Hui Julia Y, Hoffmann Matthew, Kumar Gondi
Celgene Corporation, 86 Morris Avenue, Summit, NJ 07901, USA.
Celgene Corporation, 86 Morris Avenue, Summit, NJ 07901, USA.
Reprod Toxicol. 2014 Sep;48:115-23. doi: 10.1016/j.reprotox.2014.05.002. Epub 2014 May 22.
Studies in pregnant rabbits were conducted to evaluate if there are any differences in the uptake of thalidomide into the intrauterine compartment and developmental toxicity risk following oral and intravaginal administration. Thalidomide concentrations in maternal plasma, yolk sac cavity (YSC) fluid and embryo following intravaginal administration were 2- to 7-fold lower than their respective levels after oral administration. Ratios of thalidomide concentration in YSC fluid to maternal plasma were similar between these two routes, indicating no difference in uptake into the intrauterine compartment. A rabbit embryo-fetal development study using oral and intravaginal thalidomide administration at 2mg/kg/day (a dose >10,000-fold higher than the expected amount of thalidomide in human semen) did not result in any developmental abnormalities. These data demonstrated no preferential transfer mechanism of thalidomide from vagina to conceptus, and no additional embryo-fetal developmental toxicity risks with thalidomide exposure via the vaginal route.
开展了对怀孕兔子的研究,以评估口服和经阴道给药后,沙利度胺进入子宫内环境的摄取情况及发育毒性风险是否存在差异。经阴道给药后,母体血浆、卵黄囊腔(YSC)液和胚胎中的沙利度胺浓度比口服给药后的各自水平低2至7倍。这两种给药途径下,YSC液中沙利度胺浓度与母体血浆浓度的比值相似,表明进入子宫内环境的摄取情况没有差异。一项使用口服和经阴道给予沙利度胺(剂量为2mg/kg/天,比人类精液中预期的沙利度胺量高10000倍以上)的兔子胚胎-胎儿发育研究未导致任何发育异常。这些数据表明,沙利度胺不存在从阴道到胎儿的优先转运机制,且经阴道途径接触沙利度胺不会增加胚胎-胎儿发育毒性风险。