关键词: 2-羟丙基-β-环糊精, 左炔诺孕酮, 炔雌醚, 包合物, 布氏田鼠, 不育控制

Abstract: EP series rodent contraception is mainly composed of levonorgestrel and quinestrol. However,neither component do not readily dissolves in water,which limits the precision of research and application. In the present study, solubilization was measured in hydroxypropyl-β-cyclodextrin (HPCD) inclusion complexes of levonorgestrel and quinestrol, respectively. Afterwards,the effects of treatment times (after 2 and 4 weeks)and doses (0,1, 2, 4 mg/ kg) of EP-1 inclusion complexes on reproductive organs were investigated using a gastric gavage method. The results showed that the solubility of levonorgestrel and quinestrol reached 4 mg /mL and 0. 5 mg/ mL in 20% aqueous HPCD solution,respectively. For females, there were no significant differences after 2 or 4 weeks between the control and treatment groups that received gavage. For males,the average weight of reproductive organs of the group that received gavage for 2 weeks of 2 mg/ kg group was less than that of the control group. Our results indicate that the solubility of EP-1 was significantly enhanced by forming inclusion complexes with HPCD; the suppressive effects on reproduction in male Brandt’s voles is more obvious than those in females. Moreover,inclusion did not affect the anti-fertility effect of EP-1.

Key words: Antifertility control, HPCD, Inclusion complex, Lasiopodomys brandtii, Levonorgestrel, Quinestrol