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.
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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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