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Niclosamide controlled release dispersing agent for killing blood fluke cercaria and preparation method thereof

A technology for killing schistosomiasis cercariae and niclosamide, which is applied in the field of new niclosamide controlled-release diffusion formulations, can solve the problems of difficulty in ensuring uniform release and free diffusion of active ingredients, difficulty in achieving control effects, dependence on drug efficacy release, and the like, To achieve the effect of preventing infection, good effect, scientific and reasonable ratio

Inactive Publication Date: 2011-04-27
扬州绿源生物化工有限公司 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing sustained-release agents are generally made of niclosamide wettable powder and carrier, which are physical sustained-release agents. The drug release depends on the solubility of niclosamide in water, and it is difficult to ensure the effective ingredients. Uniform release and free diffusion, it is difficult to achieve effective control effect

Method used

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  • Niclosamide controlled release dispersing agent for killing blood fluke cercaria and preparation method thereof
  • Niclosamide controlled release dispersing agent for killing blood fluke cercaria and preparation method thereof
  • Niclosamide controlled release dispersing agent for killing blood fluke cercaria and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] The final product of the present invention is a niclosamide controlled-release diffusing agent for killing schistosomiasis cercariae with an active ingredient niclosamide content in the range of 5% to 15%, and the content (percentage by weight) of each component is as follows:

[0017] Niclosamide: 5-15%

[0018] p-Dichlorobenzene: 35-45%

[0019] Floating carrier: 40-55%

[0020] Diffusion agent NNO: 2-4%. The preparation of the niclosamide controlled-release diffusion agent for killing the cercariae of schistosomiasis is carried out according to the following steps:

[0021] 1. According to the content (5-15% by weight) requirement of the finished product, the former powder of niclosamide (effective weight percentage content more than 95%) and the diffusing agent NNO weight percentage are 2-15% by weight. 4% is fully mixed, and is pulverized into niclosamide powder with a particle size passing through a 300-mesh sieve by a jet mill.

[0022] 2. The niclosamide pow...

Embodiment 2

[0030] Toxic effect of niclosamide controlled-release diffuser on cercariae: take a certain amount of 5% niclosamide controlled-release diffuser prepared in Example 1 and suspend it in dechlorinated water, measure the concentration of niclosamide released in the water , so that the final concentration of niclosamide is 0.1mg / L, 0.2mg / L, 0.3mg / L, 0.4mg / L and 0.5mg / L respectively, take 0.3mL of solutions of different concentrations in the wells of enzyme labeling strips, put 30-60 cercariae were inserted, and the mortality rate of cercariae at different times was observed under the dissecting microscope at 5, 10, 25, and 35 minutes after the cercariae were inserted. Those who lost their tails, swollen epidermis, and were inactive after being stimulated by the dissecting needle were considered dead. The above concentration tests were repeated 3 times, and dechlorinated water treatment was set up as a control. The test results show that when the concentration of niclosamide in the...

Embodiment 3

[0034] Anti-cercariae invasion test: Take 550mL of solutions of different concentrations released by 5% niclosamide controlled-release diffuser in Example 2, place them in a white disk of 23cm×15cm×5cm, the solution is about 1.6cm deep, and place them in each white disk. About 1,500 cercariae were added to the disk and mixed evenly. After 10 minutes, 10 healthy mice were put into them. After 30 minutes of infection, they were taken out and fed for 35 days. Adult schistosomes were collected and counted. The results showed that the niclosamide controlled-release diffusion agent had a significant inhibitory effect on the cercariae of Schistosoma japonicum, and when the water concentration reached 0.1 mg / L after a small amount of controlled-release diffusion agent was administered, it could significantly inhibit the infection of the cercariae to mice. Only 3 of the first mice were infected with schistosomiasis, and the number of schistosome adult worms was only 0.7 / head, far lower ...

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Abstract

The invention discloses a niclosamide controlled-release dispersing agent for killing schistosoma japonicum cercaria and a preparation method thereof. The niclosamide controlled-release dispersing agent for killing the schistosoma japonicum cercaria is characterized in that the compositions of the niclosamide controlled-release dispersing agent are niclosamide, paradichlorobenzene, floating carriers and a dispersing agent and the main compositions of the niclosamide controlled-release dispersing agent are the niclosamide and the paradichlorobenzene, wherein the weight ratio of the niclosamideto the paradichlorobenzene is between 10 and 30 to between 90 and 70. The niclosamide controlled-release dispersing agent and the preparation method have scientific and reasonable formula and ratio, advanced and simple technique and good effect of killing the schistosoma japonicum cercaria. The controlled-release dispersing agent for killing the schistosoma japonicum cercaria, which is prepared by processing the niclosamide, the paradichlorobenzene, corncob particles and so on as materials, is applied to a pathogen generation water area, releases the niclosamide at a fixed quantity in virtue of sublimation of the paradichlorobenzene, freely diffuses in virtue of the molecular tension and the function of the dispersing agent, reaches the predicted concentration in a water body, has long lasting period, effectively kills the schistosoma japonicum cercaria, and prevents the schistosoma japonicum cercaria from infecting human beings and livestock; and the death rate of the schistosoma japonicum cercaria reaches 100 percent.

Description

technical field [0001] The invention relates to a new dosage form of controlled-release diffusion of niclosamide for killing cercariae of schistosomiasis, in particular to a new dosage form of niclosamide, which uses niclosamide as the original drug, p-dichlorobenzene as the melting agent and corn cob as the floating carrier, with quantitative release, A controlled-release diffusion agent for killing schistosomiasis cercariae with the functions of free diffusion, stable floating and sustained effect and a preparation method thereof. Background technique [0002] Schistosomiasis japonicum is a zoonotic disease parasitized by Schistosoma japonicum as the pathogen, humans and animals are the final hosts, and snails are the only intermediate hosts of Schistosoma japonicum. The life cycle of schistosomiasis includes six stages: adult, egg, miracidium, sporidia, cercariae and juvenile worm. From the miracidium to the snail to the formation of the cercariae, the asexual reproducti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01N25/12A01N37/22A01P7/00
Inventor 刘琴曹国群徐健朱荫昌苏建坤
Owner 扬州绿源生物化工有限公司
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