Cyclodextrin inclusion compound of rodents sterilant and preparation method thereof

A cyclodextrin inclusion complex and cyclodextrin technology, applied in the field of medicine, can solve the problems of difficult accurate quantification, limited research, and affect the palatability of bait, and achieve the effects of good UV stability and poor water solubility.

Inactive Publication Date: 2010-10-27
INST OF PLANT PROTECTION CHINESE ACAD OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the water solubility of the main sterile agents developed and applied in my country's market is generally poor.
In quantitative drug efficacy experiments, it can only be used as a suspension with water, which is difficult to quantify accurately, and the use of organic solvents as solvents will limit some research, such as behavioral tests.
In addition, in actual production, the sterilant is often directly attached to the surface of wheat and other base baits, which will not only affect the palatability of the bait, but also be easily exposed to sunlight in the field release, resulting in accelerated degradation of the sterilant, affecting the quality of the drug. The infertility effect and duration of action

Method used

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  • Cyclodextrin inclusion compound of rodents sterilant and preparation method thereof
  • Cyclodextrin inclusion compound of rodents sterilant and preparation method thereof
  • Cyclodextrin inclusion compound of rodents sterilant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Weigh 10g of hydroxypropyl-β-cyclodextrin (HP-β-CD) and dissolve it in water to make a saturated solution. The temperature of the water bath is controlled at 50°C. According to the mass of levonorgestrel (LNG) and HP-β-CD The ratio is 1:50, and the ethanol solution of levonorgestrel is slowly added dropwise. The solution was continuously stirred on a magnetic stirrer at a constant temperature for 15 h under the conditions of feeding nitrogen and protecting from light, and filtered through a microporous membrane. The filtrate was left to stand in an ice bath for 12 h to crystallize, filtered, and the crystals were washed twice with water and acetone respectively. Vacuum drying to constant weight finally gives white crystal powder, which is the HP-β-CD clathrate of levonorgestrel, and its degradation rate under ultraviolet light is as follows: Figure 1A As shown, the UV stability was significantly improved.

Embodiment 2

[0022] Take by weighing 10g methyl-β-cyclodextrin (M-β-CD) and dissolve in water to make a saturated solution, at room temperature press the mass ratio of levonorgestrel and M-β-CD to be 1: 100, slowly A solution of levonorgestrel in ethyl acetate was added dropwise. Stirring was continued on a magnetic stirrer for 10 h, filtered through a microporous membrane, and the crystals were washed twice with water and acetone respectively. Vacuum-dried to constant weight, finally obtained the white crystal powder of the M-β-CD clathrate of levonorgestrel, and its degradation rate under ultraviolet light is as follows: Figure 1B As shown, the UV stability was significantly improved.

Embodiment 3

[0024] Weigh 10g of β-cyclodextrin (β-CD) and dissolve it in water to make a saturated solution. The temperature of the water bath is controlled at 60°C. According to the mass of ethinylestradiol and β-CD at 1:200, slowly add mouse sterile ethanol solution of the agent. Stirring was continued on a magnetic stirrer for 24 h, filtered with a microporous membrane, and the crystals were washed twice with water and acetone respectively. Vacuum-dried to constant weight, finally obtained the white crystal powder of the β-CD clathrate of ethinylestradiol, and its degradation rate under ultraviolet light was as follows: Figure 1C As shown, the UV stability was significantly improved.

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Abstract

The invention relates to the field of medicaments, in particular to a cyclodextrin inclusion compound of a rodents sterilant and a preparation method thereof. By the method, the rodents sterilant is mixed with cyclodextrin or a derivative of the cyclodextrin in a mass ratio of 1:1-200 to prepare the inclusion compound. The obtained inclusion compound not only has high water solubility, but also has a high ultraviolet stability. The invention initially provides the cyclodextrin inclusion compound of the rodents sterilant. The cyclodextrin inclusion compound has a tubular structure formed by glucosamine residues to form a unique conformation which is externally hydrophilic and internally hydrophobic, and can form a compound supramolecular system with an indissolvable compound to play a solubilization role and solve the problem of low water solubility of the conventional rodents sterilant; moreover, the inclusion compound has the high ultraviolet stability to meet the requirement of field administration; in addition, the cyclodextrin compound has no toxicity or low toxicity and is a good carrier for performing a medicinal effect research.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a cyclodextrin inclusion compound of a mouse sterility agent and a preparation method thereof. Background technique [0002] Rodent infestation has become a major problem threatening the world's food security and hindering the sustainable development of agriculture. In my country, about 5-10 million tons of grain are lost each year due to rodent infestation, the forestry damage area is about 10 million mu, the grassland damage area is about 600 million mu, and the direct economic loss can reach nearly 10 billion yuan. The main reason for the plague of rodents is the vigorous fecundity and strong environmental adaptability of rodents, which also make them the most diverse, largest and most widely distributed group of mammals. Not only that, with global warming and the acceleration of modernization, the ecological environment is under tremendous pressure, and extreme weather occurs freque...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N45/00A01N31/00A01N43/90A01N43/16A01P23/00
Inventor 王大伟刘晓辉刘琪刘明李宁
Owner INST OF PLANT PROTECTION CHINESE ACAD OF AGRI SCI
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