阅读说明：本技术 环丙酰亚胺在杀钉螺药物中的应用 (Application of cyclopropylimine in oncomelania killing medicine ) 是由 邢云天 戴建荣 于 2019-10-16 设计创作，主要内容包括：本发明提供一种环丙酰亚胺在杀钉螺药物中的应用,属于血吸虫病防治技术领域。本发明以环丙酰亚胺活性成分制备杀螺剂,杀螺剂形态为悬浮剂、乳剂、微乳剂,应用于钉螺杀灭。所述环丙酰亚胺作为杀螺剂活性成分时的使用量为1.00-10.00mg/L,浸杀时间为24或48h。本发明的发明人通过实验证实,环丙酰亚胺对钉螺有杀灭活性,可以制备成杀螺制剂应用于血吸虫病防治领域。(The invention provides an application of cyclopropaneimine in oncomelania killing drugs, belonging to the technical field of schistosomiasis control. The invention uses the active component of the cyclopropane imine to prepare the molluscicide, the molluscicide takes the forms of suspending agent, emulsion and microemulsion, and is applied to killing oncomelania. The usage amount of the cyclopropanimide as the molluscicide active ingredient is 1.00-10.00mg/L, and the soaking and killing time is 24 or 48 hours. Experiments prove that the cyclopropanimide has killing activity on oncomelania, and can be prepared into a molluscicidal preparation to be applied to the field of schistosomiasis control.)

1. The application of the cyclopropanimide in preparing the oncomelania killing medicine is characterized in that: the molluscicide is prepared by taking the cyclopropaneimine as an active ingredient, and the molluscicide is selected from suspending agents, emulsions, microemulsions and granules.

2. Use of a cyclopropylimine according to claim 1 in the preparation of a oncomelania killing drug, characterized in that: the dosage of the cyclopropanimide as the molluscicide active ingredient is 1.00-10.00 mg/L.

3. Use of a cyclopropylimine according to claim 2 in the preparation of a oncomelania killing drug, characterized in that: the leaching time of the cyclopropionimide as the molluscicide active ingredient is 24 or 48 hours.

4. Use of a cyclopropylimine according to claim 1 in the preparation of a oncomelania killing drug, characterized in that: the molluscicide also comprises one or more excipients acceptable in formulation.

5. Use of a cyclopropylimine according to claim 4 in the preparation of a oncomelania killing drug, characterized in that: the auxiliary materials comprise diluents, fillers, adhesives, wetting agents, absorption promoters, surfactants, adsorption carriers and lubricants which are conventional in the field of pharmaceutical science.

Technical Field

The invention relates to a new application of cyclopropanimide, belonging to the field of schistosomiasis control.

Background

Schistosomiasis japonica is an infectious parasitic disease which seriously affects the health of people in China, is popular in 74 countries in the world and belongs to zoonosis. According to the WHO estimates that 6 million people worldwide are in a dangerous environment for schistosome infection, of which about 2 million people are infected. The Yangtze river basin and 12 provinces, direct prefectures and autonomous regions in the south of China are popular. Oncomelania hupensis is found to be the only intermediate host of Schistosoma japonicum. Molluscicidal activity is an important link in the control of schistosomiasis japonica.

The method for preventing and treating oncomelania includes environmental oncomelania killing, physical oncomelania killing, biological oncomelania killing, drug oncomelania killing and the like.

The drug has a relatively long molluscacidal effect, can determine the application range according to regions, and is a method for more molluscacidal use. At present, the method for killing snail by using a medicament commonly used at home and abroad is the chemical medicament snail killing. Sodium pentachlorophenate which is popularized and used in the past has good snail killing effect and low price, but has serious harm to human, livestock, aquatic animals and plants and serious environmental pollution, and is forbidden to be used by WHO.

Niclosamide is a chemical molluscicide still used at present, has good drug effect, but the oncomelania obviously climbs away from water after contacting with the drug, reduces the molluscicidal effect, is expensive, has high toxicity to non-target organisms, and influences the popularization and application of the drug.

Cyclopropaneimine, also known as cyclopropanoylamin, ipramine, english name: carpopamid, CAS No.104030-54-8, molecular formula C15H18CL3NO, molecular weight 334.67, pure colorless crystal, with a solubility in water of 1.9mg/l (br) at pH 7 and 20 ℃. The cyclopropanimide is a systemic and protective bactericide, is mainly used for preventing and treating rice blast of rice fields at present, and has no toxic action on rice seedlings under the recommended dosage.

WHO and China always focus on the research of molluscicidal drugs, and the molluscicide with good molluscicidal effect, low toxicity, less pollution and low price is expected to be developed. Therefore, the development of new molluscicides has wide application prospect and huge market value.

Disclosure of Invention

In view of the above-mentioned disadvantages of niclosamide in the prior art, it is an object of the present invention to provide a novel use of a cyclopropylimine for the preparation of molluscicidal drugs.

The inventor proves that the low-dose cyclopropionimide has a killing effect on oncomelania through a large number of screening experiments at the early stage, has the activity of killing the oncomelania as an intermediate host of schistosoma japonicum, and can be prepared into a molluscicide to be applied to the field of prevention and control of schistosomiasis.

If necessary, one or more auxiliary materials acceptable in the dosage form can be added into the molluscicide. The auxiliary materials comprise conventional diluents, fillers, adhesives, wetting agents, absorption promoters, surfactants, adsorption carriers, lubricants and the like in the field of pharmaceutics. The molluscicide taking the cyclopropaneimine as the active ingredient is mainly sprayed to be administrated and can be prepared into various pesticide formulations such as suspending agent, emulsion, microemulsion and the like. The various dosage forms can be prepared according to the conventional method in the field of pesticide preparation.

The invention observes the killing effect of the cyclopropionimine with different dosages on oncomelania, proves that the cyclopropionimine has obvious snail killing effect, and therefore, the cyclopropionimine can be widely applied to the field of schistosome prevention and control.

In order to achieve the above objects and other related objects, the present invention provides use of a cyclopropylimine in the preparation of a oncomelania-killing drug, characterized in that: the molluscicide is prepared by taking the cyclopropaneimine as an active ingredient, and the molluscicide is selected from suspending agents, emulsions, microemulsions and granules.

Preferably, the use amount of the cyclopropanimide for killing oncomelania is 1.00-10.00 mg/L.

Preferably, the use amount of the cyclopropanimidate for killing oncomelania is 10.00mg/L, and the soaking time is 24 or 48 hours.

Preferably, the molluscicide also comprises one or more auxiliary materials acceptable on dosage forms.

Preferably, the adjuvant includes a diluent, a filler, a binder, a wetting agent, an absorption enhancer, a surfactant, an adsorption carrier and a lubricant, which are conventional in the field of pharmaceutical formulation.

The invention has the beneficial effects that: the novel application of the cyclopropanimide is found, and the cyclopropanimide can be used for killing the snails. Simultaneously overcomes the defects of the prior medicine niclosamide, has lower price and lower toxicity to non-target organisms (particularly fishes).

Detailed Description

The following description of the embodiments of the present invention is provided for illustrative purposes, and other advantages and effects of the present invention will become apparent to those skilled in the art from the present disclosure.