罗格列酮在体外人灌注模型中的胎盘转运。
Placental transfer of rosiglitazone in the ex vivo human perfusion model.
作者信息
Holmes Heather J, Casey Brian M, Bawdon Roger E
机构信息
Department of Obstetrics and Gynecology, University of Texas Southwestern Medical Center at Dallas, Dallas, TX, USA.
出版信息
Am J Obstet Gynecol. 2006 Dec;195(6):1715-9. doi: 10.1016/j.ajog.2006.03.054. Epub 2006 May 16.
OBJECTIVE
The objective of the study was to determine transplacental passage of rosiglitazone (Avandia) using the ex vivo human placental model.
STUDY DESIGN
Perfusion studies were performed on 10 placentas from term, uncomplicated deliveries. Concentrations typical for an 8-mg oral dose (216 to 692 ng/mL) as well as 2- to 3-fold increased concentrations were tested (734 to 1261 ng/mL). Transfer of rosiglitazone was assessed and accumulation was determined using the 14C-antipyrine reference method.
RESULTS
The clearance index for low and high concentrations were 0.14 +/- 0.04 and 0.20 +/- 0.08, suggesting that the drug passes through the placenta at a relatively low rate. Fetal accumulation occurred in only 1 of 5 placentas at 16.4 ng/mL (5%) for the 8-mg dose and in 2 of 5 placentas ranging from 0 to 74 ng/mL (5% to 8%) at higher concentrations.
CONCLUSION
There is minimal transfer and fetal accumulation of rosiglitazone according to the ex vivo human perfusion model.
目的
本研究的目的是使用体外人胎盘模型确定罗格列酮（文迪雅）的经胎盘转运情况。
研究设计
对10例足月顺产的胎盘进行灌注研究。测试了8毫克口服剂量的典型浓度（216至692纳克/毫升）以及增加2至3倍的浓度（734至1261纳克/毫升）。使用14C-安替比林参考方法评估罗格列酮的转运并确定蓄积情况。
结果
低浓度和高浓度的清除指数分别为0.14±0.04和0.20±0.08，表明该药物经胎盘转运的速率相对较低。对于8毫克剂量，仅5个胎盘中的1个出现胎儿蓄积，浓度为16.4纳克/毫升（5%）；在较高浓度下，5个胎盘中有2个出现胎儿蓄积，浓度范围为0至74纳克/毫升（5%至8%）。
结论
根据体外人灌注模型，罗格列酮的转运和胎儿蓄积极少。
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