N,N-二甲基甲酰胺对炔雌醚不育作用和适口性的影响

Effects of N,N-Dimethylformamide on Infertility and Palatability of Quinestrol

【目的】明确添加高效、安全的助剂N,N-二甲基甲酰胺(N,N-Dimethylformamide,DMF)对提高不育剂炔雌醚(Quinestrol)药饵的不育效果,以及改善炔雌醚药饵对鼠类适口性的作用。【方法】试验设3个处理组,分别投喂三组小鼠空白饵料(C组)、炔雌醚药饵(T1组)和DMF-炔雌醚药饵(T2组),计算饵料消耗量。将3个处理组的雄、雌鼠合笼7 d,记录雌鼠怀孕及产仔情况。高效液相色谱法检测不同配制的药饵中炔雌醚的分布浓度。【结果】T1和T2组对雄、雌鼠体重均有显著影响,且T1和T2组雄鼠肾脏器官鲜重分别低于C组16.4%和19.7%。炔雌醚对雌性小鼠繁殖抑制作用明显,T1和T2组雌鼠产仔率降低至C组的37.5%和25.0%,产仔数仅为C组的35.0%和11.1%。DMF对炔雌醚药饵适口性改善作用不明显,高效液相色谱法检测药饵中药物的分布浓度结果表明,T2组的糙米中炔雌醚的含量为T1组的1.5倍;DMF提高了炔雌醚在糙米中的渗透,从而增加了小鼠的药物摄入量。【结论】DMF可快速有效溶解炔雌醚,并增强其在糙米中的渗透力,提高炔雌醚药饵的抗生育作用,有望开发为具有良好应用前景的不育剂配方。

【Objective】The study was carried out to clear and definite that the addition of efficient and safe auxiliary N,N-Dimethylformamide(DMF)can improve the sterility of quinestrol baits,and improving the palatability of quinestrol baits to mice.【Method】The mice were divided into three groups C,T1 and T2 fed with blank bait,quinestrol bait and DMF-quinestrol bait,respectively,and the bait consumption was calculated.The male and female mice of three treatment groups were caged for 7 days,and the pregnancy and delivery of the female mice were recorded.The high-performance liquid chromatography used to detection the content of quinestrol in brown rice in the different formulations of baits【.Result】Both the T1 and T2 groups had significant effects on the body weight of male and female mice.The wet weights of the kidney organs in the T1 and T2 groups were 16.4%and 19.7%lower than the C group,respectively.Quinestrol had significant inhibitory effect on the reproduction of female mice,with the reproductive rate of female mice in T1 and T2 groups decreased to 37.5%and 25.0%of group C,and the number of litters was only 35.0%and 11.1%of group C,respectively.DMF did not significantly improve the palatability of quinestrol drug bait,but the results of high-performance liquid chromatography showed that the content of quinestrol in brown rice in the T2 group was 1.5 times higher than that in the T1 group.DMF increased the permeability of quinestrol in brown rice,thereby increasing the drug intake of mice.【Conclusion】This study shows that DMF can effectively dissolve quinestrol and enhance its permeability in brown rice,improving the contraceptive effect of quinestrol drug bait,and has the potential to be developed into a promising contraceptive formulation.