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利洛司酮与米非司酮均为孕酮受体拮抗剂,它们能在受体水平阻断孕酮作用而发挥催经止孕作用。本文将国产利洛司酮与米非司酮的实验药效学进行了比较性研究,结果表明:利洛司酮与米非司酮经口给药终止小鼠早孕的半数有效量即ED_50(95%可信限)分别为0.38mg/kg(0.27~0.55mg/kg)及0.67mg/kg(0.43~1.06mg/kg),两者药效有显著性差异(P<O.05);其终止大鼠早孕的ED_50(95%可信限)为1.06mg/kg(0.68~1.64mg/kg),及2.46mg/kg(1.72~3.51mg/kg),两者药效有极显著性差异(P<0.01)。此外,利洛司酮经口给药与塞普酮肌内注射给药联合应用时,终止小鼠早孕的效果呈明显的协同效应。
Both lilopristone and mifepristone are progesterone receptor antagonists, which can block the progesterone effect at the receptor level and exert their effects on the inhibition of pregnancy. In this paper, the experimental pharmacodynamics of domestic lilopristone and mifepristone were compared, the results showed that: the half effective dose of lilopristone and mifepristone oral administration termination of early pregnancy in mice that ED_50 ( 95% confidence limits) were 0.38mg / kg (0.27-0.55mg / kg) and 0.67mg / kg (0.43-1.06mg / kg), respectively. The ED_50 (95% confidence interval) for termination of early pregnancy in rats was 1.06 mg / kg (0.68-1.64 mg / kg) and 2.46 mg / kg (1.72-3.51 mg / kg) Difference (P <0.01). In addition, the combination of oral administration of lilopristone and intraperitoneal injection of plug test ketones, the termination of early pregnancy in mice showed a significant synergistic effect.