamide ethanolamine self-emulsifying micro-emulsion has the following beneficial effects: 1, the dissolving rate of the pesticide is greatly improved and the dispersity of the pesticide in a water body system is improved; 2, the product does not contain aromatic series organic solvents, and organic solvents which seriously pollute the environments, such as N-methyl pyrrolidone, dimethylformamide and cyclohexanone, the content of effective components is high and the transportation convenience is improved; and 3, the formula and the method are simple and feasible, special equipment is not needed and the large-scale industrial production is easy to realize.

Description

Technical field [0001] The invention relates to the technical field of pharmacy, in particular to a self-emulsifying microemulsion of niclosamide ethanolamine salt used for killing oncomelania snails and a preparation method thereof. Background technique [0002] Schistosomiasis is a major zoonotic parasitic disease that seriously endangers human health. Niclosamide ethanolamine salt (NES) is the only snail-killing drug recommended by the World Health Organization. It achieves the purpose of blocking the transmission route and eliminating schistosomiasis by killing the snails, the parasite of schistosomiasis, with excellent effects. However, the solubility of the drug is only 7.8mg / L, which is a poorly soluble substance that is almost insoluble or insoluble, and its practical application is limited. In order to improve the water solubility of NES, people mix it with carriers, fillers, surfactants and other auxiliary materials to make 50% niclosamide ethanolamine salt wettable po...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01N37/40A01N25/04A01P9/00
Inventor 易承学陈宏张明辉徐虹郝世轩仲志鸿曹文婷
Owner 镇江市疾病预防控制中心
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