论文部分内容阅读
EP系列鼠类不育剂的主要成分——左炔诺孕酮和炔雌醚在常温下难溶于水,给研究和应用造成很大不便。本研究利用2-羟丙基-β-环糊精(HPCD)提高了EP不育剂的水溶性,制备包合物;设置4个浓度梯度的EP-1包合物水溶液,分别对雌雄布氏田鼠进行灌胃,并在第2周和第4周测量繁殖器官指标,评价不育效果。结果表明,在20%的HPCD水溶液中,左炔诺孕酮和炔雌醚的溶解度分别可达约4 mg/mL和0.5 mg/mL;在第2周,2 mg/kg EP-1灌胃组雄鼠的繁殖器官受到了明显抑制,但各剂量组雌鼠未表现出明显影响。本研究结果说明,HPCD与EP-1可通过形成包合物,显著增加其常温下的溶解度;EP-1包合物对雄性布氏田鼠的繁殖器官有抑制效果,但是对雌鼠作用不明显。本研究结果表明包合作用未影响EP系列不育剂的不育效果。
Levonorgestrel and ethynylestradiol, which are the main components of EP series mouse sterilants, are hardly soluble in water at room temperature, causing great inconvenience to the research and application. In this study, 2-hydroxypropyl-β-cyclodextrin (HPCD) was used to improve the water-solubility of EP sterile agent to prepare inclusion compound. Four concentrations of EP-1 inclusion complex aqueous solution were set up, Microtus brandti was gavaged, and reproductive organ indexes were measured at weeks 2 and 4 to evaluate the infertility effects. The results showed that the solubility of levonorgestrel and ethynylestradiol was about 4 mg / mL and 0.5 mg / mL in 20% aqueous solution of HPCD respectively. In the second week, the intragastric administration of 2 mg / kg EP-1 The reproductive organs of the male rats were significantly inhibited, but the female rats in each dose group did not show significant effect. The results of this study show that HPCD and EP-1 can significantly increase their solubility at room temperature by forming an inclusion complex. EP-1 inclusion complex can inhibit the growth of male Brandt’s voles, but have no obvious effect on female rats . The results of this study show that inclusion does not affect the sterility of EP series inoculants.